地诺前列素

PGF-2α类药物生物活性靶点体外研究地诺前列素试剂级价格

地诺前列素

CAS号:551-11-1
英文名:Prostaglandin F2a
中文名:地诺前列素
CBNumber:CB3161368
分子式:C20H34O5
分子量:354.49
MOL File:551-11-1.mol

地诺前列素化学性质

熔点 :25-35°
比旋光度 :D25 +23.5° (c = 1 in tetrahydrofuran)
沸点 :407.69°C (rough estimate)
密度 :1.0458 (rough estimate)
折射率 :1.6120 (estimate)
储存条件 :Store at -20°C
溶解度 :DMSO:100.0(Max Conc. mg/mL);282.1(Max Conc. mM)
Water:100.0(Max Conc. mg/mL);282.1(Max Conc. mM)
酸度系数(pKa) :pKa 4.90(H2O,t=25±2,I=0.0，c<0.01,N2) (Uncertain)
形态 :Low melting white solid or colorless oil.
颜色 :White to light brown
InChIKey :PXGPLTODNUVGFL-JPYXJAOSNA-N
SMILES :C([C@H]1[C@H](C[C@@H](O)[C@@H]1/C=C/[C@@H](O)CCCCC)O)/C=C\CCCC(=O)O |&1:1,2,4,6,9,r|
CAS 数据库 :551-11-1(CAS DataBase Reference)

安全信息

毒害物质数据 :551-11-1(Hazardous Substances Data)
毒性 :LD50 in rabbits (mg/kg): 2.5-5.0 i.v.; 2.5-5.0 i.m. (Fujita)

地诺前列素 MSDS

(5Z,9a,11a,13E,15S)-9,11,15-Trihydroxyprosta-5,13-diene-1-oic acid

地诺前列素性质、用途与生产工艺

PGF-2α类药物地诺前列素是天然的前列腺素 F2α (PGF2α)，可直接作用于子宫肌层，刺激妊娠子宫使子宫肌收缩，并可使子宫颈变软和扩张，故可用于人工流产和晚期引产。但是由于地诺前列素的常温下性质不稳定、保存与运输不方便、合成工艺复杂、成本高等局限性，地诺前列素的应用较难普及。加之后来发现米索联合米非司酮可以取得更好的人工流产效果，地诺前列素逐渐淡出人们的视野。
生物活性 Dinoprost (Prostaglandin F2α) 是一种口服有效的前列腺素 F (PGF) 受体 (FP receptor) 激动剂。Dinoprost 是在子宫内膜腔上皮和黄体 (CL) 中局部产生的溶酶激素。Dinoprost 在分娩过程中起关键作用。
靶点

Human Endogenous Metabolite

FP Receptor

体外研究

Dinoprost (Prostaglandin F2α; 1 μM; for 24 hours) induces ER stress, autophagy, and apoptosis in goat luteal cells.
Dinoprost (1 μM; for 24 hours) significantly increases the expression of GRP78 and UPR sensors.

Apoptosis Analysis

Cell Line:	Goat luteal cells
Concentration:	1 μM
Incubation Time:	For 24 hours
Result:	Significantly increased the apoptotic rate (15.62±3.12%).

Cell Autophagy Assay

Cell Line:	Goat luteal cells
Concentration:	1 μM
Incubation Time:	For 24 hours
Result:	There was extensive overlap between LC3 and LAMP1 in luteal cells and autophagolysosomes were formed in goat luteal cells.

Western Blot Analysis

Cell Line:	Goat luteal cells
Concentration:	1 μM
Incubation Time:	For 24 hours
Result:	The expression of GRP78 and UPR sensors including cleaved ATF6, phosphorylated-EIF2S1, EIF2S1, ATF4, phosphorylated-IRE1, autophagy-related protein LC3-II, and pro-apoptosis factor cleaved Caspase3 increased significantly in the cells.