JTP-96193 | TACE inhibitor | Probechem Biochemicals

Chemical Structure : JTP-96193

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JTP-96193 (JTP96193)

货号: PC-20476Not For Human Use, Lab Use Only.

JTP-96193 (JTP96193) is a potent, selective TNF-α converting enzyme (TACE/ADAM17) inhibitor with IC50 of 5.4 nM, >1800-fold selectivity against ADAM10.

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生物&药学活性

JTP-96193 (JTP96193) is a potent, selective TNF-α converting enzyme (TACE/ADAM17) inhibitor with IC50 of 5.4 nM, >1800-fold selectivity against ADAM10.
JTP-96193 also displays >500-fold selectivity against other MMP family members such as MMP-1, -2, -3, -7, -8, -9, -10, -12, -13, -15, -16, -17, and -24.
JTP-96193 (10 uM) completely inhibited LPS-induced TNF-α production in rat whole, with IC50 of 0.17 uM.
JTP-96193 significantly inhibited TNF-α production in Lewis rats induced by LPS injection with ED50 3.8 mg/kg.
JTP-96193 dose-dependently reduced the TNF-α release from fat tissue in DIO mice, prevented delay of sciatic MNCV without any effects on blood glucose or insulin levels in STZ-induced diabetic mice.

物理化学性质&存储条件

分子量	525.60
分子式	C26H28FN5O4S
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	4-((7,8-dimethyl-1,2,3,4-tetrahydroquinolin-5-yl)methoxy)-2-fluoro-N-((3S,4S)-1-formyl-4-(5-oxo-4,5-dihydro-1,3,4-thiadiazol-2-yl)pyrrolidin-3-yl)benzamide

参考文献

1. Maekawa M, et al. Biol Pharm Bull. 2019;42(11):1906-1912.

JTP-96193 (JTP96193)

生物&药学活性

物理化学性质&存储条件

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JTP-96193 (JTP96193)

生物&药学活性

物理化学性质&存储条件

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