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JMV3002 (CAS 925239-03-8) LS-H64

Ghrelin receptor antagonist
LS-H64-100 / 100 µg / $195
LS-H64-500 / 500 µg / $305
LS-H64-1000 / 1000 µg / $425
LS-H64-5000 / 5000 µg / $1650
USA Shipment Only
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Description: Ghrelin is an endogenous ligand for the growth hormone secretagogue receptor that stimulates food intake and transduces signals to hypothalamic regulatory nuclei that control energy homeostasis. JMV3002 is a potent ghrelin receptor antagonist with an IC50 value of 1.1 nM in vitro. At 80 ug/kg, JMV3002 inhibits hexarelin-stimulated food intake by as much as 98% in rats. JMV3002 alone does not elicit growth hormone release nor does it inhibit hexarelin-stimulated growth hormone secretion when tested in infant rats at a dose of 160 ug/kg. H64_ChemicalStructureImage.png
N-[(1R)-1-[4-[(2,4-dimethoxyphenyl)methyl]-5-(2-phenyylethyl)-4H-1,2,4-triazol-3-yl]-2-(1H-indol-3-yl)ethyl]-2-pyridinecarboxamide
 
biochemical, chemical, antagonist
LS-H64
925239-03-8
C35H34N6O3
≥98%
A solution in methyl acetate
 
COc1ccc(Cn2c(CCc3ccccc3)nnc2C(NC(=O)c2ccccn2)Cc2c[nH]c3ccccc23)c(OC)c1
InChI=1S/C35H34N6O3/c1-43-27-17-16-25(32(21-27)44-2)23-41-33(18-15-24-10-4-3-5-11-24)39-40-34(41)31(38-35(42)30-14-8-9-19-36-30)20-26-22-37-29-13-7-6-12-28(26)29/h3-14,16-17,19,21-22,31,37H,15,18,20,23H2,1-2H3,(H,38,42)/t31-/m1/s1
UMGBPWZCCHVQAY-WJOKGBTCSA-N
Shipped Ambient, store at -20°C, ≥ 1 year 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: GHSR / Ghrelin Receptor related products

Usage Information

JMV3002 is supplied as a solution in methyl acetate. To change the solvent, simply evaporate the methyl acetate under a gentle stream of nitrogen and immediately add the solvent of choice. Solvents such as ethanol, DMSO, and dimethyl formamide purged with an inert gas can be used. The solubility of JMV3002 in these solvents is approximately 20 mg/ml. JMV3002 is sparingly soluble in aqueous buffers. For maximum solubility in aqueous buffers, the methyl acetate solution of JMV3002 should be diluted with the aqueous buffer of choice. JMV3002 has a solubility of approximately 0.25 mg/ml in a 1:3 solution of ethanol:PBS (pH 7.2) using this method. We do not recommend storing the aqueous solution for more than one day.

References:
  1. Moulin, A., Demange, L., Ryan, J., et al. New trisubstituted 1,2,4-triazole derivatives as potent ghrelin receptor antagonists. 3. Synthesis and pharmacological in vitro and in vivo evaluations. J. Med. Chem. 51, 689-693 (2008).

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