BIO-32546
CAS号 | 1548743-66-3 | 货号 | BCP28835 |
中文名 | BIO-32546 | ||
英文名 | BIO-32546 | ||
中文别名 | |||
英文别名 | BIO32546;BIO 32546; | ||
分子式 | C28H31F6NO3 | 分子量 | 543.54 |
生物活性 | BIO-32546 is an autotaxin (ATX) modulator. BIO-32546 has demonstrated in vivo efficacy in a model of acute pain with good PK/PD correlation. BIO-32546 showed a moderate blocking effect with lowered clearance (CL = 29 mL/min/kg) in rat PK, while maintaining good ATX potency (IC50 = 1.0 ±0.5 nM, N = 5) and low human microsomal clearance (CL =7.6 mL/min/kg). Compound 6 maintained low hERG inhibition (21.3% @ 10 μM) and excellent selectivity over receptors S1P1−5 and LPA1−3,5 (IC50 > 10 μM). | ||
信号通路 | Protease/Metabolic Enzyme | ||
靶 点 | Phosphodiesterase/PDE |
结构式
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