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首页-小分子抑制剂&激动剂-GPCR-5-HT Receptor-JNJ-18038683
JNJ-18038683

Chemical Structure : JNJ-18038683

CAS No.: 851376-05-1

JNJ-18038683 (JNJ18038683)

货号: PC-63400Not For Human Use, Lab Use Only.

JNJ-18038683 is a potent, selective 5-HT7 receptor antagonist with pKi of 8.19 and 8.20 for rat and human 5-HT7 in cell-based assays.

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5 mg ¥2580 In stock
10 mg ¥3980 In stock
25 mg ¥5980 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

JNJ-18038683 is a potent, selective 5-HT7 receptor antagonist with pKi of 8.19 and 8.20 for rat and human 5-HT7 in cell-based assays.
JNJ-18038683 decreases 5-HT (100 nM)-stimulated adenylyl cyclase in rat and human 5-HT7/HEK293 cells with pKb of 8.01 and 7.99, respectively.
JNJ-18038683 shows 10-fold selectivity over h5-HT6 receptor, 15-fold selectivity over rat adrenergic α1 receptor, 14- to 25-fold selectivity over the h5-HT2 receptor subtypes, and 20-fold selectivity over h5-HT1B receptor.
JNJ-18038683 prolongs rapid eye movement (REM) sleep and decreases REM duration induced by citalopram in vivo.

物理化学性质&存储条件

分子量 529.974
分子式 C26H28ClN3O7
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

3-(4-chlorophenyl)-1,4,5,6,7,8-hexahydro-1-(phenylmethyl)pyrazolo[3,4-d]azepine 2-hydroxy-1,2,3-propanetricarboxylate

参考文献

1. Bonaventure P, et al. J Pharmacol Exp Ther. 2012 Aug;342(2):429-40.

2. Shelton J, et al. Front Behav Neurosci. 2015 Jan 15;8:453.

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