JNJ-55308942 | P2X7 antagonist | Probechem Biochemicals

Chemical Structure : JNJ-55308942

CAS No.: 2166558-11-6

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JNJ-55308942 (JNJ55308942)

货号: PC-62763Not For Human Use, Lab Use Only.

JNJ-55308942 is a highly potent, selective, brain-penetrant P2X7 antagonist with Ki of 1.0 and 6.5 nM for rat and human hP2X7.

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5 mg	￥1780	In stock
10 mg	￥2880	In stock
25 mg	￥4780	In stock
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100 mg		Get quote

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生物&药学活性

JNJ-55308942 is a highly potent, selective, brain-penetrant P2X7 antagonist with Ki of 1.0 and 6.5 nM for rat and human hP2X7.
JNJ-55308942 demonstrates no significant activity against a panel of related P2X receptors (P2X1, P2X2, P2X3, P2X2/3, and P2X4.
JNJ-55308942 also shows insignificant inhibition of nine CYP isoforms (IC50>15 uM).
JNJ-55308942 exhibits excellent P2X7 receptor occupancy in the hippocampus of rats with low ED50 of 0.07 mg/kg and unbound plasma EC50 of 12 ng/mL, suppresses brain IL-1β release in vivo in freely moving rats challenged with the P2X7 agonist Bz-ATP.
JNJ-55308942 possesses good tolerability margins in preclinical species, as well as an acceptable cardiovascular safety profile in vivo.

物理化学性质&存储条件

分子量	425.323
分子式	C17H12F5N7O
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)-(3-fluoro-2-(trifluoromethyl)pyridin-4-yl)(1-(5-fluoropyrimidin-2-yl)-6-methyl-1,4,6,7-tetrahydro-5H-[1,2,3]triazolo[4,5-c]pyridin-5-yl)methanone

参考文献

1. Chrovian CC, et al. J Med Chem. 2018 Jan 11;61(1):207-223.

JNJ-55308942 (JNJ55308942)

生物&药学活性

物理化学性质&存储条件

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JNJ-55308942 (JNJ55308942)

生物&药学活性

物理化学性质&存储条件

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