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

Gisadenafil besylate  (Synonyms: UK 369003-26)

Cat. No.: HY-108619 Purity: ≥99.0%
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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).

For research use only. We do not sell to patients.

Gisadenafil besylate Chemical Structure

Gisadenafil besylate Chemical Structure

CAS No. : 334827-98-4

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5 mg USD 300 In-stock
10 mg USD 420 In-stock
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Based on 1 publication(s) in Google Scholar

Other Forms of Gisadenafil besylate:

Gisadenafil besylate Related Antibodies

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PDE1 PDE2 PDE3 PDE4 PDE5 PDE6 PDE7 PDE9 PDE10 PDE11 PDE12 PDE8 Autotaxin

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Description

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)

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].

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

Gisadenafil besylate Related Antibodies
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].

MedChemExpress (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.
Molecular Weight

677.79

Formula

C29H39N7O8S2
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C1C2=NN(CCOC)C(CC)=C2N=C(C3=CC(S(=O)(N4CCN(CC)CC4)=O)=CN=C3OCC)N1.O=S(C5=CC=CC=C5)(O)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

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

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (147.54 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : 3.33 mg/mL (4.91 mM; ultrasonic and warming and heat to 60°C)

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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

Mass
=
Concentration
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Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation

Purity: ≥99.0%

COA (253 KB) Elemental Analysis Report (111 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 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

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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Gisadenafil besylate Related Classifications

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.

Keywords:

Gisadenafil besylate334827-98-4UK 369003-26Phosphodiesterase (PDE)Inhibitorinhibitorinhibit

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