813452-14-1
Chemical Structure
Carmegliptin hydrochloride
Synonym(s): RO-4876904 hydrochloride
- CAS No.: 813452-14-1
- Formula:C20H30Cl2FN3O3
- Molecular Weight:450.37
InChIKey: DDKJYXSAKVWFLS-LSKWAPIISA-N
SMILES: COC1=C(OC)C=C2CCN(C[C@H](N3C[C@H](CC3=O)CF)[C@H](C4)N)[C@]4([H])C2=C1.Cl.Cl
Biological Activity: Carmegliptin hydrochloride (RO-4876904 hydrochloride) is an orally active and potent DPP‑IV inhibitor with a human DPP‑IV IC50 of 6.8 nM. Carmegliptin hydrochloride binds to the S1 pocket of DPP‑IV, blocks the degradation of GLP‑1, potentiates endogenous GLP‑1, increases plasma insulin levels, alleviates hyperglycemia, improves glucose tolerance. Carmegliptin hydrochloride acts as a substrate for human P‑glycoprotein without inhibiting the transporter, shows low in vitro cell permeability. Carmegliptin hydrochloride can be used for the research of type 2 diabetes, non‑insulin‑dependent diabetes mellitus[1][2][3].
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Carmegliptin hydrochloride | Carmegliptin hydrochloride (RO-4876904 hydrochloride) is an orally active and potent DPP‑IV inhibitor with a human DPP‑IV IC50 of 6.8 nM. Carmegliptin hydrochloride binds to the S1 pocket of DPP‑IV, blocks the degradation of GLP‑1, potentiates endogenous GLP‑1, increases plasma insulin levels, alleviates hyperglycemia, improves glucose tolerance. Carmegliptin hydrochloride acts as a substrate for human P‑glycoprotein without inhibiting the transporter, shows low in vitro cell permeability. Carmegliptin hydrochloride can be used for the research of type 2 diabetes, non‑insulin‑dependent diabetes mellitus. | |||||||||||||||||||||
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- [1]. Mattei P, et al. Discovery of carmegliptin: a potent and long-acting dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes. Bioorg Med Chem Lett. 2010;20(3):1109-1113. [Content Brief]
- [2]. Boehringer M, et al. (Hoffmann La Roche Inc). United States, US20040259903A1. 2004-12-23.
- [3]. Kuhlmann O, et al. Interaction potential of Carmegliptin with P-glycoprotein (Pgp) transporter in healthy volunteers. J Drug Assess. 2014;3(1):28-37. Published 2014 Mar 3. [Content Brief]
Keywords
