Linerixibat

SKU: orb1226494

Description

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.

Key Properties

• CAS Number: 1345982-69-5
• MW: 546.679
• Purity: >98% (HPLC)
• Formula: C₂₈H₃₈N₂O₇S
• 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
• Target: ASBT Transporter
• Solubility: DMSO: 21.5 mg/mL （ < 1 mg/ml refers to the product slightly soluble or insoluble )

Bioactivity

• In Vivo:
  Animal model: Male Zucker Diabetic Fatty (ZDF) rat. Dosage: 0.05 mg/kg, 0.1 mg/kg, 0.5 mg/kg, 1 mg/kg, 5 mg/kg, 10 mg/kg. Administration: Oral gavage; twice daily; for 14 days. Result: Led to a 1.30-1.64% reduction in hemoglobin A1c (HbA1c), a greater than 50% reduction in nonfasted plasma glucose to below 200 mg/dL, and statistically significant higher plasma insulin.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

GSK-2330672 | GSK2330672

Quick Database Links

Gene Symbol

ASBT Transporter