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939055-18-2

中文名稱(chēng) FIPI
英文名稱(chēng) FIPI
CAS 939055-18-2
分子式 C23H24FN5O2
分子量 421.47
MOL 文件 939055-18-2.mol
更新日期 2024/07/08 16:38:20
939055-18-2 結(jié)構(gòu)式 939055-18-2 結(jié)構(gòu)式

基本信息

中文別名
化合物FIPI
5-氟-2-吲哚基脫氯鹵培米特
英文別名
FIPI
CS-1511
FIPI HYDROCHLORIDE
5-Fluoro-2-Indolyl des-Chlorohalopemide
5-fluoro-N-[2-[4-(2-oxo-3H-benzimidazol-1-yl)piperidin-1-yl]ethyl]-1H-indole-2-carboxamide
N-[2-[4-(2,3-Dihydro-2-oxo-1H-benzimidazol-1-yl)-1-piperidinyl]ethyl]-5-fluoro-1H-indole-2-carboxamide
N-[2-[4-(2,3-Dihydro-2-oxo-1H-benzimidazol-1-yl)-1-piperidinyl]ethy]-5-fluoro-1H-indole-2-carboxamide hydrochloride
所屬類(lèi)別
生物化工:激動(dòng)劑抑制劑

物理化學(xué)性質(zhì)

密度1.349±0.06 g/cm3(Predicted)
儲(chǔ)存條件-20°C儲(chǔ)存
溶解度DMSO : 14.67 mg/mL (34.81 mM; Need ultrasonic and warming)
酸度系數(shù)(pKa)12.04±0.30(Predicted)
形態(tài)粉末
顏色Light yellow to khaki
FIPI價(jià)格(試劑級(jí))
報(bào)價(jià)日期產(chǎn)品編號(hào)產(chǎn)品名稱(chēng)CAS號(hào)包裝價(jià)格
2024/11/08HY-12807FIPI
FIPI
939055-18-25mg850元
2024/11/08HY-12807FIPI
FIPI
939055-18-210mM * 1mLin DMSO935元
2024/11/08HY-12807FIPI
FIPI
939055-18-210mg1100元

常見(jiàn)問(wèn)題列表

生物活性
FIPI (5-Fluoro-2-indolyl deschlorohalopemide) 是一種鹵培米特 (halopemide)的衍生物,是一種有效且選擇性的 phospholipase D 抑制劑,對(duì) PLD1 和 PLD2 的IC50值分別為25 nM和20 nM。
靶點(diǎn)
TargetValue
PLD2
(Cell-free assay)
20 nM
PLD1
(Cell-free assay)
25 nM
體外研究

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. 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.

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