Details
| Stereochemistry | ABSOLUTE |
| Molecular Formula | C16H14N2O3.C6H14N2O2 |
| Molecular Weight | 428.4815 |
| Optical Activity | UNSPECIFIED |
| Defined Stereocenters | 1 / 1 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
NCCCC[C@H](N)C(O)=O.OC(=O)COC1=NN(CC2=CC=CC=C2)C3=C1C=CC=C3
InChI
InChIKey=OCOCFNMFLNFNIA-ZSCHJXSPSA-N
InChI=1S/C16H14N2O3.C6H14N2O2/c19-15(20)11-21-16-13-8-4-5-9-14(13)18(17-16)10-12-6-2-1-3-7-12;7-4-2-1-3-5(8)6(9)10/h1-9H,10-11H2,(H,19,20);5H,1-4,7-8H2,(H,9,10)/t;5-/m.0/s1
| Molecular Formula | C16H14N2O3 |
| Molecular Weight | 282.294 |
| Charge | 0 |
| Count |
|
| Stereochemistry | ACHIRAL |
| Additional Stereochemistry | No |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Optical Activity | NONE |
| Molecular Formula | C6H14N2O2 |
| Molecular Weight | 146.1876 |
| Charge | 0 |
| Count |
|
| Stereochemistry | ABSOLUTE |
| Additional Stereochemistry | No |
| Defined Stereocenters | 1 / 1 |
| E/Z Centers | 0 |
| Optical Activity | UNSPECIFIED |
DescriptionCurator's Comment: description was created based on several sources, including:
http://database.japic.or.jp/pdf/newPINS/00056628.pdf
http://www.kegg.jp/medicus-bin/japic_med?japic_code=00056628
http://www.ncbi.nlm.nih.gov/pubmed/5317253
Curator's Comment: description was created based on several sources, including:
http://database.japic.or.jp/pdf/newPINS/00056628.pdf
http://www.kegg.jp/medicus-bin/japic_med?japic_code=00056628
http://www.ncbi.nlm.nih.gov/pubmed/5317253
Bendazac, (1-benzyl-1H-indazol-3-yl-oxy)-acetic acid, is structurally related to indomethacin. Its lysine salt has been reported to be absorbed better than the parent compound. It is applied topically as bendazac lysine 0.5% (wt/vol) aqueous solution for delaying the progression of cataract. Topical application of bendazac is associated with transient burning sensation. It reduces the secretion of the skin ulcer surface, promotes skin formation and accelerates tissue repair.
Approval Year
Targets
| Primary Target | Pharmacology | Condition | Potency |
|---|---|---|---|
Target ID: reactive oxygen species |
|||
Target ID: CHEMBL1075246 |
0.33 mM [Ki] |
Conditions
| Condition | Modality | Targets | Highest Phase | Product |
|---|---|---|---|---|
| Primary | Zildasac Ointment Approved UseIndications: Pressure sores, burns ulcers, radiation ulcers;
Contact dermatitis, acute eczema, atopic dermatitis, chronic eczema, psoriasis vulgaris, infant eczema, herpes zoster |
|||
| Primary | Zildasac Ointment Approved UseIndications: Pressure sores, burns ulcers, radiation ulcers;
Cntact dermatitis, acute eczema, atopic dermatitis, chronic eczema, psoriasis vulgaris, infant eczema, herpes zoster |
|||
| Primary | Zildasac Ointment Approved UseIndications: Pressure sores, burns ulcers, radiation ulcers;
Cntact dermatitis, acute eczema, atopic dermatitis, chronic eczema, psoriasis vulgaris, infant eczema, herpes zoster |
|||
| Primary | Zildasac Ointment Approved UseIndications: Pressure sores, burns ulcers, radiation ulcers;
Cntact dermatitis, acute eczema, atopic dermatitis, chronic eczema, psoriasis vulgaris, infant eczema, herpes zoster |
|||
| Palliative | Zildasac Ointment Approved UseIndications: Pressure sores, burns ulcers, radiation ulcers;
Cntact dermatitis, acute eczema, atopic dermatitis, chronic eczema, psoriasis vulgaris, infant eczema, herpes zoster |
|||
| Primary | BENDAZAC LYSINE Approved UseAdjuvant in the treatment of cataracts (cataract degenerative presenile and senile, juvenile cataracts, diabetic cataract, opacification of the cortex or the crystalline core of different origin and nature) |
Cmax
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
41.9 mg/L EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/3197747/ |
500 mg single, oral dose: 500 mg route of administration: Oral experiment type: SINGLE co-administered: |
BENDAZAC plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
36.4 mg/L EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/3197747/ |
500 mg single, oral dose: 500 mg route of administration: Oral experiment type: SINGLE co-administered: |
BENDAZAC plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
41.9 mg/L EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/3691618/ |
500 mg single, oral dose: 500 mg route of administration: Oral experiment type: SINGLE co-administered: |
BENDAZAC plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
27.6 mg/L EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/3691618/ |
500 mg single, oral dose: 500 mg route of administration: Oral experiment type: SINGLE co-administered: |
BENDAZAC plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
31.2 mg/L EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/3691618/ |
500 mg single, oral dose: 500 mg route of administration: Oral experiment type: SINGLE co-administered: |
BENDAZAC plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
25.5 mg/L EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/3691618/ |
500 mg single, oral dose: 500 mg route of administration: Oral experiment type: SINGLE co-administered: |
BENDAZAC plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
AUC
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
159 mg × h/L EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/3197747/ |
500 mg single, oral dose: 500 mg route of administration: Oral experiment type: SINGLE co-administered: |
BENDAZAC plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
339 mg × h/L EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/3197747/ |
500 mg single, oral dose: 500 mg route of administration: Oral experiment type: SINGLE co-administered: |
BENDAZAC plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
159 mg × h/L EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/3691618/ |
500 mg single, oral dose: 500 mg route of administration: Oral experiment type: SINGLE co-administered: |
BENDAZAC plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
150 mg × h/L EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/3691618/ |
500 mg single, oral dose: 500 mg route of administration: Oral experiment type: SINGLE co-administered: |
BENDAZAC plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
149 mg × h/L EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/3691618/ |
500 mg single, oral dose: 500 mg route of administration: Oral experiment type: SINGLE co-administered: |
BENDAZAC plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
84 mg × h/L EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/3691618/ |
500 mg single, oral dose: 500 mg route of administration: Oral experiment type: SINGLE co-administered: |
BENDAZAC plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
T1/2
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
3.5 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/3197747/ |
500 mg single, oral dose: 500 mg route of administration: Oral experiment type: SINGLE co-administered: |
BENDAZAC plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
8 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/3197747/ |
500 mg single, oral dose: 500 mg route of administration: Oral experiment type: SINGLE co-administered: |
BENDAZAC plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
3.5 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/3691618/ |
500 mg single, oral dose: 500 mg route of administration: Oral experiment type: SINGLE co-administered: |
BENDAZAC plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
4.7 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/3691618/ |
500 mg single, oral dose: 500 mg route of administration: Oral experiment type: SINGLE co-administered: |
BENDAZAC plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
3.8 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/3691618/ |
500 mg single, oral dose: 500 mg route of administration: Oral experiment type: SINGLE co-administered: |
BENDAZAC plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
3.1 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/3691618/ |
500 mg single, oral dose: 500 mg route of administration: Oral experiment type: SINGLE co-administered: |
BENDAZAC plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
Funbound
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
1% EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/3197747/ |
BENDAZAC plasma | Homo sapiens |
||
0.4% EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/3691618/ |
500 mg single, oral dose: 500 mg route of administration: Oral experiment type: SINGLE co-administered: |
BENDAZAC plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
0.8% EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/3691618/ |
500 mg single, oral dose: 500 mg route of administration: Oral experiment type: SINGLE co-administered: |
BENDAZAC plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
0.7% EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/3691618/ |
500 mg single, oral dose: 500 mg route of administration: Oral experiment type: SINGLE co-administered: |
BENDAZAC plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
1% EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/3691618/ |
500 mg single, oral dose: 500 mg route of administration: Oral experiment type: SINGLE co-administered: |
BENDAZAC plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
Doses
| Dose | Population | Adverse events |
|---|---|---|
500 mg 3 times / day multiple, oral Studied dose Dose: 500 mg, 3 times / day Route: oral Route: multiple Dose: 500 mg, 3 times / day Sources: |
unhealthy |
Disc. AE: Hepatotoxicity... AEs leading to discontinuation/dose reduction: Hepatotoxicity (2 patients) Sources: |
AEs
| AE | Significance | Dose | Population |
|---|---|---|---|
| Hepatotoxicity | 2 patients Disc. AE |
500 mg 3 times / day multiple, oral Studied dose Dose: 500 mg, 3 times / day Route: oral Route: multiple Dose: 500 mg, 3 times / day Sources: |
unhealthy |
PubMed
| Title | Date | PubMed |
|---|---|---|
| Antidenaturant drugs for cataract and other condensation diseases. | 2001 Jan |
|
| Advances in pharmacological strategies for the prevention of cataract development. | 2009 May-Jun |
|
| Synthesis and biological evaluations of novel bendazac lysine analogues as potent anticataract agents. | 2010 Apr 1 |
Patents
Sample Use Guides
In Vivo Use Guide
Curator's Comment: http://www.chinaphar.com/1671-4083/18/109.pdf
http://rbsapp.net:8080/rcap/
Single Dose Eye drops: 2 drops in each eye or half the contents of a single-dose, three times a day
Multi-dose eye drops: 2 drops in each eye, three times a day
oral: single dosage benzadac lysine in tables (500 mg)
Skin ulcers: An appropriate amount of this product is applied to the affected area several times a day. Incidentally, it performs patch therapy 1-2 times daily as needed.
Inflammatory skin disease: An appropriate amount of this product is applied to the affected area several times a day.
Route of Administration:
Other
| Substance Class |
Chemical
Created
by
admin
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Edited
Mon Mar 31 18:48:51 GMT 2025
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on
Mon Mar 31 18:48:51 GMT 2025
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| Record UNII |
CL7T957EGC
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| Record Status |
Validated (UNII)
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| Record Version |
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CL7T957EGC
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100000084995
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DTXSID701002309
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m2307
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SOLVATE->ANHYDROUS | |||
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PARENT -> SALT/SOLVATE | |||
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PARENT -> SALT/SOLVATE |
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ACTIVE MOIETY |