345888 | Ghrelin Receptor Antagonist, JMV 2959 - Calbiochem

345888
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      Overview

      Replacement Information

      Pricing & Availability

      Catalog NumberAvailability Packaging Qty/Pack Price Quantity
      345888-10MG
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      Stocked 
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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
          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

          SDS

          Title

          Safety Data Sheet (SDS) 

          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.