FIPI

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

FIPI 是 halopemide 的衍生物，可有效抑制 PLD1 (IC50 = 25 nM) 和 PLD2 (IC50 = 20 nM)。

FIPI is a derivative of halopemide which potently inhibits both PLD1 (IC50 = 25 nM) and PLD2 (IC50 = 20 nM); prevents PLD regulation of F-actin cytoskeleton reorganization, cell spreading, and chemotaxis.

Despite the high clearance of greater than 2 L/h/kg, FIPI shows a half-life of greater than 5 h, a Cmax of greater than 10-fold the 50 versus PLD2, and moderate bioavailability of 18%. FIPI inhibits both PLD1 and PLD2 in a dose-dependent manner, with 50% loss of activity observed at approximately 25 nM. FIPI is not an irreversible suicide inhibitor but neither is it rapidly and completely reverses upon removal of the drug. IPI does not alter PLD subcellular localization, access to PIP2, actin stress fibers, or upstream signaling events. FIPI rescues PLD2-suppressed membrane ruffling and cell spreading.

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5-Fluoro-2-indolyl deschlorohalopemide

PI3K/Akt/mTOR signaling

S6 Kinase

PLD1| PLD2

Inflammation/Immunology

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939055-18-2

421.48

C23H24FN5O2

>98% (HPLC)

DMSO : 14.67 mg/mL 34.81 mM;

O=C(c1cc2c(ccc(F)c2)[nH]1)NCCN1CCC(n2c(=O)[nH]c3c2cccc3)CC1

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(-20℃)

With Ice Pack

≥ 2 years