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首页-小分子抑制剂&激动剂-Membrane Transporter/Ion Channel-TRP Channel-JNJ-28583113
JNJ-28583113

Chemical Structure : JNJ-28583113

CAS No.: 2765255-93-2

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JNJ-28583113 (JNJ28583113)

货号: PC-72125Not For Human Use, Lab Use Only.

JNJ-28583113 (JNJ28583113) is a potent, selective, brain penetrant TRPM2 antagonist with IC50 of 126 nM (hTRPM2).

规格 价格 库存 数量
5 mg ￥2280 In stock
10 mg ￥3680 In stock
25 mg ￥5880 In stock
50 mg Get quote
100 mg Get quote
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

JNJ-28583113 (JNJ28583113) is a potent, selective, brain penetrant TRPM2 antagonist with IC50 of 126 nM (hTRPM2).
JNJ-28583113 shows similar potency against species chimpanzee and rat TRPM2 with IC50 of 100 and 25 nM, respectively.
JNJ-28583113 shows no significant (IC50>10 uM) reactivity towards PARP or PARG and a panel for multiple known kinases GPCRs and ion channels, nine other TRP channels with exception of TRPM5 (IC50<1 uM).
Blocking TRPM2 via JNJ-28583113 caused phosphorylation of GSK3α and β subunits in cell assays.
JNJ-28583113 also protected cells from oxidative stress induced cell death as well as morphological changes induced by non-cytotoxic concentrations of H2O2。
JNJ-28583113 blunted cytokine release in response to pro-inflammatory stimuli in microglia.
JNJ-28583113 was brain penetrant but not suitable for systemic dosing as it was rapidly metabolized in vivo, but the in-vitro pharmacology of JNJ-28583113 is the best in class.

物理化学性质&存储条件

分子量 366.384
分子式 C19H21F3N2O2
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

ethyl 2-(3-(4-(trifluoromethyl)phenyl)-5,6,7,8-tetrahydrocyclohepta[c]pyrazol-1(4H)-yl)acetate

参考文献

1. Lawrence Fourgeaud, et al. Eur J Pharmacol. 2019 Jun 15;853:299-307.

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