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IPBT-5CA (CAS 306935-41-1) LS-H115

GPR109B agonist
LS-H115-50 / 50 mg / $175
LS-H115-100 / 100 mg / $185
LS-H115-500 / 500 mg / $245
LS-H115-1000 / 1000 mg / $305
USA Shipment Only
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Description: The G protein-coupled receptors GPR109A and GPR109B are recognized to be receptors for hydroxy-carboxylic acid (HCA) metabolites, are abundant in adipocytes, and are relevant to atherosclerosis and dyslipidemia. IPBT-5CA is a selective agonist of GPR109B (HCA3; EC50 = 400 nM). It displays no activity at GPR109A (HCA2). IBC-293 inhibits forskolin-stimulated cAMP release in Chinese hamster ovary cells stably expressing GPR109B (EC50 = 54 nM) but not in cells expressing GPR109A. This is accompanied by a rapid and transient increase in intracellular calcium and activation of ERK1/2 through a pertussis toxin-sensitive Gi signaling pathway. H115_ChemicalStructureImage.png
1-(1-methylethyl)-1H-benzotriazole-5-carboxylic acid
IBC-293
biochemical, chemical, agonist
LS-H115
306935-41-1
C10H11N3O2
≥98%
A crystalline solid
 
OC(C1=CC=C(N(C(C)C)N=N2)C2=C1)=O
InChI=1S/C10H11N3O2/c1-6(2)13-9-4-3-7(10(14)15)5-8(9)11-12-13/h3-6H,1-2H3,(H,14,15)
RUTVRAJKELSHCC-UHFFFAOYSA-N
Shipped Ambient, store at -20°C, ≥ 2 years shelf life.
This product is for research use only. Not for administration to humans, or for human or veterinary diagnostic or therapeutic use.
Data Sheet DataSheet    SDS SDS
Related Products: HCAR3 / GPR109B / HM74 related products

Usage Information

IPBT-5CA is supplied as a crystalline solid. A stock solution may be made by dissolving the IPBT-5CA in the solvent of choice. IPBT-5CA is soluble in organic solvents such as ethanol, DMSO, and dimethyl formamide (DMF), which should be purged with an inert gas. The solubility of IPBT-5CA in these solvents is approximately 5, 25, and 16 mg/ml, respectively. IPBT-5CA is sparingly soluble in aqueous buffers. For maximum solubility in aqueous buffers, IPBT-5CA should first be dissolved in DMF and then diluted with the aqueous buffer of choice. IPBT-5CA has a solubility of approximately 0.5 mg/ml in a 1:1 solution of DMF:PBS (pH 7.2) using this method. We do not recommend storing the aqueous solution for more than one day.

References:
  1. Ahmed, K., Tunaru, S., and Offermanns, S. Trends Pharmacol. Sci. 30(11), 557-562 (2009).
  2. Offermanns, S., Colletti, S.L., Lovenberg, T.W., et al. Pharmacol. Rev. 63(2), 269-290 (2011).
  3. Semple, G., Skinner, P.J., Cherrier, M.C., et al. J. Med. Chem. 49(4), 1227-1230 (2006).
  4. Zhou, Q., Li, G., Deng, X.Y., et al. Br. J. Pharmacol. 166(6), 1756-1773 (2012).

 


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