JMV 2959 hydrochloride
目录号 : GC34207
JMV2959hydrochloride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±3nM。
Cas No.:2448414-54-6
Sample solution is provided at 25 µL, 10mM.
;)
,-1-7$$$37316672.jpg');)
;)
;)
$$$36806353.jpg');)
;33(7)%EF%BC%9A546-561$$$37156877.jpg');)
;)
;)
;)
%201124-1138.$$$35908550.jpg');)
%20766-780.$$$37100057.jpg');)
%20418-432.$$$36893736.jpg');)
%EF%BC%9A-240-255.$$$35108512.jpg');)
533-545$$$36543525.jpg');)
%201-13.$$$36600053.jpg');)
;)
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[1].
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)[2].
[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.
Animal experiment: | Rats[2]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 i.p. injection of JMV 2959 (1, 3, and 6 mg/kg) (or vehicle) 17 min prior to being placed in the startle cages (i.e., 25 min prior to the first pulse)[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. | |
| Cas No. | 2448414-54-6 | SDF | |
| Canonical 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.[H]Cl | ||
| 分子式 | C30H33ClN6O2 | 分子量 | 545.08 |
| 溶解度 | DMSO : ≥ 100 mg/mL (183.46 mM) | 储存条件 | Store at -20°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℃，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。 | ||
| 制备储备液 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 1.8346 mL | 9.173 mL | 18.3459 mL |
| 5 mM | 0.3669 mL | 1.8346 mL | 3.6692 mL |
| 10 mM | 0.1835 mL | 0.9173 mL | 1.8346 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet