JNJ-64251330 | JAK inhibitor | Probechem Biochemicals

Chemical Structure : JNJ-64251330

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JNJ-64251330 (Lorpucitinib, JNJ 64251330)

货号: PC-21596Not For Human Use, Lab Use Only.

Lorpucitinib (JNJ-64251330) is potent, selective and orally bioavailable pan-JAK inhibitor with IC50 of 0.37/8.6/92/7.4 nM for JAK1/JAK2/JAK3/Tyk2 respectively.

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生物&药学活性

Lorpucitinib (JNJ-64251330) is potent, selective and orally bioavailable pan-JAK inhibitor with IC50 of 0.37/8.6/92/7.4 nM for JAK1/JAK2/JAK3/Tyk2 respectively.
Lorpucitinib (JNJ-64251330) shows comparable potency to tofacitinib in an IFNα-stimulated STAT4 (54 nM and 31 nM, respectively) and an IL-12-stimulated STAT4 (257 nM and 440 nM, respectively) assay.
Lorpucitinib (JNJ-64251330) is 5-6 fold less potent in GM-CSF-stimulated pSTAT5 (303 nM and 51 nM, respectively) and IL-2-stimulated pSTAT5 (61 nM and 12 nM, respectively) assays.
Lorpucitinib (JNJ-64251330) is a GI tract-restricted JAK inhibitor that selectively inhibited cytokine responses in colonic tissue and not in plasma.

物理化学性质&存储条件

分子量	408.51
分子式	C22H28N6O2
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	2-(1-((1r,4r)-4-(cyanomethyl)cyclohexyl)-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-2-yl)-N-(2-hydroxy-2-methylpropyl)acetamide

参考文献

1. Kristi A Leonard, et al. J Med Chem. 2020 Mar 26;63(6):2915-2929.

JNJ-64251330 (Lorpucitinib, JNJ 64251330)

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JNJ-64251330 (Lorpucitinib, JNJ 64251330)

生物&药学活性

物理化学性质&存储条件

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