| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
PDE5/phosphodiesterase 5
Homo Sildenafil targets and inhibits phosphodiesterase type 5 (PDE5), the same enzyme targeted by sildenafil. By blocking PDE5, it prevents the degradation of cyclic GMP, which can lead to vasodilation. It has also been reported to have activity against PDE9 and PDE5A1. Its potency and selectivity relative to sildenafil are not consistently detailed. |
|---|---|
| ln Vitro |
Homosildenafil is a sulfonamide.
A PHOSPHODIESTERASE TYPE-5 INHIBITOR; VASODILATOR AGENT and UROLOGICAL AGENT that is used in the treatment of ERECTILE DYSFUNCTION and PRIMARY PULMONARY HYPERTENSION.
Like sildenafil, Homo Sildenafil acts as a phosphodiesterase type 5 (PDE5) inhibitor, which is a vasodilator and a urological medication used to treat erectile dysfunction. In vitro, it is identified as a sulfonamide-based PDE5 inhibitor. The specific IC50 value for PDE5 is not detailed in the product datasheet. |
| ln Vivo |
There are no specific in vivo activity data reported for Homo Sildenafil in these documents, as it is not intended for therapeutic use. Its presence as an adulterant in dietary supplements implies that it can be absorbed and produce the classic vasodilatory effects associated with PDE5 inhibition, such as increased penile blood flow.
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| Enzyme Assay |
Homo Sildenafil is not used as a test compound in a typical non-cellular enzyme assay. Instead, it is used as a reference standard. To confirm its identity, a liquid chromatography-mass spectrometry (LC-MS) protocol would be used. A solution of Homo Sildenafil is injected into the LC-MS system. Its retention time and mass spectrum (m/z of its parent ion and fragments) are compared to that of a previously characterized reference material.
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| Cell Assay |
As an analytical standard, the primary cell-based protocol is not to study its biology but to test for its presence as an unlabeled adulterant. In such a test, an extract of the supplement is prepared and mixed with a blank matrix. A known amount of Homo Sildenafil-d5 (a deuterated version) might be added as an internal standard. This mixture is then analyzed by LC-MS/MS to quantify the amount of Homo Sildenafil present.
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| Animal Protocol |
There are no standard in vivo animal protocols for Homo Sildenafil. If studied, a typical protocol for a PDE5 inhibitor would be the measurement of intracavernosal pressure (ICP) in an anesthetized rat. However, as an analytical standard, its in vivo use is not required. It is detected in animal studies when its parent product is tested as part of a safety screen.
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| ADME/Pharmacokinetics |
No specific pharmacokinetic data is provided for Homo Sildenafil. As an analog of sildenafil, it is expected to have similar properties, such as being metabolized by CYP3A4 and having an oral bioavailability of around 40%. Its use as a reference standard implies that its exact mass and fragmentation pattern are known, but its ADME profile is typically not the focus.
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| Toxicity/Toxicokinetics |
No detailed toxicological data is provided, as Homo Sildenafil is a reference standard. The safety profile of the parent molecule sildenafil is well-established. Adverse effects of PDE5 inhibitors, which may also apply to Homo Sildenafil, include headaches, flushing, dyspepsia, and, at high doses, visual disturbances due to off-target PDE6 inhibition.
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| References |
[1]. Jackie D Corbin, et al. Vardenafil: Structural Basis for Higher Potency Over Sildenafil in Inhibiting cGMP-specific phosphodiesterase-5 (PDE5). Neurochem Int. 2004 Nov;45(6):859-63.
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| Additional Infomation |
Gosildenafil is a sulfonamide drug. It is a phosphodiesterase type 5 inhibitor; a vasodilator and urological medication used to treat erectile dysfunction and primary pulmonary hypertension.
Homo Sildenafil is significant primarily in the context of regulatory and forensic science. It is one of several so-called "sildenafil analogs" that have been found as undeclared ingredients in herbal and dietary supplements marketed for sexual enhancement. The presence of these unapproved analogs poses a public health risk because of potential unknown pharmacological interactions and side effects. |
| Molecular Formula |
C23H32N6O4S
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|---|---|
| Molecular Weight |
488.60
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| Exact Mass |
488.22
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| CAS # |
642928-07-2
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| Related CAS # |
Homo Sildenafil-d5;1216711-61-3
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| PubChem CID |
135565273
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| Appearance |
White to off-white solid powder
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| Density |
1.4±0.1 g/cm3
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| Melting Point |
200-202ºC
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| Index of Refraction |
1.656
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| LogP |
2.8
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
8
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| Heavy Atom Count |
34
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| Complexity |
854
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CCOC1=CC=C(S(N2CCN(CC)CC2)(=O)=O)C=C1C1=NC(=O)C2N(N=C(CCC)C=2N1)C
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| InChi Key |
MJEXYQIZUOHDGY-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C23H32N6O4S/c1-5-8-18-20-21(27(4)26-18)23(30)25-22(24-20)17-15-16(9-10-19(17)33-7-3)34(31,32)29-13-11-28(6-2)12-14-29/h9-10,15H,5-8,11-14H2,1-4H3,(H,24,25,30)
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| Chemical Name |
5-[2-ethoxy-5-(4-ethylpiperazin-1-yl)sulfonylphenyl]-1-methyl-3-propyl-6H-pyrazolo[4,3-d]pyrimidin-7-one
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| Synonyms |
Homo Sildenafil; homosildenafil; 642928-07-2; UNII-0Z3JH0S0QK; 0Z3JH0S0QK; 5-(2-Ethoxy-5-((4-ethylpiperazin-1-yl)sulfonyl)phenyl)-1-methyl-3-propyl-1H-pyrazolo[4,3-d]pyrimidin-7(6H)-one; CHEMBL3769434; DTXSID10214510;
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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 |
| 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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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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 | 2.0467 mL | 10.2333 mL | 20.4666 mL | |
| 5 mM | 0.4093 mL | 2.0467 mL | 4.0933 mL | |
| 10 mM | 0.2047 mL | 1.0233 mL | 2.0467 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.
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