915729-95-2
Chemical Structure
BMS-767778
- CAS No.: 915729-95-2
- Formula:C19H20Cl2N4O2
- Molecular Weight:407.29
IUPAC Name: (R)-2-(3-(aminomethyl)-4-(2,4-dichlorophenyl)-2-methyl-5-oxo-5,7-dihydro-6H-pyrrolo[3,4-b]pyridin-6-yl)-N,N-dimethylacetamide
InChIKey: PECDPZCIECMGCM-UHFFFAOYSA-N
SMILES: O=C(N(C)C)CN1CC2=NC(C)=C(CN)[C@]([C@]3=CC=C(Cl)C=C3Cl)=C2C1=O
Biological Activity:
BMS-767778 is an orally active and selective DPP4 inhibitor with Ki values of 0.94 nM, 4.9, 3.2 nM for DPP4, DPP8 and DPP9 respectively. BMS-767778 exhibits >3,000-fold selectivity over the related enzymes DPP8 and DPP9. BMS-767778 inhibits CYP-3A4 with IC50 of 5.2 μM. BMS-767778 significantly reduces blood glucose levels in high fat fed (HFD) ob/ob mice with safety profile. BMS-767778 can be used for diabetes mellitus research[1].
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BMS-767778 | BMS-767778 is an orally active and selective DPP4 inhibitor with Ki values of 0.94 nM, 4.9, 3.2 nM for DPP4, DPP8 and DPP9 respectively. BMS-767778 exhibits >3,000-fold selectivity over the related enzymes DPP8 and DPP9. BMS-767778 inhibits CYP-3A4 with IC50 of 5.2 μM. BMS-767778 significantly reduces blood glucose levels in high fat fed (HFD) ob/ob mice with safety profile. BMS-767778 can be used for diabetes mellitus research. |
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References
- [1]. Pratik Devasthale, et al. Optimization of activity, selectivity, and liability profiles in 5-oxopyrrolopyridine DPP4 inhibitors leading to clinical candidate (Sa)-2-(3-(aminomethyl)-4-(2,4-dichlorophenyl)-2-methyl-5-oxo-5H-pyrrolo[3,4-b]pyridin-6(7H)-yl)-N,N-dimethylacetamide (BMS-767778). J Med Chem . 2013 Sep 26;56(18):7343-57. [Content Brief]
