Details
| Stereochemistry | ABSOLUTE |
| Molecular Formula | 2C22H30N6OS.5BrH |
| Molecular Weight | 1257.716 |
| Optical Activity | UNSPECIFIED |
| Defined Stereocenters | 4 / 4 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
Br.Br.Br.Br.Br.CC1=NN(C(=C1)N2CCN(CC2)[C@@H]3CN[C@@H](C3)C(=O)N4CCSC4)C5=CC=CC=C5.CC6=NN(C(=C6)N7CCN(CC7)[C@@H]8CN[C@@H](C8)C(=O)N9CCSC9)C%10=CC=CC=C%10
InChI
InChIKey=LUXIOMHUGCXFIU-MAYGPZJUSA-N
InChI=1S/2C22H30N6OS.5BrH/c2*1-17-13-21(28(24-17)18-5-3-2-4-6-18)26-9-7-25(8-10-26)19-14-20(23-15-19)22(29)27-11-12-30-16-27;;;;;/h2*2-6,13,19-20,23H,7-12,14-16H2,1H3;5*1H/t2*19-,20-;;;;;/m00...../s1
| Molecular Formula | C22H30N6OS |
| Molecular Weight | 426.578 |
| Charge | 0 |
| Count |
|
| Stereochemistry | ABSOLUTE |
| Additional Stereochemistry | No |
| Defined Stereocenters | 2 / 2 |
| E/Z Centers | 0 |
| Optical Activity | UNSPECIFIED |
| Molecular Formula | BrH |
| Molecular Weight | 80.912 |
| Charge | 0 |
| Count |
|
| Stereochemistry | ACHIRAL |
| Additional Stereochemistry | No |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Optical Activity | NONE |
DescriptionCurator's Comment: description was created based on several sources, including https://www.pmda.go.jp/files/000153594.pdf
Curator's Comment: description was created based on several sources, including https://www.pmda.go.jp/files/000153594.pdf
Teneligliptin is a DPP IV inhibitor which was developed by Mitsubishi Tanabe Pharma and now is used for the treatment of type 2 diabetes mellitus in Asia under the name Tenelia.
Approval Year
Cmax
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
236.2 ng/mL |
20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered: |
TENELIGLIPTIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
187.5 ng/mL |
20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered: |
TENELIGLIPTIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED |
|
13.9 ng/mL |
2.5 mg single, oral dose: 2.5 mg route of administration: Oral experiment type: SINGLE co-administered: |
TENELIGLIPTIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
77.22 ng/mL |
10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered: |
TENELIGLIPTIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
187.2 ng/mL |
20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered: |
TENELIGLIPTIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
382.4 ng/mL |
40 mg single, oral dose: 40 mg route of administration: Oral experiment type: SINGLE co-administered: |
TENELIGLIPTIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
955.77 ng/mL |
80 mg single, oral dose: 80 mg route of administration: Oral experiment type: SINGLE co-administered: |
TENELIGLIPTIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
2107.83 ng/mL |
160 mg single, oral dose: 160 mg route of administration: Oral experiment type: SINGLE co-administered: |
TENELIGLIPTIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
420.67 ng/mL |
40 mg single, oral dose: 40 mg route of administration: Oral experiment type: SINGLE co-administered: |
TENELIGLIPTIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED |
|
160.6 ng/mL |
20 mg 1 times / day multiple, oral dose: 20 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
TENELIGLIPTIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
220.14 ng/mL |
20 mg 1 times / day multiple, oral dose: 20 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
TENELIGLIPTIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
926.73 ng/mL |
80 mg 1 times / day multiple, oral dose: 80 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
TENELIGLIPTIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
1180.9 ng/mL |
80 mg 1 times / day multiple, oral dose: 80 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
TENELIGLIPTIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
176.5 ng/mL |
20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered: |
TENELIGLIPTIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
208 ng/mL |
20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered: |
TENELIGLIPTIN plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
203.6 ng/mL |
20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered: |
TENELIGLIPTIN plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
191.6 ng/mL |
20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered: |
TENELIGLIPTIN plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
195.8 ng/mL |
20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered: |
TENELIGLIPTIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
219 ng/mL |
20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered: |
TENELIGLIPTIN plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
164.5 ng/mL |
20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered: |
TENELIGLIPTIN plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
185.9 ng/mL |
20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered: |
TENELIGLIPTIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
229.3 ng/mL |
20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered: |
TENELIGLIPTIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
247.6 ng/mL |
20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered: |
TENELIGLIPTIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
AUC
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
1861.1 ng × h/mL |
20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered: |
TENELIGLIPTIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
1814.6 ng × h/mL |
20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered: |
TENELIGLIPTIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED |
|
298 ng × h/mL |
2.5 mg single, oral dose: 2.5 mg route of administration: Oral experiment type: SINGLE co-administered: |
TENELIGLIPTIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
876.9 ng × h/mL |
10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered: |
TENELIGLIPTIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
2028.9 ng × h/mL |
20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered: |
TENELIGLIPTIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
3705.1 ng × h/mL |
40 mg single, oral dose: 40 mg route of administration: Oral experiment type: SINGLE co-administered: |
TENELIGLIPTIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
7649.7 ng × h/mL |
80 mg single, oral dose: 80 mg route of administration: Oral experiment type: SINGLE co-administered: |
TENELIGLIPTIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
18180.6 ng × h/mL |
160 mg single, oral dose: 160 mg route of administration: Oral experiment type: SINGLE co-administered: |
TENELIGLIPTIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
3613.5 ng × h/mL |
40 mg single, oral dose: 40 mg route of administration: Oral experiment type: SINGLE co-administered: |
TENELIGLIPTIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED |
|
1057.2 ng × h/mL |
20 mg 1 times / day multiple, oral dose: 20 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
TENELIGLIPTIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
1514.6 ng × h/mL |
20 mg 1 times / day multiple, oral dose: 20 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
TENELIGLIPTIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
5257.7 ng × h/mL |
80 mg 1 times / day multiple, oral dose: 80 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
TENELIGLIPTIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
7292.2 ng × h/mL |
80 mg 1 times / day multiple, oral dose: 80 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
TENELIGLIPTIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
1772.7 ng × h/mL |
20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered: |
TENELIGLIPTIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
2234.2 ng × h/mL |
20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered: |
TENELIGLIPTIN plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
3090.3 ng × h/mL |
20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered: |
TENELIGLIPTIN plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
2833.3 ng × h/mL |
20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered: |
TENELIGLIPTIN plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
1843.1 ng × h/mL |
20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered: |
TENELIGLIPTIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
2472.9 ng × h/mL |
20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered: |
TENELIGLIPTIN plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
2162.5 ng × h/mL |
20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered: |
TENELIGLIPTIN plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
1548.8 ng × h/mL |
20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered: |
TENELIGLIPTIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
2207.9 ng × h/mL |
20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered: |
TENELIGLIPTIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
2418.9 ng × h/mL |
20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered: |
TENELIGLIPTIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
T1/2
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
27.8 h |
20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered: |
TENELIGLIPTIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
28.3 h |
20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered: |
TENELIGLIPTIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED |
|
31.4 h |
2.5 mg single, oral dose: 2.5 mg route of administration: Oral experiment type: SINGLE co-administered: |
TENELIGLIPTIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
25.7 h |
10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered: |
TENELIGLIPTIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
24.2 h |
20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered: |
TENELIGLIPTIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
20.8 h |
40 mg single, oral dose: 40 mg route of administration: Oral experiment type: SINGLE co-administered: |
TENELIGLIPTIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
24.8 h |
80 mg single, oral dose: 80 mg route of administration: Oral experiment type: SINGLE co-administered: |
TENELIGLIPTIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
23.5 h |
160 mg single, oral dose: 160 mg route of administration: Oral experiment type: SINGLE co-administered: |
TENELIGLIPTIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
27.5 h |
40 mg single, oral dose: 40 mg route of administration: Oral experiment type: SINGLE co-administered: |
TENELIGLIPTIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED |
|
25.8 h |
20 mg 1 times / day multiple, oral dose: 20 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
TENELIGLIPTIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
30.2 h |
20 mg 1 times / day multiple, oral dose: 20 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
TENELIGLIPTIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
17.6 h |
80 mg 1 times / day multiple, oral dose: 80 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
TENELIGLIPTIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
23.7 h |
80 mg 1 times / day multiple, oral dose: 80 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
TENELIGLIPTIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
26.1 h |
20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered: |
TENELIGLIPTIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
27.7 h |
20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered: |
TENELIGLIPTIN plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
36 h |
20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered: |
TENELIGLIPTIN plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
29.8 h |
20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered: |
TENELIGLIPTIN plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
18.3 h |
20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered: |
TENELIGLIPTIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
23.6 h |
20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered: |
TENELIGLIPTIN plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
22.7 h |
20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered: |
TENELIGLIPTIN plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
24.8 h |
20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered: |
TENELIGLIPTIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
27.9 h |
20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered: |
TENELIGLIPTIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
30.9 h |
20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered: |
TENELIGLIPTIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
Funbound
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
17.8% |
TENELIGLIPTIN plasma | Homo sapiens |
Doses
| Dose | Population | Adverse events |
|---|---|---|
40 mg 1 times / day multiple, oral Recommended Dose: 40 mg, 1 times / day Route: oral Route: multiple Dose: 40 mg, 1 times / day Sources: |
healthy, ADULT Health Status: healthy Age Group: ADULT Sex: M+F Food Status: FED Sources: |
Disc. AE: Vomiting... AEs leading to discontinuation/dose reduction: Vomiting (grade 3, 5%) Sources: |
AEs
| AE | Significance | Dose | Population |
|---|---|---|---|
| Vomiting | grade 3, 5% Disc. AE |
40 mg 1 times / day multiple, oral Recommended Dose: 40 mg, 1 times / day Route: oral Route: multiple Dose: 40 mg, 1 times / day Sources: |
healthy, ADULT Health Status: healthy Age Group: ADULT Sex: M+F Food Status: FED Sources: |
PubMed
| Title | Date | PubMed |
|---|---|---|
| Comparative Binding Analysis of Dipeptidyl Peptidase IV (DPP-4) with Antidiabetic Drugs - An Ab Initio Fragment Molecular Orbital Study. | 2016 |
|
| Teneligliptin, a Dipeptidyl Peptidase-4 Inhibitor, Improves Early-Phase Insulin Secretion in Drug-Naïve Patients with Type 2 Diabetes. | 2015-09 |
|
| Teneligliptin improves glycemic control with the reduction of postprandial insulin requirement in Japanese diabetic patients. | 2015 |
|
| Add-on treatment with teneligliptin ameliorates glucose fluctuations and improves glycemic control index in Japanese patients with type 2 diabetes on insulin therapy. | 2014-12 |
|
| Teneligliptin as an initial therapy for newly diagnosed, drug naive subjects with type 2 diabetes. | 2014-08 |
|
| Efficacy and safety of teneligliptin in combination with pioglitazone in Japanese patients with type 2 diabetes mellitus. | 2013-11-27 |
|
| Efficacy, safety and dose-response relationship of teneligliptin, a dipeptidyl peptidase-4 inhibitor, in Japanese patients with type 2 diabetes mellitus. | 2013-09 |
|
| Teneligliptin: a DPP-4 inhibitor for the treatment of type 2 diabetes. | 2013 |
|
| Discovery and preclinical profile of teneligliptin (3-[(2S,4S)-4-[4-(3-methyl-1-phenyl-1H-pyrazol-5-yl)piperazin-1-yl]pyrrolidin-2-ylcarbonyl]thiazolidine): a highly potent, selective, long-lasting and orally active dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes. | 2012-10-01 |
Sample Use Guides
The usual adult dosage is 20 mg of teneligliptin administered orally once daily. If efficacy is insufficient, the dose may be increased up to 40 mg once daily while closely monitoring the clinical course.
Route of Administration:
Oral
Human umbilical vein endothelial cells were cultured under normal (5 mmol/L) or high glucose level (25 mmol/L) during 21 days, or at high glucose during 14 days followed by 7 days at normal glucose, to reproduce the high-metabolic memory state. At this time, different concentrations of teneligliptin (0.1, 1.0 and 3.0 umol/L) were added to cells. Teneligliptin was shown to protect human umbilical vein endothelial cells from oxidative stress.
| Substance Class |
Chemical
Created
by
admin
on
Edited
Mon Mar 31 19:10:30 GMT 2025
by
admin
on
Mon Mar 31 19:10:30 GMT 2025
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| Record UNII |
556RZT8JPF
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| Record Status |
Validated (UNII)
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| Record Version |
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906093-29-6
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556RZT8JPF
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11996485
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DTXSID90238219
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SOLVATE->ANHYDROUS |
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PARENT -> SALT/SOLVATE |
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ACTIVE MOIETY |