Details
Stereochemistry | ACHIRAL |
Molecular Formula | C22H18Cl2N8.ClH |
Molecular Weight | 501.799 |
Optical Activity | NONE |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
Cl.CC1=CNC(=N1)C2=CN=C(NCCNC3=NC=C(C=C3)C#N)N=C2C4=CC=C(Cl)C=C4Cl
InChI
InChIKey=SCQDMKUZHIGAIB-UHFFFAOYSA-N
InChI=1S/C22H18Cl2N8.ClH/c1-13-10-29-21(31-13)17-12-30-22(32-20(17)16-4-3-15(23)8-18(16)24)27-7-6-26-19-5-2-14(9-25)11-28-19;/h2-5,8,10-12H,6-7H2,1H3,(H,26,28)(H,29,31)(H,27,30,32);1H
Molecular Formula | ClH |
Molecular Weight | 36.461 |
Charge | 0 |
Count |
|
Stereochemistry | ACHIRAL |
Additional Stereochemistry | No |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Optical Activity | NONE |
Molecular Formula | C22H18Cl2N8 |
Molecular Weight | 465.338 |
Charge | 0 |
Count |
|
Stereochemistry | ACHIRAL |
Additional Stereochemistry | No |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Optical Activity | NONE |
DescriptionSources: http://adisinsight.springer.com/drugs/800015112Curator's Comment: Description was created based on several sources, including
https://www.ncbi.nlm.nih.gov/pubmed/12606497
Sources: http://adisinsight.springer.com/drugs/800015112
Curator's Comment: Description was created based on several sources, including
https://www.ncbi.nlm.nih.gov/pubmed/12606497
CHIR 99021 is a selective, pyridimidine-based, glycogen synthase kinase 3 inhibitor that is effective at low nanomolar concentrations in enzyme assays and submicromolar concentrations in isolated cells and tissues. Chiron was developing CHIR 99021 for potential use in the treatment of type 2 diabetes mellitus. CHIR 99021 promoted insulin-mediated glucose uptake and increased glucose disposal in rodent models of diabetes. However, there has been no recent development reported.
Originator
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: CHEMBL2850 Sources: https://www.ncbi.nlm.nih.gov/pubmed/12606497 |
10.0 nM [IC50] | ||
Target ID: CHEMBL262 Sources: https://www.ncbi.nlm.nih.gov/pubmed/12606497 |
6.7 nM [IC50] |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Primary | Unknown Approved UseUnknown |
Sample Use Guides
In Vivo Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/12606497
In ZDF rats, a single oral dose
30 mg/kg of CHIR 99021 rapidly lowered plasma glucose.
Route of Administration:
Oral
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/26655496
rostral (r2–3) hindbrain hindbrain neural stem cells are efficiently specified by 1.4 µM CHIR99021
Substance Class |
Chemical
Created
by
admin
on
Edited
Sat Dec 16 16:10:28 GMT 2023
by
admin
on
Sat Dec 16 16:10:28 GMT 2023
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Record UNII |
5AW8G37ZX5
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Record Status |
Validated (UNII)
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Record Version |
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