BAY 41-2272
目录号 : GC10192
An activator of soluble guanylate cyclase
Cas No.:256376-24-6
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
BAY 41-2272 is an activator of nitric oxide-sensitive guanylyl cyclase (NO-sensitive GC) with EC50 values of 0.3 μmol/L and 3 μmol/L in the presence and absence of 100 nmol/L DEA-NO, respectively [1].
NO-sensitive GC catalyzes the cGMP formation. It is generally considered as the most important receptor of the signaling molecule NO. The NO/cGMP pathway plays a role in many physiological processes such as the inhibition of platelet aggregation and the relaxation of smooth muscle [1].
In platelets, GSNO at 3 μmol/L (a submaximally effective concentration) was used to assess a possible sensitizing effect of BAY 41-2272 on NO-sensitive GC. The cGMP response resulted from the application of NO at this concentration in the absence of BAY 41-2272 was only marginal. In the presence of BAY 41-2272 at 100 μmol/L, treatment with GSNO at 3 μmol/L resulted in a rapid increase in cGMP up to 1000 pmol/109 platelets [1].
The sGC/NO system was implicated in the pathogenesis of erectile dysfunction. Intravenous treatment with BAY 41-2272 at 1 mg/kg induced only a very weak erection in rabbits, with a maximal length of exposed mucosa of about 3mm at 10 min, and the effect lasted for approximate 30 minutes. SNP is a NO donor. Simultaneous administration of SNP potentiated the effect of BAY 41-2272. Intravenous treatment with SNP at 0.2 mg/kg resulted in a short-lasting erection of about 5~10 minutes, and a peak length of uncovered penile mucosa of 5 mm. Administration with BAY 41-2272 at 1 mg/kg IV followed by SNP at 0.2 mg/kg IV 5 minutes later, resulted in lengths of ensuing erection with a mean of 15 mm, longer than lengths resulted from treatments with two compounds separately [2].
References:
[1]. Mullershausen F, Russwurm M, Friebe A, et al. Inhibition of phosphodiesterase type 5 by the activator of nitric oxide-sensitive guanylyl cyclase BAY 41-2272. Circulation, 2004, 109(14): 1711-1713.
[2]. Bischoff E, Schramm M, Straub A, et al. BAY 41-2272: a stimulator of soluble guanylyl cyclase induces nitric oxide-dependent penile erection in vivo. Urology, 2003, 61(2): 464-467.
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.7748 mL | 13.8739 mL | 27.7477 mL |
| 5 mM | 0.555 mL | 2.7748 mL | 5.5495 mL |
| 10 mM | 0.2775 mL | 1.3874 mL | 2.7748 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。
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