Almitrine mesylate
目录号: PL09977 纯度: ≥99.0%
CAS No. :29608-49-9
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中文名称
Almitrine mesylate
中文别名
甲磺酸阿米三嗪;N,N'-二烯丙基-6-[4-[二(4-氟苯基)甲基]哌嗪-1-基]-1,3,5-三嗪-2,4-二胺二甲磺酸盐;二甲磺酸阿米三嗪;甲磺酸阿米三嗪,企标;他克莫司;二甲基阿咪三嗪
英文名称
Almitrine mesylate
英文别名
N,N'-diallyl-6-[4-[bis(4-fluorophenyl)methyl]piperazin-1-yl]-1,3,5-triazine-2,4-diamine dimethanesulphonate;Almitrine dimesylate;2,4-bis(allylamino)-6-[4-[bis(p-fluorophenyl)methyl]-1-piperazinyl]-s-triazine dimethanesulfonate;ALMITRINE BISMESYLATE;ALMITRINE DIMESILATE;S2620 bismethanesulfonate;Almitrine (Vectarion);Almitrine mesylate;Almitrine dimethanesulfonate;Vectarion;Almitrine mesylate [USAN];6RY6V6XM8T;S 2620 bismethanesulfonate;Almitrine bismethane sulfonate;N2,N4-Diallyl-6-(4-(bis(4-fluorophenyl)methyl)piperazin-1-yl)-1,3,5-triazine-2,4-diamine dimethanesulfonate;Almitrine mesylate (USAN);(Diallylamino-4'-6'-triazinyl-2')-1-(bis p-fluorobenzydryl)-4 piperazine bis methanesulfonate;2,4-Bis(allyl
Cas No.
29608-49-9
分子式
C28H37F2N7O6S2
分子量
669.76
包装储存
4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
产品详情
Almitrine mesylate 是一种外周化学感受器的激动剂,选择性抑制 Ca2+依赖性的 K+ 通道。
生物活性
Almitrine mesylate, a peripheral chemoreceptor agonist, inhibits selectively the Ca-dependent K channel.
性状
Solid
IC50 & Target[1][2]
K channel
体外研究(In Vitro)
Almitrine inhibits the activity of a high-conductance (152±13 pS), Ca-dependent K channel by decreasing its open probability. The IC50 value of the effect is 0.22 μM. The inhibitory effect of Almitrine on Ca-dependent K channels also is observed in GH3 cells. Almitrine at concentrations up to 10 μM does not affect whole-cell voltage-dependent K, Ca, or Na currents in rat or rabbit cells. However, this concentration of Almitrine significantly inhibits the Ca-dependent component of K currents in rat chemoreceptor cells. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
Almitrine acts via the peripheral arterial chemoreceptors raising carotid sinus nerve output and minute ventilation. Almitrine also has a pulmonary vascular action causing a dose-dependent constriction and dilatation. At low doses Almitrine enhances hypoxic pulmonary vasoconstriction and may improve the overall ventilation/perfusion ratio. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
参考文献
[1]. López-López JR, et al. Effects of Almitrine bismesylate on the ionic currents of chemoreceptor cells from the carotid body. Mol Pharmacol. 1998 Feb;53(2):330-9.
[2]. Bee D, et al. An analysis of the action of an analogue of Almitrine bismesylate in the rat model of hypoxic lung disease. Exp Physiol. 1992 Nov;77(6):819-28.
溶解度数据
In Vitro: DMSO : 100 mg/mL (149.31 mM; Need ultrasonic)配制储备液
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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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