1. Metabolic Enzyme/Protease
  2. Phosphodiesterase (PDE)
  3. Gisadenafil besylate

Gisadenafil besylate  (Synonyms: UK 369003-26)

目录号: HY-108619 纯度: ≥99.0%
COA 产品使用指南

Gisadenafil besylate (UK 369003-26) 是一种特异性的,口服活性的磷酸二酯酶 5 (PDE5) 抑制剂,IC50 为 3.6 nM,可防止环状鸟苷单磷酸 (cGMP) 降解。

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Gisadenafil besylate Chemical Structure

Gisadenafil besylate Chemical Structure

CAS No. : 334827-98-4

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5 mg ¥3000
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10 mg ¥4200
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Customer Review

Other Forms of Gisadenafil besylate:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Gisadenafil besylate (UK 369003-26) is a specific, orally active phosphodiesterase 5 (PDE5) inhibitor with an IC50 of 3.6 nM and prevents degradation of cyclic guanosine monophosphate (cGMP)[1].

IC50 & Target[1]

PDE5A

3.6 nM (IC50)

PDE1A

9.1 μM (IC50)

体外研究
(In Vitro)

Since some PDE5 inhibitors can also interact with PDE1 isotypes found within the cerebral vasculature, the specificity of Gisadenafil for PDE5 is confirmed. This is directly tested with recombinant PDE5A and PDE1A overexpressed in COS-7 cells. The IC50 of Gisadenafil for PDE5A is 3.6 nM. In contrast, the IC50 of Gisadenafil for PDE1A is 9.1 μM, an approximately 2500-fold difference in specificity[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

Gisadenafil (2 mg/kg; intraperitoneal injection; for 2 hours; male Tat-transgenic mice) treatment largely restores the normal increase in cortical flow following hypercapnia in Tat-tg mice (17.5% above baseline). Gisadenafil also restores the dilation of small (<25 μm) arterioles following hypercapnia, although it fails to restore full dilation of larger (>25 μm) vessels[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male Tat-transgenic (Tat-tg) mice (8 weeks old) exposed to hypercapnia[1]
Dosage: 2 mg/kg
Administration: Intraperitoneal injection; for 2 hours
Result: Largely restored the normal increase in cortical flow following hypercapnia in Tat-tg mice (17.5% above baseline). Also restored the dilation of small (<25 μm) arterioles following hypercapnia.
分子量

677.79

Formula

C29H39N7O8S2

CAS 号
性状

固体

颜色

White to off-white

中文名称

吉沙那非苯磺酸盐

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据
细胞实验: 

DMSO 中的溶解度 : 100 mg/mL (147.54 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

H2O 中的溶解度 : 3.33 mg/mL (4.91 mM; 超声助溶 (<60°C))

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.4754 mL 7.3769 mL 14.7538 mL
5 mM 0.2951 mL 1.4754 mL 2.9508 mL
查看完整储备液配制表

* 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, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-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。

* 备注:如您选择水作为储备液,请稀释至工作液后,再用 0.22 μm 的滤膜过滤除菌后使用。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料

纯度: ≥99.0%

参考文献

完整储备液配制表

* 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, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-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。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
H2O / DMSO 1 mM 1.4754 mL 7.3769 mL 14.7538 mL 36.8846 mL
DMSO 5 mM 0.2951 mL 1.4754 mL 2.9508 mL 7.3769 mL
10 mM 0.1475 mL 0.7377 mL 1.4754 mL 3.6885 mL
15 mM 0.0984 mL 0.4918 mL 0.9836 mL 2.4590 mL
20 mM 0.0738 mL 0.3688 mL 0.7377 mL 1.8442 mL
25 mM 0.0590 mL 0.2951 mL 0.5902 mL 1.4754 mL
30 mM 0.0492 mL 0.2459 mL 0.4918 mL 1.2295 mL
40 mM 0.0369 mL 0.1844 mL 0.3688 mL 0.9221 mL
50 mM 0.0295 mL 0.1475 mL 0.2951 mL 0.7377 mL
60 mM 0.0246 mL 0.1229 mL 0.2459 mL 0.6147 mL
80 mM 0.0184 mL 0.0922 mL 0.1844 mL 0.4611 mL
100 mM 0.0148 mL 0.0738 mL 0.1475 mL 0.3688 mL

* 备注:如您选择水作为储备液,请稀释至工作液后,再用 0.22 μm 的滤膜过滤除菌后使用。

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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产品名称:
Gisadenafil besylate
目录号:
HY-108619
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