Win 58237
目录号 : GC31327Win58237是一种phosphodiesterase(PDE)抑制剂,对PDEV有很强的亲和力,Ki值为170nM,具有舒张血管的作用。
Cas No.:158001-76-4
Sample solution is provided at 25 µL, 10mM.
Win 58237 is a cyclic nucleotide phosphodiesterase (PDE) inhibitor, with Ki of 170 nM for PDE V, possessing vasorelaxant activity.
Win 58237 is a competitive inhibitor of cGMP PDE V from canine aorta, with a Ki value of 170 nM. Win 58237 is a potent inhibitor of PDE V isolated from vascular tissue with an IC50 value of 240 nM. It is a relatively less potent inhibitor of calmodulin-sensitive PDE I and cGMP-inhibitable cyclic AMP PDE III; but does inhibit cyclic AMP PDE IV with an IC50 value of approximately 300 nM. Win 58237 possesses vasorelaxant activity in the presence of an intact endothelium or nitric oxide[1].
Win 58237 (0.3-3.0 mg/kg i.v.) decreases mean arterial pressure in conscious spontaneously hypertensive rats with an associated increase in vascular (aortic) cGMP content in vivo. Win 58237 (10 mg/kg i.v.) increases plasma cGMP levels, from basal levels of 6.7 ± 1.0 to 31.4 ± 3.5 fmol/μL[1].
[1]. Silver PJ, et al. Cyclic GMP potentiation by WIN 58237, a novel cyclic nucleotide phosphodiesterase inhibitor. J Pharmacol Exp Ther. 1994 Dec;271(3):1143-9.
Cas No. | 158001-76-4 | SDF | |
Canonical SMILES | O=C1C2=C(N(C3CCCC3)N=C2C)NC(C4=CC=NC=C4)=N1 | ||
分子式 | C16H17N5O | 分子量 | 295.34 |
溶解度 | Soluble in DMSO | 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 | 3.3859 mL | 16.9296 mL | 33.8593 mL |
5 mM | 0.6772 mL | 3.3859 mL | 6.7719 mL |
10 mM | 0.3386 mL | 1.693 mL | 3.3859 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。
Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet