345888 Ghrelin Receptor Antagonist, JMV 2959 - Calbiochem

345888
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345888-10MGCN
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      Glass bottle 10 mg
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      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 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.