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Pheniramine Maleate
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Pheniramine Maleate图片
CAS NO:132-20-7
包装与价格:
包装价格(元)
10 mM * 1 mL in Water电议
100mg电议
500mg电议
1 g电议
5 g电议

产品名称
马来酸非尼拉敏
Prophenpyridamine maleate
Tripoton maleate
产品介绍
Pheniramine (Prophenpyridamine; Tripoton) maleate 是第一代组胺H1受体拮抗剂,作用于中枢神经系统 (CNS) ,产生镇静、助眠的作用。Pheniramine maleate 也是安全、有效的局部麻醉剂,并有止痒作用。
生物活性

Pheniramine (Prophenpyridamine; Tripoton) maleate is a first-generationhistamine H1 receptorantagonist, acts on the central nervous system (CNS) with sedative and hypnotic effect. Pheniramine maleate displays antitumor effect and induces leukemia cellsapoptosis. Pheniramine maleate is also a safe and effective local anesthetic, with antipruritic effects[1][2][3][4].

IC50& Target

H1Receptor

1.01 mM (IC50)

体外研究
(In Vitro)

Pheniramine maleate inhibits CYP2D6, the specific P450-isozymes, to delay metabolic time and prolong antihistaminic effects[1].
Pheniramine maleate regulates cellular Ca2+transmembrane action, and inhibits Ca2+influx into BC3H-1 cells by inhibiting histamine with an IC50value of 1.01 mM[2].
Pheniramine maleate (0.5, 1.0 mM; 24 h) induces cell apoptosis in human T-cell acute lymphoblastic leukemia cell lines[3].
Pheniramine maleate (1 μM-1 mM; 12-48 h) inhibits cell proliferation in a time-dependent manner and shows inhibitory concentration IC50s of 550 μM (CCRF-CEM cells) and 420 μM (Jurkat cells), respectively[3].

Cell Viability Assay[3]

Cell Line:Human T-cell acute lymphoblastic leukemia cell lines: CCRF-CEM and Jurkat ALL
Concentration:0.5, 1.0 mM
Incubation Time:24 hours
Result:Induced cells apoptosis with chromatin condenses and marginalizes, and nuclear debris spreaded into the cytoplasm.

Cell Viability Assay[3]

Cell Line:Human T-cell acute lymphoblastic leukemia cell lines: CCRF-CEM and Jurkat ALL
Concentration:1 μM-1 mM
Incubation Time:12, 24, 48 hours
Result:Inhibited cell proliferation and survival in a time- and dose-dependent manner.
体内研究
(In Vivo)

Pheniramine maleate (1.75 μM; i.t.) exerts local anesthesia effect and results spinal block in rats[4].

Animal Model:Sprague–Dawley rats (300-350 g; male)[4]
Dosage:0.30, 0.60, 0.90, 1.50, 1.75 μM
Administration:Intrathecal injection; one time
Result:Resulted the spinal block and displayed dose-dependent effect.
Showed 100% blockades in motor function, proprioception, and nociception, with full recoveryduration of action about 41, 56, and 88 min, respectively, at 1.75 μM.
分子量

356.42

性状

Solid

Formula

C20H24N2O4

CAS 号

132-20-7

中文名称

马来酸非利拉明 (右氯苯那敏EP杂质A 马来酸盐)

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据
In Vitro: 

H2O : ≥ 38 mg/mL(106.62 mM)

*"≥" means soluble, but saturation unknown.

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM2.8057 mL14.0284 mL28.0568 mL
5 mM0.5611 mL2.8057 mL5.6114 mL
10 mM0.2806 mL1.4028 mL2.8057 mL
*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80℃, 6 months; -20℃, 1 month (sealed storage, away from moisture)。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。