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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

Images & Validation

Key Properties

CAS Number447410-57-3
MW500.59
Purity98.78%
FormulaC21H28N2O8S2
SMILESCOc1ccc(cc1OC)S(=O)(=O)N1CCCN(CC1)S(=O)(=O)c1ccc(OC)c(OC)c1
TargetGPCR19
SolubilityDMSO: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.
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.

Storage & Handling

StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Expiration Date12 months from date of receipt.
DisclaimerFor 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

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  • SB-756050 [orb1223125]

    >98% (HPLC)

    447410-57-3

    500.6

    C21H28N2O8S2

    1 g, 500 mg, 10 mg, 50 mg, 100 mg, 5 mg, 25 mg
Quality Guarantee

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Key Properties

No computed properties available.

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Protocol Information

SB756050 (orb1302926)

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% DMSO +
%+
% Tween 80 +
%

Available Sizes

Select a size below

1 ml x 10 mM (in DMSO)
¥ 1,040.00
5 mg
¥ 1,040.00
10 mg
¥ 1,300.00
25 mg
¥ 1,820.00
50 mg
¥ 2,470.00
100 mg
¥ 3,380.00
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