Diazoxide-d3
(Synonyms: 二氮嗪D3,Sch-6783-d3; SRG-95213-d3) 目录号 : GC46131An internal standard for the quantification of diazoxide
Cas No.:1432063-51-8
Sample solution is provided at 25 µL, 10mM.
Diazoxide-d3 is intended for use as an internal standard for the quantification of diazoxide by GC- or LC-MS. Diazoxide is an activator of sulfonylurea receptor 1 (SUR1) linked to ATP-sensitive potassium channel Kir6.2 (EC50 = 14.1 μM in a FLIPR assay using HEK293 cells).1 It also activates SUR2A/Kir6.2 and SUR2B/Kir6.2 channels in HEK293T cells in a patch-clamp assay when used at concentrations of 30 and 300 μM.2 Diazoxide inhibits glucose-induced insulin release from isolated rat pancreatic β cells and induces relaxation of isolated rat aortic rings precontracted with potassium chloride (IC50s = 22.6 and 22.4 μM, respectively).3 It reduces mean arterial pressure and cerebral blood flow in spontaneously hypertensive rats when administered intravenously as a 5 mg/kg bolus dose.4 Diazoxide (50 mg/kg, i.p.) increases blood glucose levels in mice.5 Formulations containing diazoxide have been used in the treatment of hypoglycemia.
|1. Gopalakrishnan, M., Molinari, E.J., Char-Change, S., et al. Pharmacology of human sulphonylurea receptor SUR1 and inward rectifier K+ channel Kir6.2 combination expressed in HEK-293 cells. Br. J. Pharmacol. 129(7), 1323-1332 (2000).|2. Matsuoka, T., Matsushita, K., Katayama, Y., et al. C-Terminal tails of sulfonylurea receptors control ADP-induced activation and diazoxide modulation of ATP-sensitive K+ channels. Circ. Res. 87(10), 873-880 (2000).|3. de Tullio, P., Becker, B., Boverie, S., et al. Toward tissue-selective pancreatic B-cells KATP channel openers belonging to 3-alkylamino-7-halo-4H-1,2,4-benzothiadiazine 1,1-dioxides. J. Med. Chem. 46(15), 3342-3353 (2003).|4. Barry, D.I., Strandgaard, S., Graham, D.I., et al. Effect of diazoxide-induced hypotension on cerebral blood flow in hypertensive rats. Eur. J. Clin. Invest. 13(3), 201-207 (1983).|5. Foy, J.M., and Furman, B.L. Effect of single dose administration of diuretics on the blood sugar of alloxan-diabetic mice or mice made hyperglycaemic by the acute administration of diazoxide. Br. J. Pharmacol. 47(1), 124-132 (1973).
Cas No. | 1432063-51-8 | SDF | |
别名 | 二氮嗪D3,Sch-6783-d3; SRG-95213-d3 | ||
Canonical SMILES | ClC1=CC=C(NC(C([2H])([2H])[2H])=NS2(=O)=O)C2=C1 | ||
分子式 | C8H4ClD3N2O2S | 分子量 | 233.7 |
溶解度 | DMSO: slightly soluble | 储存条件 | Store at -20°C |
General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,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 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。 为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。 |
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Shipping Condition | 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。 |
制备储备液 | |||
1 mg | 5 mg | 10 mg | |
1 mM | 4.279 mL | 21.395 mL | 42.7899 mL |
5 mM | 0.8558 mL | 4.279 mL | 8.558 mL |
10 mM | 0.4279 mL | 2.1395 mL | 4.279 mL |
第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量) | ||||||||||
给药剂量 | mg/kg | 动物平均体重 | g | 每只动物给药体积 | ul | 动物数量 | 只 | |||
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系GLPBIO为您提供正确的澄清溶液配方) | ||||||||||
% DMSO % % Tween 80 % saline | ||||||||||
计算重置 |
计算结果:
工作液浓度: mg/ml;
DMSO母液配制方法: mg 药物溶于 μL DMSO溶液(母液浓度 mg/mL,
体内配方配制方法:取 μL DMSO母液,加入 μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入 μL saline,混匀澄清。
1. 首先保证母液是澄清的;
2.
一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
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- Purity: >99.00%
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