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JMV 2959 hydrochloride (925238-89-7 free base)

CAS No. 2448414-54-6

JMV 2959 hydrochloride (925238-89-7 free base)( —— )

Catalog No. M32974 CAS No. 2448414-54-6

JMV 2959 hydrochloride (925238-89-7 free base) is a growth hormone secretagogue receptor type 1a (GHS-R1a) antagonist with an IC50 of 32±3 nM in LLC-PK1 cells.

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
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Biological Information

  • Product Name
    JMV 2959 hydrochloride (925238-89-7 free base)
  • Note
    Research use only, not for human use.
  • Brief Description
    JMV 2959 hydrochloride (925238-89-7 free base) is a growth hormone secretagogue receptor type 1a (GHS-R1a) antagonist with an IC50 of 32±3 nM in LLC-PK1 cells.
  • Description
    JMV 2959 hydrochloride is a growth hormone secretagogue receptor type 1a (GHS-R1a) antagonist with an IC50 of 32±3 nM in LLC-PK1 cells.
  • In Vitro
    JMV 2959 is a growth hormone secretagogue receptor type 1a (GHS-R1a) antagonist with an IC50 of 32 nM. JMV 2959 does not induce any intracellular calcium mobilization by itself. The dissociation constant of the receptor/JMV 2959 complex is determined by the Schild method. This experiment reveals a dissociation constant Kb of 19±6 nM.
  • In Vivo
    Intraperitoneal (i.p.) administration of Ghrelin (0.033, 0.1, and 0.33 mg/kg) does not alter the acoustic startle responses (ASR) or prepulse inhibition (PPI) in rats. Conversely, i.p. injection of JMV 2959 (1, 3, and 6 mg/kg), dose dependently decrease the ASR and increase PPI. Pretreatment with JMV 2959 at a dose with no effect on ASR or PPI per se, completely blocks Phencyclidine (PCP)-induced (2 mg/kg) deficits in PPI while pretreatment with the highest dose of Ghrelin does not potentiate or alter PPI responses of a sub-threshold dose of PCP (0.75 mg/kg).
  • Synonyms
    ——
  • Pathway
    GPCR/G Protein
  • Target
    GHSR
  • Recptor
    GHSR
  • Research Area
    ——
  • Indication
    ——

Chemical Information

  • CAS Number
    2448414-54-6
  • Formula Weight
    545.08
  • Molecular Formula
    C30H33ClN6O2
  • Purity
    >98% (HPLC)
  • Solubility
    In Vitro:?DMSO : 250 mg/mL (458.65 mM; Ultrasonic ) H2O : 25 mg/mL (45.86 mM; Ultrasonic)
  • SMILES
    COC1=CC=C(CN2C(CCC3=CC=CC=C3)=NN=C2[C@H](NC(CN)=O)CC4=CNC5=CC=CC=C54)C=C1.Cl
  • Chemical Name
    ——

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

1. Moulin A, et al. The 1,2,4-triazole as a scaffold for the design of ghrelin receptor ligands: development of JMV 2959, a potent antagonist. Amino Acids. 2013 Feb;44(2):301-14.?
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