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Carbinoxamine maleate salt {[allProObj[0].p_purity_real_show]}

货号:A242556 同义名: Carbinoxamine (maleate);CarbinoxaMine Maleate

Carbinoxamine maleate is a blocker of histamine-H1 receptor with antihistamine and anticholinergic effects.

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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+
Carbinoxamine maleate salt 化学结构 CAS号:3505-38-2
Carbinoxamine maleate salt 化学结构
CAS号:3505-38-2
Carbinoxamine maleate salt 3D分子结构
CAS号:3505-38-2
Carbinoxamine maleate salt 化学结构 CAS号:3505-38-2
Carbinoxamine maleate salt 3D分子结构 CAS号:3505-38-2
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Carbinoxamine maleate salt 纯度/质量文件 产品仅供科研

货号:A242556 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 99%
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。

Carbinoxamine maleate salt 生物活性

靶点
  • H1 receptor

描述 Carbinoxamine maleate is a histamine-H1 receptor blocking agent with antihistamine and anticholinergic properties[3]. Carbinoxamine maleate is an antihistamine drug with mild sedation effects, which is used to treat seasonal and perennial allergic rhinitis clinically[4]. The short half-life and bitter taste of carbinoxamine maleate (CAM) lead to poor compliance by pediatric patients who are being treated for allergic rhinitis. The homemade preparations had release behaviors similar to that of the reference in vitro and achieved sustained release in vivo. The low drug loading preparation had a higher relative bioavailability of 109% owing to its faster release and better dispersibility. The suspensions based on MCRCs (microencapsulated carbinoxamine-resin complexes) could be successfully applied to treating allergic rhinitis in children[5].

Carbinoxamine maleate salt 参考文献

[1]Ramadan AA, Mandil H. Spectrophotometric determination of carbinoxamine maleate in pharmaceutical formulations by ternary complex formation with Cu(II) and eosin. Anal Biochem. 2006 Jun 1;353(1):133-7. Epub 2006 Mar 9.

[2]Mansour AM. Determination of pseudoephedrine hydrochloride and carbinoxamine maleate in combination drug formulation by liquid chromatography. J AOAC Int. 1998 Sep-Oct;81(5):958-62.

[3]LiverTox: Clinical and Research Information on Drug-Induced Liver Injury [Internet]. Bethesda (MD): National Institute of Diabetes and Digestive and Kidney Diseases; 2012–. Carbinoxamine. 2017 Jan 16. PMID: 31643335

[4]Li P, Xiao J, Liu J, Liu R, Bi K, Li Q. Development and full validation of a liquid chromatography-tandem mass spectrometry method for determination of carbinoxamine in beagle plasma and its application to a pharmacokinetic study. J Chromatogr B Analyt Technol Biomed Life Sci. 2018 Sep 1;1093-1094:183-189

[5]Deng Y, Wang T, Li J, Sun W, He H, Gou J, Wang Y, Yin T, Zhang Y, Tang X. Studies on the in vitro ion exchange kinetics and thermodynamics and in vivo pharmacokinetics of the carbinoxamine-resin complex. Int J Pharm. 2020 Oct 15;588:119779

Carbinoxamine maleate salt 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.46mL

0.49mL

0.25mL

12.29mL

2.46mL

1.23mL

24.58mL

4.92mL

2.46mL

Carbinoxamine maleate salt 技术信息

CAS号3505-38-2
分子式C20H23ClN2O5
分子量 406.86
别名 Carbinoxamine (maleate);CarbinoxaMine Maleate;NSC 62362
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Keep in dark place,Sealed in dry,Room Temperature

溶解度

DMSO: 105 mg/mL(258.07 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

H2O: 50 mg/mL(122.89 mM),配合低频超声助溶

动物实验配方

PO 0.5% CMC-Na 40 mg/mL clear

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