Carmegliptin
Carmegliptin (RO-4876904) is an orally active and potent DPP IV inhibitor with a human DPP IV IC50 of 6.8 nM. Carmegliptin 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 acts as a substrate for human P glycoprotein without inhibiting the transporter, shows low in vitro cell permeability. Carmegliptin can be used for the research of type 2 diabetes, non insulin dependent diabetes mellitus.
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- No. CAS: 813452-18-5
- Fòrmula: C20H28FN3O3
- Peso molecular:377.45
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Chemical Information
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Actividad biológica
Descripciòn
IC50 & Target
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DPP-4 6.8 nM (IC50) |
In Vitro
Carmegliptin potently inhibits human DPP-IV with an IC50 of 6.8 nM[1].
Carmegliptin (10 μM) 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 does not inhibit or induce CYP450 enzymes[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Parmacokinetics
| Species | Dose | Route | CL | Vss | T1/2 | F |
|---|---|---|---|---|---|---|
| Monkey2 | 1 mg/kg | i.v. | 8.5 mL/min/kg | 3.3 L/kg | 6.8 h | / |
| Monkey2 | 3 mg/kg | p.o. | / | / | / | 33 % |
| Rat2 | 1 mg/kg | i.v. | 24 mL/min/kg | 6.3 L/kg | 3.3 h | / |
| Rat2 | 3 mg/kg | p.o. | / | / | / | 28 % |
In Vivo
Carmegliptin (20 mg/kg; p.o.; daily; 7 days) 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) 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) 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.
Ensayo clínico
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 813452-18-5
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Peso molecular 377.45
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Fòrmula C20H28FN3O3
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SMILES
O=C(C1)N(C[C@H]1CF)[C@H]2CN3CCC4=CC(OC)=C(OC)C=C4[C@@]([H])3C[C@@H]2N
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Synonyms
RO-4876904
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
[1]. Boehringer M,et al. Pyrido [2,1-a] isoquinoline derivatives. US20040259903A1. 2004-12-23.
[2]. 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 Feb 1;20(3):1109-13. [Content Brief]
[3]. Kuhlmann O, et al. Interaction potential of Carmegliptin with P-glycoprotein (Pgp) transporter in healthy volunteers. J Drug Assess. 2014 Mar 3;3(1):28-37. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Carmegliptin Related Classifications
HY-10289 Related Classifications
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