An ASBT inhibitor
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GSK2330672

Item No. 23843

Technical Information
Formal Name
3-[[[(3R,5R)-3-butyl-3-ethyl-2,3,4,5-tetrahydro-7-methoxy-1,1-dioxido-5-phenyl-1,4-benzothiazepin-8-yl]methyl]amino]-pentanedioic acid
CAS Number
1345982-69-5
Molecular Formula
C28H38N2O7S
Formula Weight
Purity
≥98%
Formulation
A crystalline solid
DMF: 5 mg/mlDMSO: 2 mg/mlPBS (pH 7.2): 0.2 mg/ml
λmax
206, 238 nm
SMILES
CC[C@@](N[C@@H]1C2=CC=CC=C2)(CCCC)CS(C3=C1C=C(OC)C(CNC(CC(O)=O)CC(O)=O)=C3)(=O)=O
InChi Code
InChI=1S/C28H38N2O7S/c1-4-6-12-28(5-2)18-38(35,36)24-13-20(17-29-21(14-25(31)32)15-26(33)34)23(37-3)16-22(24)27(30-28)19-10-8-7-9-11-19/h7-11,13,16,21,27,29-30H,4-6,12,14-15,17-18H2,1-3H3,(H,31,32)(H,33,34)/t27-,28-/m1/s1
InChi Key
CZGVOBIGEBDYTP-VSGBNLITSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    OBESITY RESEARCH SOLUTIONS
    Product Description

    GSK2330672 is an inhibitor of the sodium/bile acid and sulfated solute cotransporter (ASBT; IC50s = 42, 2.1, and 1.9 nM for human, mouse, and rat ASBT, respectively).1 In vivo, GSK2330672 (0.05 mg/kg) stimulates fecal bile acid secretion, reduces hemoglobin A1c (HbA1c) and plasma glucose levels, and increases total GLP-1 (Item No. 24460) and plasma insulin in Zucker diabetic fatty (ZDF) rats.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Wu, Y., Aquino, C.J., Cowan, D.J., et alDiscovery of a highly potent, nonabsorbable apical sodium-dependent bile acid transporter inhibitor (GSK2330672) for treatment of type 2 diabetes. J. Med. Chem. 56(12), 5094-5114 (2013).