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Linerixibat

Chemical Structure : Linerixibat

CAS No.: 1345982-69-5

Linerixibat (GSK-2330672, GSK2330672)

Catalog No.: PC-61384Not For Human Use, Lab Use Only.

Linerixibat (GSK2330672) is a highly potent, selective, ileal apical sodium-dependent bile acid transporter (ASBT) inhibitor with IC50 of 2.1/1.9 nM for mouse/rat ASBT, respectively.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

Linerixibat (GSK2330672) is a highly potent, selective, ileal apical sodium-dependent bile acid transporter (ASBT) inhibitor with IC50 of 2.1/1.9 nM for mouse/rat ASBT, respectively.
Linerixibat (GSK2330672 lowers glucose in an animal model of type 2 diabetes, shows excellent developability properties for evaluating the potential therapeutic utility of a nonabsorbable ASBT inhibitor for treatment of patients with type 2 diabetes.

Physicochemical Properties

M.Wt 546.679
Formula C28H38N2O7S
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

3-[[[(3R,5R)-3-Butyl-3-ethyl-2,3,4,5-tetrahydro-7-methoxy-1,1-dioxido-5-phenyl-1,4-benzothiazepin-8-yl]methyl]amino]pentanedioic acid

References

1. Wu Y, et al. J Med Chem. 2013 Jun 27;56(12):5094-114.

2. Nunez DJ, et al. Diabetes Obes Metab. 2016 Jul;18(7):654-62.

3. Hegade VS, et al. Lancet. 2017 Mar 18;389(10074):1114-1123.

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