Bile acids (BAs) are actively reabsorbted from the gut lumen by the ileal Na+-dependent transporter apical sodium-dependent bile acid transporter (ASBT, also referred to as IBAT-ileal bile acid transporter, SLC10A2). At mealtimes, the liver produces bile acids, which are then secreted into the duodenum and stored in the gallbladder. As well as the apical surface of renal tubules and cholangiocytes, ASBT is present on the brush border/apical membrane of ileal enterocytes. Conjugated bile acids are returned to the liver through the portal circulation by being actively transported by IBAT from the lumen/apical side into the interior of the enterocyte and exported via the basolateral membrane organic solute transporter α/β heterodimer (OSTα/β; encoded by SLC51A/B).This procedure plays a significant role in the enterohepatic circulation (EHC) of BAs and the homeostasis of BAs in the body. As a result, it is thought that ASBT is a favorite target for intervention to control levels of BAs, cholesterol, lipid, and glucose, among other things. In addition, due to its intestinal localization, high expression, and high uptake capacity, ASBT is a well-liked delivery target for the development of prodrugs.
| Structure | Cat No. | Product Name | CAS No. | Product Description |
|---|---|---|---|---|
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V74152 | 264W94 | 178961-24-5 | 264W94 is a potent ileal bile acid transporter (IBAT) inhibitor and a new cholesterol-lowering drug. |
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V4279 | Elobixibat | 439087-18-0 | Elobixibat (also known as AZD-7806, AJG-533 and A 3309) is a novel, potent andfirst-in-class ileal bile acid transporter (IBAT)inhibitor withIC50values of 0.53 ± 0.17 nM, 0.13 ± 0.03 nM, and 5.8 ± 1.6 nM for human IBAT, mouse IBAT, and canine IBAT. |
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V3633 | Iinerixibat (GSK2330672) | 1345982-69-5 | Linerixibat (formerly known as GSK2330672; GSK-2330672) is a novel, highly potent and nonabsorbable inhibitor of ASBT (apical sodium-dependent bile acid transporter) under development for cholestatic pruritus in primary biliary cholangitis. |
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V9853 | Odevixibat | 501692-44-0 | Odevixibat (formerly known as A-4250; AZD-8294; A-4250; AR-H 064974; Bylvay)is a novel, potent and orally bioavailable inhibitor of ileal bile acid transporter (IBAT) with the potential to be used for the treatment of primary biliary cirrhosis. |
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V74153 | Ritivixibat | 2460667-52-9 | Ritivixibat is an inhibitor (blocker/antagonist) of ileal bile acid transporter (IBAT) and a bile acid modulator. |
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