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

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

JMV 2959 hydrochloride 是一种生长激素促分泌素受体 1a 型 (GHS-R1a) 拮抗剂，作用于 LLC-PK1 细胞，抑制 GHS-R1a，IC50 值为 32±3 nM。

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.

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.

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).

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GPCR/G Protein

GHSR

GHSR

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2448414-54-6

545.08

C30H33ClN6O2

>98% (HPLC)

In Vitro:?DMSO 中的溶解度 : 250 mg/mL (458.65 mM; 超声助溶 ) H2O 中的溶解度 : 25 mg/mL (45.86 mM; 超声助溶)

COC1=CC=C(CN2C(CCC3=CC=CC=C3)=NN=C2[C@H](NC(CN)=O)CC4=CNC5=CC=CC=C54)C=C1.Cl

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(-20℃)

With Ice Pack

≥ 2 years