甲磺酸双氢麦角汀

中文名称:

甲磺酸双氢麦角汀

中文同义词:

甲磺酸双氢麦角汀;甲磺酰双氢麦角克碱;二氢麦角碱(甲磺酸盐);二氢麦角亭甲烷硫酸盐;双氢麦角汀 甲磺酸盐;甲磺酸双氢麦角汀 EP标准品

英文名称:

DIHYDROERGOCRISTINE MESYLATE

英文同义词:

(5’-alpha,10-alpha)-nylmethyl)monomethanesulfonate(salt);(5alpha, 10alpha)-9,10-Dihydro-12-hydroxy-2-(1-methylethyl)-5-(phenylmethyl)-ergotaman-3,6,18-trione mesylate;C13168;(5α,10α)-9,10-Dihydro-12-hydroxy-2-(1-methylethyl)-5-(phenylmethyl)-ergotaman-3,6,18-trionemesylate;9,10-dihydro-ergocristinmonomethanesulfonate(salt);dihydroergocristinmesilat;ergotamane-3’,6’,18-trione,9,10-dihydro-12’-hydroxy-2’-(1-methylethyl)-5’-(phe;5alpha-benzyl-9,10alpha-dihydro-12-hydroxy-2-isopropylergotaman-3,6,18-trione monomethanesulphonate

CAS号:

24730-10-7

分子式:

C36H45N5O8S

分子量:

707.84

EINECS号:

246-434-6

相关类别:

化工原料;Organics;DID - DINDrugs of Abuse;ErgotamineForensic and Veterinary Standards;AlkaloidsAlphabetic;Chemical Structure;D;Drugs of Abuse;DrugsMetabolites;Neat Compounds;Serotonin receptor

Mol文件:

24730-10-7.mol

熔点 

210 °C

储存条件 

Store at RT

溶解度 

H2O: 10 mg/mL

形态

neat

生物活性

Dihydroergocristine mesylate (DHEC mesylate) 是γ-secretase (GSI) 的抑制剂, 可减少阿尔茨海默氏病淀粉样蛋白 β 肽 (amyloid-β) 的产生, 与 γ-secretase 和 Nicastrin 结合的平衡解离常数 (Kd) 值分别为 25.7 nM 和 9.8 μM。

体外研究

Dihydroergocristine (DHEC) (2-20 μM; 24 hours) has an IC 50 value of 25 μM for inhibiting the activity of γ-secretase in T100 cells without affecting cell viability. Dihydroergocristine (2-20 μM; 24 hours) inhibits cellular Aβ production and causes a dose-dependent accumulation of carboxy-terminal fragments of APP (APP-CTFs) in HEK293 and decreases γ-secretase activity in fibroblast cells. Western Blot Analysis Cell Line: WT HEK293 cells; Fibroblast cells Concentration: 2 μM, 5 μM, 10 μM, 20 μM Incubation Time: 24 hours Result: Increased APP-CTFs accumulation in a dose-dependent manner.

Cell Line:

WT HEK293 cells; Fibroblast cells

Concentration:

2 μM, 5 μM, 10 μM, 20 μM

Incubation Time:

24 hours

Result:

Increased APP-CTFs accumulation in a dose-dependent manner.

危险品运输编号 

UN 1544 6.1/PG 2

WGK Germany 

2

RTECS号

KE7600000

HazardClass 

6.1(b)

PackingGroup 

III

海关编码 

29396900