Gisadenafil besylate UK 369003-26|cas:334827-98-4|西域试剂

Gisadenafil besylate UK 369003-26,99.0%

产品编号：Bellancom-108619| CAS NO：334827-98-4| 分子式：C₂₉H₃₉N₇O₈S₂| 分子量：677.79

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货号	价格	库存与货期
Bellancom-108619	￥1400.00	杭州北京（现货）
Bellancom-108619	￥3000.00	杭州北京（现货）
Bellancom-108619	￥4200.00	杭州北京（现货）

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Gisadenafil besylate UK 369003-26

产品介绍

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。

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).

体外研究

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.

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

体内研究

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.

西域 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
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.

体内研究

西域 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
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.

性状

Solid

溶解性数据

In Vitro:

DMSO : 100 mg/mL (147.54 mM; Need ultrasonic)

H₂O : 3.33 mg/mL (4.91 mM; ultrasonic and warming and heat to 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
10 mM	0.1475 mL	0.7377 mL	1.4754 mL

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。

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)

参考文献