BMS-191011

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Chemical Structure| 202821-81-6 同义名 : BMS-A
CAS号 : 202821-81-6
货号 : A397321
分子式 : C16H10ClF3N2O3
纯度 : 99%+
分子量 : 370.71
MDL号 : MFCD09753285
存储条件：

Pure form Sealed in dry, room temperature

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(283.24 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：
生物活性
描述 Potassium (K+) channels participate in many physiological processes, cardiac function, cell proliferation, neuronal signaling, muscle contractility, immune function, hormone secretion, osmotic pressure, changes in gene expression, and are involved in critical biological functions, and in a variety of diseases[1]. BMS-191011 (BMS-A) is an opener of the large-conductance, Ca2+-activated potassium (maxi-K) channel, effective in stroke models[2]. BMS-191011 (10-100 µg/kg, i.v.) and NS 1619 (0.1-1.0 µg/kg, i.v.) increased the diameter of retinal arterioles without altering systemic blood pressure and heart rate significantly. The vasodilator responses to BMS-191011 were significantly diminished by intravitreal injection of iberiotoxin (an inhibitor of BK(Ca) channels, 20 pmol/eye)[3]. A 29-day treatment with L-citrulline, significantly ameliorated the impaired acetylcholine- and BMS-191011-induced retinal vasodilation in diabetic rats without affecting their plasma glucose levels[4]. BMS 191011 caused fetal coronary artery relaxation and BKCa current activation that was unaffected by maternal nutrient restriction[5].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.70mL

0.54mL

0.27mL

13.49mL

2.70mL

1.35mL

26.98mL

5.40mL

2.70mL
参考文献

[1]Vivek K Vyas,et al. Medicinal Chemistry of Potassium Channel Modulators: An Update of Recent Progress (2011-2017). Curr Med Chem. 2019. 26(12), 2062-2084.

[2]Romine JL, et al. 3-[(5-Chloro-2-hydroxyphenyl)methyl]-5-[4-(trifluoromethyl)phenyl ]-1,3,4-oxadiazol-2(3H)-one, BMS-191011: opener of large-conductance Ca(2+)-activated potassium (maxi-K) channels, identification, solubility, and SAR. J Med Chem. 2007. 50(3), 528-42.

[3]Asami Mori,et al. BMS-191011, an opener of large-conductance Ca2+-activated potassium channels, dilates rat retinal arterioles in vivo. Biol Pharm Bull. 2011. 34(1), 150-2.

[4]Asami Mori,et al. L-Citrulline ameliorates the attenuation of acetylcholine-induced vasodilation of retinal arterioles in diabetic rats. Heliyon. 2021. 7(3), e06532.

[5]Praveen Shukla,et al. Maternal nutrient restriction during pregnancy impairs an endothelium-derived hyperpolarizing factor-like pathway in sheep fetal coronary arteries. Am J Physiol Heart Circ Physiol. 2014. 307(2), H134-42.