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.
For research use only. We do not sell to patients.
- CAS No.: 813452-14-1
- Formula: C20H30Cl2FN3O3
- Molecular Weight:450.37
-
Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
-
Biological Activity
-
Chemical Information
- Purity & Documentation
- References
-
Help & FAQs
Biological Activity
|
DPP-4 6.8 nM (IC50) |
Carmegliptin hydrochloride potently inhibits human DPP-IV with an IC50 of 6.8 nM[1].
Carmegliptin (10 μM) hydrochloride is highly selective for human DPP-IV, with no significant off-target activity at 10 μM and > 100-fold selectivity over related proline-specific dipeptidyl peptidases[1].
Carmegliptin hydrochloride does not inhibit or induce CYP450 enzymes in vitro[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Carmegliptin (20 mg/kg; p.o.; daily; 7 days) hydrochloride improves insulin sensitivity via increased GIR and shows a trend toward reduced hepatic glucose production in insulin-resistant Zucker fatty (fa/fa) rats[1].
Carmegliptin (10 mg/kg; p.o.; single dose) hydrochloride produces a significant reduction in fasting blood glucose and reduces the oral glucose tolerance test AUC0-t by 30%[1].
Carmegliptin(3 mg/kg; p.o.; single dose) hydrochloride produces sustained plasma DPP-IV inhibition in non-diabetic cynomolgus monkeys, with 40% and 60% baseline activity remaining at 24 and 48 hours post-administration[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
-
CAS No. 813452-14-1
-
Molecular Weight 450.37
-
Formula C20H30Cl2FN3O3
-
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
-
Synonyms
RO-4876904 hydrochloride
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
[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]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Powered by Bioz