甲磺酸双氢麦角汀

甲磺酸双氢麦角汀用途

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。

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甲磺酸双氢麦角汀名称

[ CAS 号 ]:
24730-10-7

[ 中文名 ]:
双氢麦角汀甲磺酸盐

[ 英文名 ]:
Dihydroergocristine mesylate

[中文别名 ]:

二氢麦角亭甲烷硫酸盐

[英文别名 ]:

dihydroergocristine methanesulphonate
DIHYDROERGOCRYSTINE METHANESULFONATE SALT
dihydroergocristine methane sulfonate
Dihydroergocristine mesilate
9,10-DihydroergocristineMethanesulfonate
EINECS 246-434-6
dihydroergocristine methanesulfonate salt
PACAP 1-38
MFCD00153792
dihydroergocristinmesilat

甲磺酸双氢麦角汀生物活性

[ 描述 ]:

[ 相关类别 ]:

研究领域 >> 神经疾病

[体外研究]

二氢麦角克里斯蒂(DHEC)(2-20μm；24小时)的IC50值为25_μm,用于在不影响细胞活力的情况下抑制t100细胞中γ-分泌酶的活性[1]。二氢麦角克里斯蒂(2-20μm；24小时)抑制细胞Aβ的产生,并引起HEK293中app(app ctfs)羧基末端片段的剂量依赖性积聚,降低成纤维细胞中γ-分泌酶的活性[1]。Western blot分析[1]细胞系：wt-hek293细胞；成纤维细胞浓度：2μm、5μm、10μm、20μm孵育时间：24小时结果：剂量依赖性增加app-ctfs的积累。

[参考文献]

[1]. Lei X, et al. The FDA-approved natural product dihydroergocristine reduces the production of the Alzheimer's disease amyloid-β peptides. Sci Rep. 2015 Nov 16;5:16541.

甲磺酸双氢麦角汀物理化学性质

[ 沸点 ]:
899.3ºC at 760 mmHg

[ 分子式 ]:
C₃₆H₄₅N₅O₈S

[ 分子量 ]:
707.83600

[ 闪点 ]:
497.7ºC

[ 精确质量 ]:
707.29900

[ PSA ]:
180.96000

[ LogP ]:
3.50660

[ 外观性状 ]:
白色或近乎于白色,细结晶粉末

[ 蒸汽压 ]:
8.49E-35mmHg at 25°C

[ 储存条件 ]:
Store at RT

[ 水溶解性 ]:
H2O: 10 mg/mL

甲磺酸双氢麦角汀毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: KE7600000

CHEMICAL NAME :: Ergotamane-3',6',18-trione, 9,10-dihydro-12'-hydroxy-2'-(1-methylethyl)-5'-(pheny lmethyl)-, (5'-alpha,10-alpha)-, monomethanesulfonate (salt)

CAS REGISTRY NUMBER :: 24730-10-7

LAST UPDATED :: 199703

DATA ITEMS CITED :: 8

MOLECULAR FORMULA :: C35-H41-N5-O5.C-H4-O3-S

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 2643 mg/kg

TOXIC EFFECTS :: Behavioral - general anesthetic Behavioral - tremor Behavioral - convulsions or effect on seizure threshold

REFERENCE :: ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 42,1381,1992

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 585 mg/kg

TOXIC EFFECTS :: Behavioral - general anesthetic Behavioral - tremor Behavioral - convulsions or effect on seizure threshold

REFERENCE :: ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 42,1381,1992

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 91 mg/kg

TOXIC EFFECTS :: Behavioral - general anesthetic Behavioral - tremor Behavioral - convulsions or effect on seizure threshold

REFERENCE :: ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 42,1381,1992

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: >2500 mg/kg

TOXIC EFFECTS :: Behavioral - general anesthetic Behavioral - tremor Behavioral - convulsions or effect on seizure threshold

REFERENCE :: ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 42,1381,1992

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 120 mg/kg

TOXIC EFFECTS :: Behavioral - general anesthetic Behavioral - tremor Behavioral - convulsions or effect on seizure threshold

REFERENCE :: ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 42,1381,1992

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 70 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: USXXAM United States Patent Document. (U.S. Patent Office, Box 9, Washington, DC 20231) Volume(issue)/page/year: #4176182

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: >1250 mg/kg

TOXIC EFFECTS :: Behavioral - tremor Behavioral - excitement Gastrointestinal - nausea or vomiting

REFERENCE :: ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 42,1381,1992

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: >50 mg/kg

TOXIC EFFECTS :: Behavioral - tremor Behavioral - excitement Gastrointestinal - nausea or vomiting

REFERENCE :: ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 42,1381,1992

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甲磺酸双氢麦角汀安全信息

[ 危险品运输编码 ]:
UN 1544 6

[ WGK德国 ]:
2

[ RTECS号 ]:
KE7600000

[ 包装等级 ]:
III

[ 危险类别 ]:
6.1(b)

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