Molidustat是一種新型的HIF-PH抑制劑,對PHD1, PHD2, PHD3的IC50值分別為480 nM, 280 nM和450 nM。
BVT 2733產品描述:BVT 2733 is a new, small molecule, non-steroidal, isoform-selective inhibitor of 11beta-hydroxysteroid dehydrogenase type 1 (11β-HSD1). IC50 value: Target: 11β-HSD1 inhibitor in vitro: in vivo: BVT 2733 lowered hepatic PEPCK and glucose-6-phosphatase mRNA, blood glucose and serum insulin concentrations compared with vehicle treated mice [1]. CIA mice were treated with BVT-2733 (100 mg/kg, orally) or vehicle twice daily for 2 weeks. BVT-2733 treatment attenuated the arthritis severity and anti-CII level in CIA mice. BVT-2733 also decreased the levels of serum TNF-α, IL-1β, IL-6 and IL-17. BVT-2733 treatment also significantly reduced synovial inflammation and joint destruction [2]. Mice receiving BVT 2733 treatment exhibited decreased body weight and enhanced glucose tolerance and insulin sensitivity compared to control mice. BVT 2733 also down-regulated the expression of inflammation-related genes including monocyte chemoattractant protein 1 (MCP-1), tumor necrosis factor alpha
公司介紹:MedChemExpress(MCE)專注于各種抑制劑、激動劑、API及化合物庫,總部位于美國新澤西,分別在瑞典和上海設有歐洲區子公司和亞洲區總代理,營銷網點遍及全球20多個國家地區。MCE經過多年努力已成為全球生物活性小分子領域的一流供應商, 產品涵蓋癌癥、神經科學、抗感染、表觀遺傳學等20個熱門研究領域,PI3K、MAPK等近千個細分靶點,超過4000個活性小分子化合物現貨,以及GPCR、API、離子通道等超過20種不同類型的化合物庫,同時提供從毫克到千克的專業定制合成服務。
MCE 對每批產品都進行嚴格的LCMS和NMR檢驗,其產品已被全球近萬名客戶廣泛使用并發表大量文章、專利;
MCE 定期增加各領域熱門抑制劑、激動劑,不斷擴增已有化合物庫,以滿足最新的科研需求;
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產品鏈接:www.medchemexpress.cn/BVT-2733.html
Purity:98%
MWt:314.3027
Formula:C13H14N8O2
SMILES:O=C1C(N2N=NC=C2)=CNN1C3=NC=NC(N4CCOCC4)=C3
Pathway:metabolic Enzyme/Protease;
Mechanisms:HIF/HIF Prolyl-Hydroxylase;
Research Area:Cardiovascular Disease
電話: 021-58955995
網址: www.MedChemExpress.cn
地址: 上海市浦東新區蔡倫路720號2號樓3層
Molidustat說明
發布日期:2018-04-24 瀏覽次數:0
核心提示:Molidustat是一種新型的HIF-PH抑制劑,對PHD1, PHD2, PHD3的IC50值分別為480 nM, 280 nM和450 nM。
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