Linerixibat
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; 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.Diabetes Phase 2 Clinical (In Vitro) :The zwitterionic, nonhygroscopic, crystalline salt form of Linerixibat (Compound 56) shows good aqueous solubility at pH 7.4 (>7 mg/mL), excellent thermal stability, and did not generate reactive or humanspecific metabolite, characteristics. (In Vivo) :Linerixibat (GSK2330672; 0.05-10 mg/kg; oral gavage; twice daily; for 14 days; male ZDF rat) treatment lowers glucose in an animal model of type 2 diabetes.
Product Specifications
CAS Number
1345982-69-5
Product Name Alternative
GSK-2330672 | GSK2330672
Purity
>98% (HPLC)
Solubility
DMSO: 21.5 mg/mL (< 1 mg/ml refers to the product slightly soluble or insoluble)
Smiles
O=C (O) CC (NCC1=C (OC) C=C (C2=C1) [C@@H] (C3=CC=CC=C3) N[C@] (CC) (CCCC) CS2 (=O) =O) CC (O) =O
Molecular Formula
C28H38N2O7S
Molecular Weight
546.679
Storage Conditions
Storage temperature: -20°C. Stability: ≥ 2 years
Notes
For research use only.
Other Product Names
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
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