Gisadenafil besylate
Based on 1 Customer Validation
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.
- Purity: 99.74%
- CAS No.: 334827-98-4
- Formula: C29H39N7O8S2
- Molecular Weight:677.79
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
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PDE5A 3.6 nM (IC50) |
PDE1A 9.1 μM (IC50) |
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male Tat-transgenic (Tat-tg) mice (8 weeks old) exposed to hypercapnia[1]
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Dosage:2 mg/kg
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Administration:Intraperitoneal injection; for 2 hours
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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.
Chemical Information
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CAS No. 334827-98-4
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Appearance Solid
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Molecular Weight 677.79
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Formula C29H39N7O8S2
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Color White to off-white
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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
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Synonyms
UK 369003-26
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Shipping
Room temperature in continental US; may vary elsewhere.
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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
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (276 KB)
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SDS (419 KB)
- English - EN (419 KB)
- Français - FR (419 KB)
- Deutsch - DE (419 KB)
- Norwegian - NO (419 KB)
- Español - ES (419 KB)
- Swedish - SV (419 KB)
- Italian - IT (419 KB)
- Korean - KR (419 KB)
- Portuguese - PT (419 KB)
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Handling Instructions (2659 KB)
References
[1]. Silva J, et al. Transient hypercapnia reveals an underlying cerebrovascular pathology in a murine model for HIV-1 associated neuroinflammation: role of NO-cGMP signaling and normalization by inhibition of cyclic nucleotide phosphodiesterase-5. J Neuroinflammation. 2012 Nov 20;9:253. [Content Brief]
[2]. Rawson DJ, et al. The discovery of UK-369003, a novel PDE5 inhibitor with the potential for oral bioavailability and dose-proportional pharmacokinetics. Bioorg Med Chem. 2012 Jan 1;20(1):498-509. [Content Brief]
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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