JMV 2959 hydrochloride (925238-89-7 free base) 是一种生长激素促分泌素受体 1a 型 (GHS-R1a) 拮抗剂,在 LLC-PK1 细胞中的 IC50 为 32±3 nM。
产品描述
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.
体外活性
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.JMV 2959 is a growth hormone secretagogue receptor type 1a (GHS-R1a) antagonist with an IC50 of 32 nM.
体内活性
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).
Cas No.
T11719
分子式
C30H33ClN6O2
分子量
545.08
别名
JMV 2959 hydrochloride
储存和溶解度
DMSO:250 mg/mL (458.65 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years