Description
SB756050 is a selective TGR5 agonist. SB756050 has the potential for type 2 diabetes treatment.
Product information
CAS Number: 447410-57-3
Molecular Weight: 500.59
Formula: C21H28N2O8S2
Chemical Name: 1,4-bis(3,4-dimethoxybenzenesulfonyl)-1,4-diazepane
Smiles: COC1=CC=C(C=C1OC)S(=O)(=O)N1CCCN(CC1)S(=O)(=O)C1C=C(OC)C(=CC=1)OC
InChiKey: GJUFPAZNBPFNRI-UHFFFAOYSA-N
InChi: InChI=1S/C21H28N2O8S2/c1-28-18-8-6-16(14-20(18)30-3)32(24,25)22-10-5-11-23(13-12-22)33(26,27)17-7-9-19(29-2)21(15-17)31-4/h6-9,14-15H,5,10-13H2,1-4H3
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO : ≥ 150 mg/mL (299.65 mM).
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In Vitro:
TGR5 is a bile acid receptor and a potential target for the treatment of type 2 diabetes (T2D).
In Vivo:
SB756050 is well‐tolerated; it is readily absorbed, exhibited nonlinear pharmacokinetics with a less than dose‐proportional increase in plasma exposure above 100 mg, and demonstrates no significant changes in exposure when co‐administered with sitagliptin. SB756050 demonstrates highly variable pharmacodynamic effects both within dose groups and between doses, 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 sitagliptin are comparable to those of sitagliptin alone, even though gut hormone plasma profiles are different.
Products are for research use only. Not for human use.
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