GSK2330672 free base · Synonyms: Linerixibat

GSK2330672 is an inhibitor of the apical sodium-dependent bile acid transporter.

For research use only. Not for human or veterinary use.

Target Apical Sodium-Dependent Bile Acid Transporter

Research area Infection Metabolic Disease Inflammation/Immunology

Purity >98% Stock Inquire

Data Sheet SDS COA

GSK2330672 structure

CAS No.: 1345982-69-5

Download structure (.mol)

Pack sizes & pricing

Size	Price	SKU	Stock
50 mg	USD 450.00	BP-01872-50mg	In stock	Get quote
100 mg	USD 750.00	BP-01872-100mg	In stock	Get quote
250 mg	USD 1,250.00	BP-01872-250mg	In stock	Get quote
500 mg	USD 1,950.00	BP-01872-500mg	In stock	Get quote
1 g	Inquire	BP-01872-1g	In stock	Inquire

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Description

GSK2330672 (Linerixibat) is an inhibitor of the apical sodium-dependent bile acid transporter (ASBT; IC50s = 42, 2.1, and 1.9 nM for human, mouse, and rat ASBT, respectively).

Biological activity

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.

Identifiers

SMILES: CCCC[C@]1(CC)CS(=O)(=O)C2=CC(CNC(CC(O)=O)CC(O)=O)=C(OC)C=C2[C@H](N1)C1=CC=CC=C1
InChIKey: CZGVOBIGEBDYTP-VSGBNLITSA-N

Specifications

MW (average): 546.6760
Formula: C₂₈H₃₈N₂O₇S
CAS No.: 1345982-69-5
Physical state: Solid
Color: White to off-white
Shipping: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage: Powder -20℃ 3 years; In solvent -20℃ 1 month;

Solubility

Soluble in DMSO

Documents

References

[1]. Wu Y, et al. Discovery of a highly potent, nonabsorbable apical sodium-dependent bile acid transporter inhibitor (GSK2330672) for treatment of type 2 diabetes. J Med Chem. 2013 Jun 27;56(12):5094-114.

[2]. Wang Y, et al. HNF4α Regulates CSAD to Couple Hepatic Taurine Production to Bile Acid Synthesis in Mice. Gene Expr. 2018 Aug 22;18(3):187-196.

[3]. Linerixibat (GSK2330672) granted Orphan Status. September 24, 2019./p>

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