中文名：Omarigliptin (MK-3102)
英文名：Omarigliptin (MK-3102)
純度：Moligand?，≥99%
貨號(hào)：O414061
Cas號(hào)：1226781-44-7
存儲(chǔ)溫度：-20°C儲(chǔ)存
運(yùn)輸條件：超低溫運(yùn)輸
產(chǎn)品介紹：
Information
Omarigliptin (MK-3102) Omarigliptin (MK-3102) is a competitive, reversible inhibitor of DPP-4 (IC50 = 1.6 nM, Ki = 0.8 nM). It is highly selective over all proteases tested (IC50 > 67 μM), including QPP, FAP, PEP, DPP8, and DPP9 and has weak ion channel activity (IC50 > 30 μM at IKr, Caγ1.2, and Naγ1.5).
Targets
DPP-4 (Cell-free assay) 1.6 nM
In vitro
Omarigliptin is a potent inhibitor of DPP-4 and is highly selective over other proteases tested (IC50 > 67 μmol/L) and has 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). Omarigliptin 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 Glukagon 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 %.
查看阿拉丁官網(wǎng)此產(chǎn)品相關(guān)對(duì)應(yīng)頁(yè)面：https://www.aladdin-e.com/zh_cn/O414061.html
關(guān)鍵字： 奧格列汀 ; 奧格列汀(MK-3102);AC-28992 ; J-690074
上海阿拉丁生化科技股份有限公司是A股上市公司（（股票代碼：688179），專(zhuān)注于科研試劑的研發(fā)、生產(chǎn)和銷(xiāo)售，已陸續(xù)建立多個(gè)工廠和研發(fā)中心。作為領(lǐng)軍企業(yè)，阿拉丁始終堅(jiān)持質(zhì)量第一，連續(xù)13年被評(píng)為“最受歡迎試劑品牌”。
阿拉丁目前常備庫(kù)存試劑產(chǎn)品品種超過(guò)7萬(wàn)種，SKU總數(shù)超過(guò)46萬(wàn)，產(chǎn)品線(xiàn)涵蓋了化學(xué)試劑、生化試劑、藥靶配體、蛋白質(zhì)和抗體等多個(gè)領(lǐng)域，是國(guó)內(nèi)少數(shù)化學(xué)試劑到生物試劑全面發(fā)展的國(guó)產(chǎn)試劑品牌，產(chǎn)品同步發(fā)布在我們國(guó)內(nèi)外電商平臺(tái)。