JMV 2959

目录号: GC31274纯度: >99.50%

JMV2959是一种生长激素促分泌素受体1a型(GHS-R1a)拮抗剂,其IC50值为32nM。


JMV 2959
Cas No.: 925238-89-7
规格价格库存数量操作
5mg¥1,170.00现货
1
10mg¥1,890.00现货
1
25mg¥3,600.00现货
1
10mM (in 1mL DMSO)¥1,287.00现货
1

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产品描述 Description

JMV 2959 is a growth hormone secretagogue receptor type 1a (GHS-R1a) antagonist with an IC50 of 32 nM.

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[1].

When administered alone, it does not increase food intake and does not significantly stimulate growth hormone (GH) release[1]. JMV 2959 dose dependently decreases the startle response (F(3.42)=4.4, p

[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. [2]. Engel JA, et al. Blockade of growth hormone secretagogue receptor 1A signaling by JMV 2959 attenuates the NMDAR antagonist, phencyclidine-induced impairments in prepulse inhibition. Psychopharmacology (Berl). 2015 Dec;232(23):4285-92. [3]. Clifford PS, et al. Attenuation of cocaine-induced locomotor sensitization in rats sustaining genetic or pharmacologic antagonism of ghrelin receptors. Addict Biol. 2012 Nov;17(6):956-63.

实验参考方法 Experimental Reference Method

Animal experiment:

Two-hundred-gram male Sprague-Dawley rats are used in the study. The animals (n=15) are randomly assigned to an initial treatment dose or vehicle and subsequently receive all the different doses tested in a counter balanced design. Each test is separated by a 3- to 4-day-long washout period. The rats are given the injection of JMV 2959 (or vehicle) 17 min prior to being placed in the startle cages (i.e., 25 min prior to the first pulse). The doses of JMV 2959 used for the dose response are 1, 3, and 6 mg/kg[2].

References:

[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.
[2]. Engel JA, et al. Blockade of growth hormone secretagogue receptor 1A signaling by JMV 2959 attenuates the NMDAR antagonist, phencyclidine-induced impairments in prepulse inhibition. Psychopharmacology (Berl). 2015 Dec;232(23):4285-92.
[3]. Clifford PS, et al. Attenuation of cocaine-induced locomotor sensitization in rats sustaining genetic or pharmacologic antagonism of ghrelin receptors. Addict Biol. 2012 Nov;17(6):956-63.

产品文档 Product Documents

Purity:>99.50%

化学性质Chemical Properties

CAS 号
925238-89-7
SMILES
O=C(N[C@@H](C1=NN=C(CCC2=CC=CC=C2)N1CC3=CC=C(OC)C=C3)CC4=CNC5=C4C=CC=C5)CN
分子式
C30H32N6O2
分子量
508.61 g/mol
溶解性
DMSO : 25 mg/mL (49.15 mM; ultrasonic and warming and heat to 60°C); H<sub>2</sub>O : &lt; 0.1 mg/mL (insoluble)
保存条件
Store at -20&#176;C
General tips
请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。
储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
为了提高溶解度,请将管子加热至 37°C,然后在超声波浴中震荡一段时间。
Shipping Condition
评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备 RT,或根据请求配备蓝冰。

计算工具摩尔浓度 / 稀释 / 分子量 / 单位换算 / 体内配方 / 溶解度

g/mol