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马来酸二甲茚定

马来酸二甲茚定用途

马来酸二甲酯是一种具有抗组胺作用的选择性组胺H1拮抗剂。马来酸二甲酯可用于超敏反应的研究[1][2][3]。
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马来酸二甲茚定名称

[ CAS 号 ]:
3614-69-5

[ 中文名 ]:
马来酸二甲茚定

[ 英文名 ]:
UNII:6LL60J9E0O

[英文别名 ]:

马来酸二甲茚定生物活性

[ 描述 ]:

马来酸二甲酯是一种具有抗组胺作用的选择性组胺H1拮抗剂。马来酸二甲酯可用于超敏反应的研究[1][2][3]。

[ 相关类别 ]:

信号通路 >> 免疫及炎症 >> 组胺受体
研究领域 >> 炎症/免疫
信号通路 >> G 蛋白偶联受体/G 蛋白 >> 组胺受体

[ 靶点 ]

Human Endogenous Metabolite


[体外研究]

马来酸二甲辛酯(1-1000μM)以浓度依赖和可逆的方式抑制色甘醇诱导的/格列本脲敏感的K+电流,IC50值为29.5μM[2]。马来酸二甲酯(1-1000μM)抑制Y-26763诱导的格列本脲敏感K+电流,IC50值为49μM[2]。

[体内研究]

马来酸二甲辛酯(0.25 mg;腹腔注射一次)影响小鼠伤口愈合[1]。动物模型:伤口愈合的C57BL/6小鼠[1]剂量:0.25 mg给药:腹膜内注射;0.25 mg一次结果:显著延迟皮肤伤口,仅在伤口愈合初期显示伤口闭合受损。

马来酸二甲茚定物理化学性质

[ 沸点 ]:
416.3ºC at 760mmHg

[ 熔点 ]:
159-161℃

[ 分子式 ]:
C24H28N2O4

[ 分子量 ]:
408.490

[ 闪点 ]:
205.6ºC

[ 精确质量 ]:
408.204895

[ PSA ]:
90.73000

[ LogP ]:
3.85850

[ 储存条件 ]:
室温

[ 水溶解性 ]:
Slightly soluble in water, soluble in methanol

马来酸二甲茚定毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :
UT0830000
CAS REGISTRY NUMBER :
3614-69-5
LAST UPDATED :
199106
DATA ITEMS CITED :
4
MOLECULAR FORMULA :
C20-H24-N2.C4-H4-O4
MOLECULAR WEIGHT :
408.54
WISWESSER LINE NOTATION :
L56 BHJ C2N1&1 DY1&- BT6NJ &QV2VQ

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 :
618 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
TXAPA9 Toxicology and Applied Pharmacology. (Academic Press, Inc., 1 E. First St., Duluth, MN 55802) V.1- 1959- Volume(issue)/page/year: 3,534,1961
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
26800 ug/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
TXAPA9 Toxicology and Applied Pharmacology. (Academic Press, Inc., 1 E. First St., Duluth, MN 55802) V.1- 1959- Volume(issue)/page/year: 3,534,1961
TYPE OF TEST :
LDLo - Lowest published lethal dose
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Mammal - dog
DOSE/DURATION :
50 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
TXAPA9 Toxicology and Applied Pharmacology. (Academic Press, Inc., 1 E. First St., Duluth, MN 55802) V.1- 1959- Volume(issue)/page/year: 3,534,1961
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - guinea pig
DOSE/DURATION :
888 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
TXAPA9 Toxicology and Applied Pharmacology. (Academic Press, Inc., 1 E. First St., Duluth, MN 55802) V.1- 1959- Volume(issue)/page/year: 3,534,1961
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马来酸二甲茚定安全信息

[ 危害码 (欧洲) ]:
Xn

[ 海关编码 ]:
2933399090

马来酸二甲茚定海关

[ 海关编码 ]: 2933399090

[ 中文概述 ]:
2933399090. 其他结构含非稠合吡啶环的化合物. 增值税率:17.0%. 退税率:13.0%. 监管条件:无. 最惠国关税:6.5%. 普通关税:20.0%

[ 申报要素 ]: 品名, 成分含量, 用途, 乌洛托品请注明外观, 6-己内酰胺请注明外观, 签约日期

[ Summary ]:
2933399090. other compounds containing an unfused pyridine ring (whether or not hydrogenated) in the structure. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

马来酸二甲茚定文献

Chiral separation of alkylamine antihistamines in pharmaceuticals by capillary isotachophoresis with charged cyclodextrin.

Drug Dev. Ind. Pharm. 33(11) , 1199-204, (2007)

Cyclodextrin-mediated capillary isotachophoresis (ITP) in cationic regime of the separation was developed for the separation and quantitation of alkylamine antihistamine dimethindene (DIM) and phenira...

Identification of a novel selective H1-antihistamine with optimized pharmacokinetic properties for clinical evaluation in the treatment of insomnia.

Bioorg. Med. Chem. Lett. 20(19) , 5874-8, (2010)

Analogs of the known H(1)-antihistamine R-dimethindene with suitable selectivity for key GPCRs, P450 enzymes and hERG channel were assessed for metabolism profile and in vivo properties. Several analo...

Identification and determination of ketotifen hydrogen fumarate, azelastine hydrochloride, dimetindene maleate and promethazine hydrochloride by densitometric method.

Acta Pol. Pharm. 70(6) , 951-9, (2013)

Conditions for determination of: ketotifen hydrogen fumarate, azelastine hydrochloride, dimetindene maleate and promethazine hydrochloride by densitometric method in substances and pharmaceuticals wer...


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公司名:上海创赛科技有限公司

区域:上海市嘉定区

价格:
¥343.0/1g ¥1016.0/5g ¥3713.0/25g

联系人:夏言

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