ex 527

Selisistat R-enantiomer (EX-527 (R-enantiomer)) 是 Selisistat R 型对映体。Selisistat 是SIRT1的选择性抑制剂，IC50为98 nM。

Selisistat (EX-527) 是一种去乙酰化酶 SIRT1 的抑制剂 (IC50=38 nM)，具有有效性和特异性。Selisistat 可以用于神经系统疾病如亨廷顿舞蹈病的研究。

Selisistat S-enantiomer (EX-527 S-enantiomer) 是一种选择性的SIRT1抑制剂，IC50值为 98 nM。

PKSI-527 is an inhibitor of plasma kallikrein (Ki = 0.81 μM). It is selective for plasma kallikrein over glandular kallikrein, plasmin, thrombin, urokinase, and Factor Xa (Kis = >500, 390, >500, 200, and >500 μM, respectively). PKSI-527 reduces bradykinin generation induced by kaolin and λ-carrageenan ex vivo in human plasma. It also prolongs partial thromboplastin and euglobulin clot lysis times. In vivo, PKSI-527 (300 mg/kg per day) reduces hyperplasia, pannus formation, and infiltration of inflammatory cells in the tarsal joint of mice with collagen-induced arthritis.