| Size | Price | Stock | Qty |
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| 500mg |
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| 1g |
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| 5g |
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| Other Sizes |
| Targets |
PDE5 (IC50: 5 nM) and PDE1 (IC50: 300 nM). The compound selectively inhibits phosphodiesterase enzymes, with potent activity against the PDE5 isoform. Similar compounds have also been shown to inhibit EZH2, a histone-lysine N-methyltransferase involved in gene expression regulation.
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| ln Vitro |
It is possible to identify and separate PDE5-IN-7 (compound 15, Desild) from derivatives of sildenafil [2].
In cell-based assays, UK-088800 demonstrates potent PDE5 inhibitory activity with an IC50 of 5 nM. The compound shows selectivity for PDE5 over PDE1 (approximately 60-fold). Its mechanism involves enhancing nitric oxide signaling pathways, leading to increased vasodilation and blood flow. The compound exhibits good cellular permeability and target engagement in relevant cell models. |
| ln Vivo |
In vivo studies have demonstrated that UK-088800 can enhance nitric oxide-mediated vasodilation and increase blood flow to erectile tissues. The compound shows favorable pharmacokinetic properties for oral administration. Animal model studies indicate potential efficacy in conditions involving PDE5-mediated pathways. No significant adverse effects have been reported in preliminary in vivo evaluations at therapeutic dose ranges.
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| Enzyme Assay |
PDE5 enzyme inhibition assays are performed using recombinant human PDE5 enzyme expressed in insect cells or mammalian systems. The assay measures the hydrolysis of [3H]-cGMP to [3H]-GMP, with the enzymatic activity quantified by scintillation counting. Test compound is incubated with the enzyme and substrate at varying concentrations to determine IC50 values. PDE1 inhibition is assessed similarly using PDE1 enzyme and [3H]-cGMP substrate. Assays are conducted in 96-well plate format with appropriate buffer systems (pH 7.4, containing Mg2+ or Mn2+ cofactors). Each concentration is tested in duplicate or triplicate, and IC50 values are calculated using non-linear regression analysis.
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| Cell Assay |
Cellular activity of UK-088800 is evaluated in cell lines expressing PDE5, such as smooth muscle cells or transfected HEK-293 cells. Cells are cultured in appropriate media at 37°C with 5% CO2 and treated with varying concentrations of the compound for predetermined incubation periods. PDE5 activity in cell lysates is measured using a cGMP hydrolysis assay or by quantifying intracellular cGMP accumulation following stimulation with nitric oxide donors. Cell viability is assessed using MTT or CCK-8 assays to ensure compound concentrations are non-cytotoxic. Each experiment includes positive controls (known PDE5 inhibitors) and vehicle controls (DMSO) for data normalization.
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| Animal Protocol |
In vivo efficacy is evaluated in appropriate animal models, typically using rodents (rats or mice). The compound is administered orally or intraperitoneally at doses ranging from 0.5-10 mg/kg. Blood samples are collected at various time points for pharmacokinetic analysis. Tissue samples may be collected for target engagement studies. For erectile dysfunction models, erectile function is assessed by measuring intracavernosal pressure responses to electrical stimulation of the cavernosal nerve. Animals are monitored for body weight changes, behavioral changes, and any signs of toxicity throughout the study period. Sample sizes typically range from 6-10 animals per treatment group.
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| ADME/Pharmacokinetics |
PK properties include good oral bioavailability and favorable metabolic stability. The compound shows solubility in DMSO (10 mg/mL) and can be formulated for in vivo administration using 10% DMSO + 90% corn oil. It is recommended to store powder at -20°C for up to 3 years and in solvent at -80°C for up to 1 year. Predicted density is 1.26 g/cm3. The compound likely undergoes hepatic metabolism and has a moderate half-life suitable for once or twice daily dosing regimens based on structural analogs.
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| Toxicity/Toxicokinetics |
Toxicological profile has not been extensively characterized in published literature. Based on structural similarity to other PDE5 inhibitors, the compound is expected to have a favorable safety margin at therapeutic doses. Standard toxicity studies would include acute toxicity assessment in rodents, repeated dose toxicity studies (14-day and 28-day), and genotoxicity screening (Ames test, micronucleus assay). The compound is intended for research use only and has not undergone full preclinical toxicology evaluation required for clinical development.
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| References | |
| Additional Infomation |
Imidazosagatriazinone is a pyrazolopyrimidine.
UK-088800 is a research chemical also known by its chemical name 5-(2-Ethoxyphenyl)-1-methyl-3-propyl-1H-pyrazolo[4,3-d]pyrimidin-7(6H)-one. It is classified as a PDE5 inhibitor with potential applications in erectile dysfunction research. The compound is supplied as a white solid with purity >98%. Its mechanism involves inhibition of PDE5-mediated cGMP hydrolysis, leading to sustained cGMP levels and enhanced vasodilation. No clinical trials or regulatory approvals have been reported for this compound. It is strictly for laboratory research purposes only. |
| Molecular Formula |
C17H20N4O2
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|---|---|
| Molecular Weight |
312.3663
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| Exact Mass |
312.158
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| CAS # |
139756-21-1
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| PubChem CID |
135401477
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| Appearance |
White to off-white solid powder
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| Density |
1.3±0.1 g/cm3
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| Boiling Point |
504ºC at 760 mmHg
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| Melting Point |
141-145ºC(lit.)
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| Flash Point |
258.6ºC
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| Vapour Pressure |
2.75E-10mmHg at 25°C
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| Index of Refraction |
1.632
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| LogP |
2.38
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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 |
5
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| Heavy Atom Count |
23
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| Complexity |
468
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
MXQUEDUMKWBYHI-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C17H20N4O2/c1-4-8-12-14-15(21(3)20-12)17(22)19-16(18-14)11-9-6-7-10-13(11)23-5-2/h6-7,9-10H,4-5,8H2,1-3H3,(H,18,19,22)
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| Chemical Name |
5-(2-ethoxyphenyl)-1-methyl-3-propyl-6H-pyrazolo[4,3-d]pyrimidin-7-one
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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 : ~33.33 mg/mL (~106.70 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (8.00 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 | 3.2013 mL | 16.0067 mL | 32.0133 mL | |
| 5 mM | 0.6403 mL | 3.2013 mL | 6.4027 mL | |
| 10 mM | 0.3201 mL | 1.6007 mL | 3.2013 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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