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Tesmilifene fumarate {[allProObj[0].p_purity_real_show]}

货号:A1497082 同义名: DPPE fumarate;DPPE (fumarate)

Tesmilifene fumarate是 H1C 受体的拮抗剂,可广泛的增强化疗的细胞毒性,并保护正常细胞。

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Type HazMat fee for 500 gram (Estimated)
Excepted Quantity USD 0.00
Limited Quantity USD 15-60
Inaccessible (Haz class 6.1), Domestic USD 80+
Inaccessible (Haz class 6.1), International USD 150+
Accessible (Haz class 3, 4, 5 or 8), Domestic USD 100+
Accessible (Haz class 3, 4, 5 or 8), International USD 200+
Tesmilifene fumarate 化学结构 CAS号:1185241-83-1
Tesmilifene fumarate 化学结构
CAS号:1185241-83-1
Tesmilifene fumarate 3D分子结构
CAS号:1185241-83-1
Tesmilifene fumarate 化学结构 CAS号:1185241-83-1
Tesmilifene fumarate 3D分子结构 CAS号:1185241-83-1
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Tesmilifene fumarate 纯度/质量文件 产品仅供科研

货号:A1497082 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 H1 receptor H2 receptor H3 receptor H4 receptor Histamine receptor 其他靶点 纯度
Hydroxyzine 2HCl 99+%
Cyclizine 97%
Loratadine +

B(0)AT2, IC50: 4 μM

98%
Desloratadine ++

Histamine H1 receptor, IC50: 51 nM

98%
Doxylamine succinate 99%
Ebastine 98%
Tripelennamine HCl +

H1 receptor, IC50: 30 μM

98%
Meclizine dihydrochloride 98%
Chlorpheniramine maleate +++

Histamine H1 receptor, IC50: 12 nM

99%
Diphenhydramine HCl 99%
Alcaftadine ++++

H1 receptor, pKi: 8.5

++

H2 receptor, pKi: 7.2

99%+
Fexofenadine HCl ++

Histamine H1 receptor, IC50: 246 nM

99%+
Bilastine +++

H1 receptor, Ki: 44.15 nM

98%
Pemirolast potassium 98%
Bepotastine besilate +

Histamine H1 receptor, pIC50: 5.7

98%
Mizolastine +++

Histamine H1 receptor, IC50: 47 nM

98%
Brompheniramine maleate 98%
Carbinoxamine maleate salt 99+%
Clemastine fumarate ++++

Histamine H1 receptor, IC50: 3 nM

98%
Ketotifen fumarate salt 95%
Rupatadine Fumarate ++

Histamine H1 receptor, Ki: 102 nM

PAFR 98%
Famotidine 97%
Roxatidine Acetate HCl +

Histamine H2 receptor, IC50: 3.2 μM

98%
Lafutidine 99%
Cimetidine 98%
Nizatidine ++++

Histamine H2 receptor, IC50: 0.9 nM

AChE 98%
Ranitidine 98%
Betahistine +

Histamine H3 receptor, IC50: 1.9 μM

98%
Ciproxifan maleate +++

Histamine H3 receptor, IC50: 9.2 nM

99%+
S 38093 ++

human H3 receptor, Ki: 1.2 μM

rat H3 receptor, Ki: 1.44 μM

98%
JNJ-7777120 ++++

Histamine H4 receptor, Ki: 4.5 nM

98%
Azelastine HCl 98%
Epinastine HCl 98%
Levodropropizine 97%
Cyproheptadine hydrochloride 98%
Hesperetin 97%
Olopatadine HCl 98%
Mianserin hydrochloride 99+%
Buclizine 2HCl 97%
Latrepirdine 2HCl GluR 98%
Cetirizine 2HCl 98%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

Tesmilifene fumarate 生物活性

描述 Tesmilifene fumarate, also known as DPPE fumarate, is an antagonist of the H1C receptor. It enhances the effectiveness of various cytotoxic agents and may also provide some protection to normal cells[1][2]. Tesmilifene is thought to modulate the activity of 12(S)HETE within cancer cells and, as a result, may indirectly influence the susceptibility of cellular DNA to chemotherapy[1].

Tesmilifene fumarate 动物研究

Animal study Administered at a dose of 20 mg/kg subcutaneously and 20 μg intracerebroventricularly in 5 μL, Tesmilifene enhanced the seizure activity triggered by various convulsants[2].

Tesmilifene fumarate 参考文献

[1]Mark Vincent, et al. Tesmilifene may enhance breast cancer chemotherapy by killing a clone of aggressive, multi-drug resistant cells through its action on the p-glycoprotein pump. Med Hypotheses. 2006;66(4):715-31.

[2]G Sturman, et al. Modulation of the intracellular and H3-histamine receptors and chemically-induced seizures in mice Agents Actions. 1994 Jun;41 Spec No:C68-9.

Tesmilifene fumarate 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.50mL

0.50mL

0.25mL

12.52mL

2.50mL

1.25mL

25.03mL

5.01mL

2.50mL

Tesmilifene fumarate 技术信息

CAS号1185241-83-1
分子式C23H29NO5
分子量 399.48
别名 DPPE fumarate;DPPE (fumarate);Tesmilifene;BMS-217380-01
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Inert atmosphere,2-8°C

溶解度

DMSO: 250 mg/mL(625.81 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

动物实验配方
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