Phentolamine Mesylate|65-28-1|(甲磺酸酚妥拉明; Phentolamine methanesulfonate)-陌孚医药/Medlife

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Phentolamine Mesylate (Synonyms: 甲磺酸酚妥拉明; Phentolamine methanesulfonate)

目录号: PC10723 纯度: ≥98%

CAS No. :65-28-1

商品编号	规格	价格	会员价	是否有货	数量
PC10723-100mg	100mg	¥470.40	请登录
PC10723-10mM (in 1mL DMSO)	10mM (in 1mL DMSO)	¥490.00	请登录

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中文名称	Phentolamine Mesylate
中文别名	甲磺酸酚妥拉明;酚胺唑啉马来酸盐;瑞支亭甲基磺酸盐;甲磺酸酚妥拉明(立其丁);酚妥拉明甲磺酸盐;酚胺唑啉;酚妥拉明甲烷磺酸盐;2-(N-[M-羟基苯基]-P-甲苯氨基甲基)咪唑啉;Phentolamine Mesylate 甲磺酸酚妥拉明;甲磺酸酚妥拉明 EP标准品;甲磺酸酚妥拉明 USP标准品;甲磺酸酚妥拉明标准品;甲磺酸酚妥拉明,BR;甲磺酸酚妥拉明用于系统适应性 EP标准品;2-[N-(间羟基)-对甲苯胺甲基]-2-咪唑啉甲磺酸盐;2-[N-(间羟基苯基)对甲苯氨基甲基]-2-咪唑啉甲磺酸盐;甲烷磺酸芬妥胺;立其丁;瑞支亭
英文名称	Phentolamine Mesylate
英文别名	PHENTOLAMINE MESYLATE;REGITIN;REGITIN MESYLATE;PHENTOLAMINE MESILATE;PHENTOLAMINE METHANESULFONATE;PHENTOLAMINE METHANESULFONATE SALT;VASOMAX;m-(n-(2-imidazolin-2-ylmethyl)-p-toluidino)-phenomonomethanesulfonate(sal;Phentolamine (mesylate);Phentolamine Methane;2-[N-(m-Hydroxyphenyl)-p-toluidinomethyl]imidazoline Methanesulfonate;3-[N-(2-Imidazolin-2-ylmethyl)-p-toluidino]phenol methanesulphonate;3,6,9,23,26,29,32,35,49,52,55,69,72,75,78,81,84-Heptadecaoxatridecacyclo[65.28.1.111,37.121,47.157,8;3,6,9,23,26,29,32,35,49,52,55,69,72,75,78,81,84-Heptadecaoxatridecacyclo[65.28.1.111,37.121,47.157,8;3,6,9,23,26,29,32,35,49,52,55,69,72,75,78,81,84-Heptadecaoxatridecacyclo[65.28.1.111,37.121,47.157,8
Cas No.	65-28-1
分子式	C₈₂H₉₂O₁₇
分子量	1349.60
包装储存	4°C, sealed storage, away from moisture and light *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

生物活性

Phentolamine mesylate (Phentolamine methanesulfonate) is a reversible, non-selective, and orally active blocker of α1 and α2 adrenergic receptor that expands blood vessels to reduce peripheral vascular resistance. Phentolamine mesylate can be used for the research of pheochromocytoma-related hypertension, heart failure and erectile dysfunction.

性状

Solid

IC50 & Target[1][2]

α-adrenergic

体外研究(In Vitro)

Phentolamine (0.1-1 μM) inhibits the response to Clonidine in rat ileum, with the pA₂ and pK_B of 7.92 and 8.07, respectively.
Phentolamine (10-70 μg/mL; 48 h) inhibits proliferation of HDMECs and HBMECs in a dose-dependent manner, with IC₅₀s of 50 μg/mL and 30 μg/mL without toxicity, respectively.
Phentolamine (10-20 or 20-40 μg/mL; 12-48 h) signi?cantly delays scratch wound closure of HBMECs and HDMECs in a dose-dependent manner.
Phentolamine (30 or 50 μg/mL; 4-12 h) inhibits tube formation of HBMECs and HDMECs.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(In Vivo)

Phentolamine (1 mg/kg; i.v.) produces hypotension and tachycardia in rats.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

运输条件

Room temperature or refrigerated transportation.

储存方式

4°C, sealed storage, away from moisture and light

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

ClinicalTrial

参考文献

[1]. Gould L, et, al. Phentolamine. Am Heart J. 1976 Sep;92(3):397-402. [Information]

[2]. Goldstein I, et, al. Oral phentolamine: an alpha-1, alpha-2 adrenergic antagonist for the treatment of erectile dysfunction. Int J Impot Res. 2000 Mar;12 Suppl 1:S75-80. [Information]

[3]. Liu L, et, al. Evidence for functional alpha 2D-adrenoceptors in the rat intestine. Br J Pharmacol. 1996 Mar;117(5):787-92. [Information]

[4]. Pan L, et, al. Phentolamine inhibits angiogenesis 体外研究: Suppression of proliferation migration and differentiation of human endothelial cells. Clin Hemorheol Microcirc. 2017;65(1):31-41. [Information]

[5]. Fioretti AC, et, al. Renal and femoral venous blood flows are regulated by different mechanisms dependent on α-adrenergic receptor subtypes and nitric oxide in anesthetized rats. Vascul Pharmacol. 2017 Dec;99:53-64. [Information]

溶解度数据

体外研究:

H₂O : ≥ 50 mg/mL (132.46 mM)

* "≥" means soluble, but saturation unknown.

配制储备溶液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.6493 mL	13.2464 mL	26.4929 mL
5 mM	0.5299 mL	2.6493 mL	5.2986 mL
10 mM	0.2649 mL	1.3246 mL	2.6493 mL

产品不同，其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液；配成溶液后，建议分装保存，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°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)。-80°C 储存时，建议在 6 个月内使用，-20°C 储存时，建议在 1 个月内使用。

体内研究:

建议根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都建议先按照 体外研究 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

建议依照次序添加每种溶剂： PBS
Solubility: 100 mg/mL (264.93 mM); Clear solution; Need ultrasonic
2.

建议依照次序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.5 mg/mL (6.62 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (6.62 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

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产品使用指南

Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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