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345888 Ghrelin Receptor Antagonist, JMV 2959 - Calbiochem

345888
Purchase on Sigma-Aldrich

Overview

Replacement Information

Products

Catalogue NumberPackaging Qty/Pack
345888-10MG Glass bottle 10 mg
Description
OverviewA 1, 2, 4-triazole derived compound that acts as a potent ghrelin receptor (GHS-R1a) antagonist (IC50 = 32 nM in a binding assay, dissociation constant Kb = 19 nM). Shown to reduce hexarelin-induced food intake [hexarelin (80 µg/kg, cumulative food intake (g of food/100 g of body weight) at 6 h by acute administration (sc) of JMV 2959 (160 µg/kg)] in rats without affecting the basal food intake. Also suppresses ghrelin and fasting-induced food intake at the level of the central nervous system. Reported to suppress genes up-regulated by ghrelin. Does not affect intracellular Ca2+ mobilization.
Catalogue Number345888
Brand Family Calbiochem®
Synonyms(R)-N-(2-(1H-indol-3-yl)-1-(4-(4-methoxybenzyl)-5-phenethyl-4H-1,2,4-triazol-3-yl)ethyl)-2-aminoacetamide hydrochloride, GHSR1a Antagonist, GH secretagogue receptor antagonist, JMV2959, Growth hormone secretagogue receptor antagonist
References
ReferencesMoulin, A., et al. 2013. Amino Acids 301.
Mary, S., et al. 2012. Proc Natl Acad Sci USA 109, 8304.
Salome, N., et al. 2009. Eur J Pharmacol. 612, 167,.
Moulin, A., et al. 2007. J Med Chem 50, 579.
Product Information
FormBeige powder
FormulationSupplied as a hydrochloride salt.
Hill FormulaC₃₀H₃₂N₆O₂•HCl
Chemical formulaC₃₀H₃₂N₆O₂•HCl
Structure formula ImageStructure formula Image
Quality LevelMQ100
Applications
Biological Information
Primary TargetGhrelin receptor
Primary Target IC<sub>50</sub>32 nM
Purity≥97% by HPLC
Physicochemical Information
Dimensions
Materials Information
Toxicological Information
Safety Information according to GHS
Safety Information
Product Usage Statements
Storage and Shipping Information
Ship Code Shipped at Ambient Temperature or with Blue Ice or with Dry Ice
Toxicity Standard Handling
Storage +2°C to +8°C
Protect from Light Protect from light
Do not freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Packaging Information
Packaged under inert gas Packaged under inert gas
Transport Information
Supplemental Information
Specifications

Documentation

Ghrelin Receptor Antagonist, JMV 2959 - Calbiochem SDS

Title

Safety Data Sheet (SDS) 

Ghrelin Receptor Antagonist, JMV 2959 - Calbiochem Certificates of Analysis

TitleLot Number
345888

References

Reference overview
Moulin, A., et al. 2013. Amino Acids 301.
Mary, S., et al. 2012. Proc Natl Acad Sci USA 109, 8304.
Salome, N., et al. 2009. Eur J Pharmacol. 612, 167,.
Moulin, A., et al. 2007. J Med Chem 50, 579.
Data Sheet

Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

Revision22-August-2014 JSW
Synonyms(R)-N-(2-(1H-indol-3-yl)-1-(4-(4-methoxybenzyl)-5-phenethyl-4H-1,2,4-triazol-3-yl)ethyl)-2-aminoacetamide hydrochloride, GHSR1a Antagonist, GH secretagogue receptor antagonist, JMV2959, Growth hormone secretagogue receptor antagonist
DescriptionA 1, 2, 4-triazole derived compound that acts as a potent ghrelin receptor (GHS-R1a) antagonist (IC50 = 32 nM in a binding assay, dissociation constant Kb = 19 nM). Shown to reduce hexarelin-induced food intake [hexarelin (80 µg/kg, cumulative food intake (g of food/100 g of body weight) at 6 h by acute administration (sc) of JMV 2959 (160 µg/kg)] in rats without affecting the basal food intake. Also suppresses ghrelin and fasting-induced food intake at the level of the central nervous system. Reported to suppress genes up-regulated by ghrelin. Does not affect intracellular Ca2+ mobilization.
FormBeige powder
FormulationSupplied as a hydrochloride salt.
Intert gas (Yes/No) Packaged under inert gas
Chemical formulaC₃₀H₃₂N₆O₂•HCl
Structure formulaStructure formula
Purity≥97% by HPLC
SolubilityDMSO (100 mg/ml)or H₂O (5 mg/ml)
Storage +2°C to +8°C
Protect from light
Do Not Freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Toxicity Standard Handling
ReferencesMoulin, A., et al. 2013. Amino Acids 301.
Mary, S., et al. 2012. Proc Natl Acad Sci USA 109, 8304.
Salome, N., et al. 2009. Eur J Pharmacol. 612, 167,.
Moulin, A., et al. 2007. J Med Chem 50, 579.