Size | Price | Stock | Qty |
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1mg |
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5mg |
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10mg |
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Other Sizes |
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Targets |
PDE5A 3.6 nM (IC50) PDE1A 9.1 μM (IC50)
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ln Vitro |
Gisadenafil is confirmed to be selective for PDE5, as some PDE5 inhibitors can also interact with PDE1 isotypes present in the cerebral vasculature. Recombinant PDE5A and PDE1A overexpressed in COS-7 cells are used to directly evaluate this. Gisadenafil's half-life for PDE5A is 3.6 nM. On the other hand, the specificity of Gisadenafil for PDE1A differs by almost 2500-fold, with an IC50 of 9.1 μM[1].
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ln Vivo |
Male Tat-transgenic mice are given an intraperitoneal injection of sisadenafil (2 mg/kg) for two hours. This treatment essentially recovers the usual rise in cortical flow that occurs in these mice after hypercapnia (17.5% above baseline). After hypercapnia, sildenafil also helps to dilate small (less than 25 μm) arterioles, but it is unable to fully dilate larger (more than 25 μm) vessels[1].
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Animal Protocol |
Animal/Disease Models: Male Tat-transgenic (Tat-tg) mice (8 weeks old) exposed to hypercapnia[1]
Doses: 2 mg/kg Route of Administration: intraperitoneal (ip) injection; for 2 hrs (hours) Experimental Results: 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. |
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.
[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. |
Molecular Formula |
C29H39N7O8S2
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Molecular Weight |
677.79
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CAS # |
334827-98-4
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Related CAS # |
Gisadenafil;334826-98-1
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Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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SMILES |
CCC1=C2C(=NN1CCOC)C(=O)N=C(C3=C(N=CC(=C3)S(=O)(=O)N4CCN(CC)CC4)OCC)N2.C1=CC=C(C=C1)S(=O)(=O)O
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
DMSO: 100 mg/mL (147.54 mM)
H2O: 3.33 mg/mL (4.91 mM) |
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Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 :Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400  (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.