SB756050

SKU: orb1302926

Description

SB756050 is a potent and selective agonist of the TGR5 (GPBAR1) receptor. This small molecule is a valuable research tool for investigating TGR5's role in metabolic regulation, inflammation, and energy homeostasis in both in vitro and in vivo experimental models.

Research Area

Pharmacology & Drug Discovery

Key Properties

• CAS Number: 447410-57-3
• MW: 500.586
• Purity: >99.99% (May vary between batches)
• Formula: C₂₁H₂₈N₂O₈S₂
• SMILES: COC1=CC=C(C=C1OC)S(=O)(=O)N1CCCN(CC1)S(=O)(=O)C1=CC(OC)=C(OC)C=C1
• Target: GPCR19
• Solubility: DMSO:55 mg/mL (109.87 mM)

Bioactivity

• In Vivo:
  SB756050 is well‐tolerated with nonlinear pharmacokinetics. It shows dose‐proportional increase in plasma exposure above 100 mg, and has no marked changes in exposure when co‐administered with sitagliptin. SB756050 has highly variable pharmacodynamic effects both within between doses and dose groups, with increases in glucose seen at the two lowest doses and no reduction in glucose seen at the two highest doses. The glucose effects of SB756050 t sitagliptin are comparable to those of sitagliptin alone, even though gut hormone plasma profiles are different.
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• In Vitro:
  TGR5 is a potential target for the therapy of type 2 diabetes (T2D). Thus, SB756050 is used in phase 1clinical trials for the treatment of type 2 diabetes.
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Storage & Handling

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

Alternative Names

Inhibitor, GPCR19, GPBAR1, G-protein coupled receptor 19, G protein-coupled Bile Acid Receptor 1, inhibit, SB 756050, SB756050, SB-756050, TGR5

Compound Identifiers

PubChem CID

1520267