| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 10mg |
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| 100mg | |||
| 250mg | |||
| Other Sizes |
| Targets |
Phosphodiesterase 5 (PDE5).
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|---|---|
| ln Vitro |
FR-229934 is a PDE5 inhibitor. By inhibiting PDE5, it prevents the breakdown of cyclic GMP, leading to sustained vasodilation and increased blood flow. The compound has been studied for its potential in pulmonary arterial hypertension and erectile dysfunction.
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| ln Vivo |
In vivo, FR-229934 has been applied in models of asthma, arthritis, and dermatologic inflammation to evaluate BLT1-mediated signaling. It has been studied for pulmonary hypertension and erectile dysfunction. PDE5 inhibitors like FR-229934 are known to be effective in these conditions.
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| Enzyme Assay |
PDE5 inhibition is assessed using in vitro enzyme assays. Recombinant PDE5 is incubated with a substrate (e.g., cyclic GMP) in the presence of varying concentrations of FR-229934. The hydrolysis of the substrate is measured, and IC50 values are calculated. Selectivity is assessed against other PDE isoforms.
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| Cell Assay |
Cellular activity is evaluated in cells expressing PDE5, such as vascular smooth muscle cells. Cells are treated with FR-229934, and the levels of cyclic GMP are measured. The compound's ability to increase cyclic GMP levels and induce vasodilation is assessed.
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| Animal Protocol |
In vivo efficacy is studied in animal models of pulmonary arterial hypertension and erectile dysfunction. FR-229934 is administered orally or intravenously. Hemodynamic parameters, such as pulmonary artery pressure, are measured. In models of erectile dysfunction, the compound's effect on erectile function is assessed.
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| ADME/Pharmacokinetics |
FR-229934 has a molecular formula of C21H23Cl2N3O4S and a molecular weight of 484.40 g/mol. It is a small molecule PDE5 inhibitor. The compound is typically supplied as a powder.
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| Toxicity/Toxicokinetics |
Specific toxicological data for FR-229934 are not extensively published. As a PDE5 inhibitor, it may have vasodilatory effects and cause side effects such as headache, flushing, and hypotension. The compound is for research use only.
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| Additional Infomation |
FR-229934 is a research tool compound for studying PDE5 function. It is not approved for clinical use. The compound has been investigated for pulmonary arterial hypertension and erectile dysfunction. It is also applied in models of asthma, arthritis, and dermatologic inflammation to evaluate BLT1-mediated signaling.
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| Molecular Formula |
C21H23CL2N3O3S
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|---|---|
| Molecular Weight |
468.4
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| Exact Mass |
467.084
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| CAS # |
799841-02-4
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| PubChem CID |
11259905
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| Appearance |
White to yellow solid powder
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| LogP |
6.605
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
8
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| Heavy Atom Count |
30
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| Complexity |
688
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| Defined Atom Stereocenter Count |
0
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| SMILES |
ClC1=C(C=CC(=C1)CN1C(C)=NC2C=CC(C(NS(CCCCC)(=O)=O)=O)=CC1=2)Cl
|
| InChi Key |
QLXVZAXTUBLQJW-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C21H23Cl2N3O3S/c1-3-4-5-10-30(28,29)25-21(27)16-7-9-19-20(12-16)26(14(2)24-19)13-15-6-8-17(22)18(23)11-15/h6-9,11-12H,3-5,10,13H2,1-2H3,(H,25,27)
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| Chemical Name |
3-[(3,4-dichlorophenyl)methyl]-2-methyl-N-pentylsulfonylbenzimidazole-5-carboxamide
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| Synonyms |
FR 229934; FR229934; FR-229934
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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) |
DMSO : ~100 mg/mL (~213.49 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.34 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.34 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1349 mL | 10.6746 mL | 21.3493 mL | |
| 5 mM | 0.4270 mL | 2.1349 mL | 4.2699 mL | |
| 10 mM | 0.2135 mL | 1.0675 mL | 2.1349 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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