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

Gisadenafil besylate  (Synonyms: UK 369003-26)

目錄號(hào): HY-108619 純度: ≥99.0%
COA 產(chǎn)品使用指南

Gisadenafil besylate (UK 369003-26) 是一種特異性的,口服活性的磷酸二酯酶 5 (PDE5) 抑制劑,IC50 為 3.6 nM,可防止環(huán)狀鳥苷單磷酸 (cGMP) 降解。

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Gisadenafil besylate Chemical Structure

Gisadenafil besylate Chemical Structure

CAS No. : 334827-98-4

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1 mg ¥1400
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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:

查看 Phosphodiesterase (PDE) 亞型特異性產(chǎn)品:

  • 生物活性

  • 純度 & 產(chǎn)品資料

  • 參考文獻(xiàn)

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)

體外研究
(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.

體內(nèi)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 號(hào)
性狀

固體

顏色

White to off-white

中文名稱

吉沙那非苯磺酸鹽

運(yùn)輸條件

Room temperature in continental US; may vary elsewhere.

儲(chǔ)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)

溶解性數(shù)據(jù)
細(xì)胞實(shí)驗(yàn): 

DMSO 中的溶解度 : 100 mg/mL (147.54 mM; 超聲助溶; 吸濕的 DMSO 對(duì)產(chǎn)品的溶解度有顯著影響,請(qǐng)使用新開封的 DMSO)

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

配制儲(chǔ)備液
濃度 溶劑體積 質(zhì)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
查看完整儲(chǔ)備液配制表

* 請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液;一旦配成溶液,請(qǐng)分裝保存,避免反復(fù)凍融造成的產(chǎn)品失效。
儲(chǔ)備液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C儲(chǔ)存時(shí),請(qǐng)?jiān)?個(gè)月內(nèi)使用,-20°C儲(chǔ)存時(shí),請(qǐng)?jiān)?個(gè)月內(nèi)使用。

* 備注:如您選擇水作為儲(chǔ)備液,請(qǐng)稀釋至工作液后,再用 0.22 μm 的濾膜過濾除菌后使用。

  • 摩爾計(jì)算器

  • 稀釋計(jì)算器

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

質(zhì)量
=
濃度
×
體積
×
分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

濃度 (start)

C1

×
體積 (start)

V1

=
濃度 (final)

C2

×
體積 (final)

V2

動(dòng)物溶解方案計(jì)算器
請(qǐng)輸入動(dòng)物實(shí)驗(yàn)的基本信息:

給藥劑量

mg/kg

動(dòng)物的平均體重

g

每只動(dòng)物的給藥體積

μL

動(dòng)物數(shù)量

由于實(shí)驗(yàn)過程有損耗,建議您多配一只動(dòng)物的量
計(jì)算結(jié)果
工作液所需濃度 : mg/mL
純度 & 產(chǎn)品資料

純度: ≥99.0%

參考文獻(xiàn)

完整儲(chǔ)備液配制表

* 請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液;一旦配成溶液,請(qǐng)分裝保存,避免反復(fù)凍融造成的產(chǎn)品失效。
儲(chǔ)備液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C儲(chǔ)存時(shí),請(qǐng)?jiān)?個(gè)月內(nèi)使用,-20°C儲(chǔ)存時(shí),請(qǐng)?jiān)?個(gè)月內(nèi)使用。

可選溶劑 濃度 溶劑體積 質(zhì)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

* 備注:如您選擇水作為儲(chǔ)備液,請(qǐng)稀釋至工作液后,再用 0.22 μm 的濾膜過濾除菌后使用。

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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產(chǎn)品名稱:
Gisadenafil besylate
目錄號(hào):
HY-108619
需求量: