FIPI 是 halopemide 的衍生物，能够有效抑制

FIPI  (Synonyms: 5-Fluoro-2-indolyl deschlorohalopemide)

FIPI 是 halopemide 的衍生物，能够有效抑制 PLD1 和 PLD2，IC₅₀ 值分别为 25 nM 和 20 nM。

美国medchemexpress（MCE)浙江省一级代理:杭州昊鑫生物科技股份有限公司
MCE中国是全球领先的科研化学品和生物活性化合物供应商，总部位于美国新泽西。我们的产品范围覆盖各种抑制剂、激动剂、API和化合物库。专业、高效的企业灵魂铸造了在行业的卓越地位。热情和充满活力的研发团队拥有着大量的化学和生物科学家。专注于生物活性化合物，拥有着多年的发展历程和丰富的行业经验。从产品的HNMR数据解析到生物活性数据，从客户的询价到产品的售后服务，我们拥有着完善的管理体系，从而保证我们的服务更加高效、准确。努力为中国的医药行业发展注入新的活力，我们将成为您研发工作值得信赖的伙伴。

生物活性    
FIPI is a derivative of halopemide which potently inhibits both PLD1 and PLD2 with IC50s of 25 nM and 20 nM, respectively.

IC50 & Target    
IC50: 25 nM (PLD1), 20 nM (PLD2)

体外研究(In Vitro)    
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%[1]. 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[2]. FIPI attenuats the thimerosal-induced PLD activation, and the Hg-induced PLD activation in MAECs in a dose-dependent manner, and the agonist- and oxidant-induced PLD activation in a dose-dependent manner in MAECs[3].

分子量    
421.47

性状    
Solid

Formula    
C23H24FN5O2

CAS 号    
939055-18-2

中文名称    
5-氟-2-吲哚基脱氯卤培米特

运输条件    
Room temperature in continental US; may vary elsewhere.

储存方式    
Powder    -20°C    3 years
4°C    2 years
In solvent    -80°C    6 months
-20°C    1 month
溶解性数据    
In Vitro: 
DMSO : 14.67 mg/mL (34.81 mM; Need ultrasonic and warming)

配制储备液    
浓度溶剂体积质量    1 mg    5 mg    10 mg
1 mM    2.3726 mL    11.8632 mL    23.7265 mL
5 mM    0.4745 mL    2.3726 mL    4.7453 mL
10 mM    0.2373 mL    1.1863 mL    2.3726 mL
*
请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

参考文献

• [1]. Monovich L, et al. Optimization of halopemide for phospholipase D2 inhibition. Bioorg Med Chem Lett. 2007 Apr 15;17(8):2310-1.  [Content Brief]

  [2]. Su W, et al. 5-Fluoro-2-indolyl des-chlorohalopemide (FIPI), a phospholipase D pharmacological inhibitor that alters cell spreading and inhibits chemotaxis. Mol Pharmacol. 2009 Mar;75(3):437-46.  [Content Brief]

  [3]. Secor JD, et al. Novel lipid-soluble thiol-redox antioxidant and heavy metal chelator, N,N'-bis(2-mercaptoethyl)isophthalamide (NBMI) and phospholipase D-specific inhibitor, 5-fluoro-2-indolyl des-chlorohalopemide (FIPI) attenuate mercury-induced lipid si  [Content Brief]