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首页-小分子抑制剂&激动剂-GPCR-Somatostatin Receptor-J-2156
J-2156

Chemical Structure : J-2156

CAS No.: 848647-56-3

J-2156 (J2156)

货号: PC-49080Not For Human Use, Lab Use Only.

J-2156 is a highly potent, selective somatostatin SST4 receptor agonist with binding Ki value of 1.2 nM (hSST4R), >400-fold selectivity over other human somatostatin receptor subtypes.

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10 mg ¥2580 In stock
25 mg ¥4580 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

J-2156 is a highly potent, selective somatostatin SST4 receptor agonist with binding Ki value of 1.2 nM (hSST4R), >400-fold selectivity over other human somatostatin receptor subtypes.
J-2156 acts as a apparent full agonist by completely inhibiting the forskolin-stimulated adenylyl cyclase activity with EC50 of 70 nM.
J-2156 (1-100 microg/kg i.p.) inhibited nocifensive behaviour of mice in the second phase of the formalin test.
J-2156 inhibited sciatic nerve ligation-induced neuropathic mechanical hyperalgesia.

物理化学性质&存储条件

分子量 468.572
分子式 C24H28N4O4S
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

(S)-4-amino-N-((S)-1-amino-1-oxo-3-phenylpropan-2-yl)-2-((4-methylnaphthalene)-1-sulfonamido)butanamide

参考文献

1. Engström M, et al. J Pharmacol Exp Ther. 2005 Jan;312(1):332-8.

2. Engström M, et al. J Pharmacol Exp Ther. 2006 Mar;316(3):1262-8.

3. Sándor K, et al. Eur J Pharmacol. 2006 Jun 6;539(1-2):71-5.

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