Odevixibat, also known as AZD 8294, is a potent, once-daily, non-systemic ileal bile acid transport inhibitor (IBATi). Odevixibat is being developed to treat rare pediatric cholestatic liver diseases, including progressive familial intrahepatic cholestasis (PFIC), biliary atresia and Alagille syndrome. Odevixibat acts locally in the small intestine. A4250 is well tolerated. By blocking ileal bile acid transporter in the terminal ileum, it highly efficiently interrupts the enterohepatic circulation of BAs, and should be of benefit to patients with cholestatic liver diseases. Odevixibat was approved in 2021 to treat pruritus.
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名称 | Odevixibat |
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Iupac 化学名称 | (S)-2-((R)-2-(2-((3,3-dibutyl-7-(methylthio)-1,1-dioxido-5-phenyl-2,3,4,5-tetrahydrobenzo[f][1,2,5]thiadiazepin-8-yl)oxy)acetamido)-2-(4-hydroxyphenyl)acetamido)butanoic acid |
同义词 | AZD 8294; AZD8294; AZD-8294; A-4250; A4250; A 4250; AR-H 064974; AR-H064974; AR-H-064974; Odevixibat |
英文同义词 | AZD 8294; AZD8294; AZD-8294; A-4250; A4250; A 4250; AR-H 064974; AR-H064974; AR-H-064974; Odevixibat |
分子式 | C37H48N4O8S2 |
分子量 | 740.93 |
Smile | CC[C@H](NC([C@H](NC(COC1=C(SC)C=C(C2=C1)N(C3=CC=CC=C3)CC(CCCC)(CCCC)NS2(=O)=O)=O)C4=CC=C(O)C=C4)=O)C(O)=O |
InChiKey | XULSCZPZVQIMFM-IPZQJPLYSA-N |
InChi | InChI=1S/C37H48N4O8S2/c1-5-8-19-37(20-9-6-2)24-41(26-13-11-10-12-14-26)29-21-31(50-4)30(22-32(29)51(47,48)40-37)49-23-33(43)39-34(25-15-17-27(42)18-16-25)35(44)38-28(7-3)36(45)46/h10-18,21-22,28,34,40,42H,5-9,19-20,23-24H2,1-4H3,(H,38,44)(H,39,43)(H,45,46)/t28-,34+/m0/s1 |
Cas号 | 501692-44-0 |
相关CAS号 |
包装 | 价格 | 库存 | 纯度 | 备货期 |
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大货 | 询价 | 询价 | 询价 |
外观性状 | 固体粉末 |
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纯度 | 98% Min. |
存储 | 短期(几天到几周)为0-4摄氏度,长期(几个月)为-20摄氏度 |
可溶性 | 溶于DMSO |
处理方式 | |
运输条件 | 作为非危险化学品在环境温度下装运。这种产品在正常运输和海关工作期间可以稳定几周. |
海关编码 |
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Mechanism | |
Cell study | |
Animal study | |
Clinical study |
1: Saveleva EE, Tyutrina ES, Nakanishi T, Tamai I, Salmina AB. Ingibitory natriĭ-zavisimogo perenoschika zhelchnykh kislot (ASBT) kak perspektivnye lekarstvennye sredstva [The inhibitors of the apical sodium-dependent bile acid transporter (ASBT) as promising drugs]. Biomed Khim. 2020 May;66(3):185-195. Russian. doi: 10.18097/PBMC20206603185. PMID: 32588824.
2: Al-Dury S, Wahlström A, Wahlin S, Langedijk J, Elferink RO, Ståhlman M, Marschall HU. Pilot study with IBAT inhibitor A4250 for the treatment of cholestatic pruritus in primary biliary cholangitis. Sci Rep. 2018 Apr 27;8(1):6658. doi: 10.1038/s41598-018-25214-0. PMID: 29704003; PMCID: PMC5923243.
3: Baghdasaryan A, Fuchs CD, Österreicher CH, Lemberger UJ, Halilbasic E, Påhlman I, Graffner H, Krones E, Fickert P, Wahlström A, Ståhlman M, Paumgartner G, Marschall HU, Trauner M. Inhibition of intestinal bile acid absorption improves cholestatic liver and bile duct injury in a mouse model of sclerosing cholangitis. J Hepatol. 2016 Mar;64(3):674-81. doi: 10.1016/j.jhep.2015.10.024. Epub 2015 Oct 31. PMID: 26529078.
4: Graffner H, Gillberg PG, Rikner L, Marschall HU. The ileal bile acid transporter inhibitor A4250 decreases serum bile acids by interrupting the enterohepatic circulation. Aliment Pharmacol Ther. 2016 Jan;43(2):303-10. doi: 10.1111/apt.13457. Epub 2015 Nov 2. PMID: 26527417.