MK-3102 (Omarigliptin)

製品コードS8565 バッチS856501

印刷

化学情報

Chemical Structure Synonyms N/A Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C17H20F2N4O3S
分子量 398.43 CAS No. 1226781-44-7
Solubility (25°C)* 体外 DMSO 79 mg/mL (198.27 mM)
Water Insoluble
Ethanol Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 Omarigliptin (MK-3102)は、DPP-4の競合的、可逆的阻害剤です（IC50 = 1.6 nM、Ki = 0.8 nM）。QPP、FAP、PEP、DPP8、DPP9を含む、試験したすべてのプロテアーゼに対して高い選択性を示し（IC50 > 67 μM）、弱いイオンチャネル活性を持ちます（IKr、Caγ1.2、Naγ1.5でIC50 > 30 μM）。
in vitro Omarigliptin (MK-3102) is a potent inhibitor of DPP-4 and is highly selective over other proteases tested (IC50 > 67 μmol/L) with weak ion channel activity (IC50 > 30 μmol/L at IKr, Caγ1.2, and Naγ1.5). Additionally, an IC50 > 10 μmol/L was obtained in all assays in an expansive selectivity counterscreen (168 radioligand binding or enzymatic assays). It binds rapidly and competitively to the active site of DPP-4, a process that is reversible and highly selective, and thus leads to increased levels of insulin and decreased levels of glucagon under hyperglycaemic conditions.
in vivo In lean mice, when orally administered 1 h prior to dextrose challenge in an oral glucose tolerance test (OGTT), it 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). the administration of omarigliptin dose-dependently increases plasma concentrations of active GLP-1. The pharmacokinetics of omarigliptin in male Sprague−Dawley rat and beagle dog are characterized by a low plasma clearance (0.9−1.1 mL/min/kg), a volume of distribution at steady state of 0.8−1.3 L/kg, and a long terminal half-life (∼11−22 h). The oral bioavailability of omarigliptin is good in both dogs and rats (∼100%). Omarigliptin is well-tolerated over the duration of the study, with no mortality or physical signs noted. Following the administration of a single oral dose of 25 mg in volunteers, omarigliptin was rapidly absorbed, with peak concentrations (Cmax) of 750 nmol/L reached within 1 h (Tmax). Bioavailability was estimated to be ≥74 %.

プロトコル(参考用のみ)

参考

  • https://pubmed.ncbi.nlm.nih.gov/24660890/
  • https://pubmed.ncbi.nlm.nih.gov/26507988/

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

The Effects of Traumatic Stress & Role of the Neuropeptide Y System as a Therapeutic in Females [ NYMC Student Theses and Dissertations, 2023, ] PubMed: none
Distal mutation V486M disrupts the catalytic activity of DPP4 by affecting the flap of the propeller domain [ Acta Pharmacol Sin, 2021, 1-9] PubMed: 34907358
Intranasal Neuropeptide Y as a Potential Therapeutic for Depressive Behavior in the Rodent Single Prolonged Stress Model in Females [ Front Behav Neurosci, 2021, 15:705579] PubMed: 34566592

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。