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Omarigliptin

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Chemical Structure| 1226781-44-7 同义名 : MK-3102
CAS号 : 1226781-44-7
货号 : A115550
分子式 : C17H20F2N4O3S
纯度 : 98%
分子量 : 398.428
MDL号 : -
存储条件：

粉末 Keep in dark place,Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 50 mg/mL(125.49 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 Omarigliptin is a competitive, potent and selective inhibitor of dipeptidyl peptidase 4 (DPP-4) (IC50 = 1.6 nM, Ki = 0.8 nM) developed for the treatment of type 2 diabetes, which is highly selective over all proteases tested (IC50 > 67 μM). Omarigliptin has weak ion channel activity (IC50 > 30 μM at IKr, Cav1.2, and Nav1.5)[3]. Omarigliptin is indicated to have favorable effects on glycosylated hemoglobin (HbA1c), fasting and postmeal plasma glucose[4]. Omarigliptin improves glucose control in patients with type 2 diabetes by increasing the circulating concentration of glucagon-like peptide 1 and glucose-dependent insulinotropic polypeptide. Administration of omarigliptin dose-dependently increased plasma concentrations of active GLP-1, with maximal increases in active GLP-1 observed at the 0.3 to 1 mg/kg doses[3]. Omarigliptin resulted in ∼2-fold increases in weighted average postprandial active GLP-1. The average renal clearance of omarigliptin was ∼2 L/h and DPP-4 inhibition ranged from ∼77% to 89% at 168 hours [5].When orally administered 1 h prior to dextrose challenge, omarigliptin significantly reduced blood glucose excursion in a dose-dependent manner from 0.01 mg/kg (7% reduction in glucose AUC) to 0.3 mg/kg (51% reduction) in lean mice[3]. The oral bioavailability of omarigliptin was good in both dogs and rats (∼100%),and the mean percentage of unbound omarigliptin (1, 10, and 100 μM) in CD-1 mouse, Sprague–Dawley rat, beagle dog, and human plasma was 38%, 15%, 43%, and 68%, respectively[3].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.51mL

0.50mL

0.25mL

12.55mL

2.51mL

1.25mL

25.10mL

5.02mL

2.51mL
参考文献

[1]Sheu WH, Gantz I, et al. Safety and Efficacy of Omarigliptin (MK-3102), a Novel Once-Weekly DPP-4 Inhibitor for the Treatment of Patients With Type 2 Diabetes. Diabetes Care. 2015 Nov;38(11):2106-14.

[2]Biftu T, Sinha-Roy R, et al. Omarigliptin (MK-3102): a novel long-acting DPP-4 inhibitor for once-weekly treatment of type 2 diabetes. J Med Chem. 2014 Apr 24;57(8):3205-12.

[3]Biftu T, Sinha-Roy R, Chen P, Qian X, Feng D, Kuethe JT, Scapin G, Gao YD, Yan Y, Krueger D, Bak A, Eiermann G, He J, Cox J, Hicks J, Lyons K, He H, Salituro G, Tong S, Patel S, Doss G, Petrov A, Wu J, Xu SS, Sewall C, Zhang X, Zhang B, Thornberry NA, Weber AE. Omarigliptin (MK-3102): a novel long-acting DPP-4 inhibitor for once-weekly treatment of type 2 diabetes. J Med Chem. 2014 Apr 24;57(8):3205-12. doi: 10.1021/jm401992e. Epub 2014 Apr 2. PMID: 24660890.

[4]Tan X. Omarigliptin for the treatment of type 2 diabetes. Endocrine. 2016 Oct;54(1):24-31. doi: 10.1007/s12020-016-1011-9. Epub 2016 Jul 2. PMID: 27372109.

[5]Krishna R, Addy C, Tatosian D, Glasgow XS, Gendrano Iii IN, Robberechts M, Haazen W, de Hoon JN, Depré M, Martucci A, Peng JZ, Johnson-Levonas AO, Wagner JA, Stoch SA. Pharmacokinetics and Pharmacodynamics of Omarigliptin, a Once-Weekly Dipeptidyl Peptidase-4 (DPP-4) Inhibitor, After Single and Multiple Doses in Healthy Subjects. J Clin Pharmacol. 2016 Dec;56(12):1528-1537. doi: 10.1002/jcph.773. Epub 2016 Jun 17. PMID: 27225334; PMCID: PMC5111764.