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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- CAS 番号: 813452-18-5
- 分子式: C20H28FN3O3
- 分子量:377.45
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
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DPP-4 6.8 nM (IC50) |
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.
| 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 % |
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.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 813452-18-5
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分子量 377.45
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分子式 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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別名
RO-4876904
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
[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
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
Carmegliptin 関連分類
HY-10289 関連分類
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