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.
Product information
CAS Number: 2448414-54-6
Molecular Weight: 545.08
Formula: C30H33ClN6O2
Chemical Name: 2-amino-N-[(1R)-2-(1H-indol-3-yl)-1-{4-[(4-methoxyphenyl)methyl]-5-(2-phenylethyl)-4H-1,2,4-triazol-3-yl}ethyl]acetamide hydrochloride
Smiles: Cl.COC1C=CC(CN2C(=NN=C2CCC2C=CC=CC=2)[C@@H](CC2=CNC3C=CC=CC2=3)NC(=O)CN)=CC=1
InChiKey: QRRDZYKIVMLOJQ-HZPIKELBSA-N
InChi: InChI=1S/C30H32N6O2.ClH/c1-38-24-14-11-22(12-15-24)20-36-28(16-13-21-7-3-2-4-8-21)34-35-30(36)27(33-29(37)18-31)17-23-19-32-26-10-6-5-9-25(23)26;/h2-12,14-15,19,27,32H,13,16-18,20,31H2,1H3,(H,33,37);1H/t27-;/m1./s1
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO : 250 mg/mL (458.65 mM; Need ultrasonic). H2O : 25 mg/mL (45.86 mM; Need ultrasonic).
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
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).
Products are for research use only. Not for human use.
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