A TGR5 agonist
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SB-756050

Item No. 27998

Technical Information
Formal Name
1,4-bis[(3,4-dimethoxyphenyl)sulfonyl]hexahydro-1H-1,4-diazepine
CAS Number
447410-57-3
Molecular Formula
C21H28N2O8S2
Formula Weight
Purity
≥95%
Formulation
A crystalline solid
DMF: 10 mg/mlDMF:PBS (pH 7.2) (1:2): 0.25 mg/mlDMSO: 10 mg/ml
λmax
249, 283 nm
SMILES
COC1=CC=C(S(N2CCCN(S(C3=CC=C(OC)C(OC)=C3)(=O)=O)CC2)(=O)=O)C=C1OC
InChi Code
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
InChi Key
GJUFPAZNBPFNRI-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    SB-756050 is an agonist of the bile acid G protein-coupled receptor TGR5 (EC50 = 1.3 μM for the human receptor).1 It is selective for TGR5 over the farnesoid X receptor (FXR) and a panel of other receptors, channels, and transporters. SB-756050 (10-100 mg/kg) decreases fasting glucose levels and increases glucose disposal rate and insulin secretion in diabetic Goto Kakizaki rats.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Hodge, R.J., Lin, J., Vasist Johnson, L.S., et alSafety, pharmacokinetics, and pharmacodynamic effects of a selective TGR5 agonist, SB-756050, in type 2 diabetes. Clin. Pharmacol. Drug Dev. 2(3), 213-222 (2013).