research use only
Cat.No.S4683
| Molecular Weight | 474.58(free base) | Formula | C22H30N6O4S.xCH4O3S |
Storage (From the date of receipt) | |
|---|---|---|---|---|---|
| CAS No. | 1308285-21-3 | Download SDF | Storage of Stock Solutions |
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| Synonyms | UK-92480 Mesylate | Smiles | CCCC1=NN(C2=C1N=C(NC2=O)C3=C(C=CC(=C3)S(=O)(=O)N4CCN(CC4)C)OCC)C.CS(=O)(=O)O | ||
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In vitro |
DMSO
: 100 mg/mL
Water : 100 mg/mL Ethanol : 4 mg/mL |
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In vivo |
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Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
| Targets/IC50/Ki |
PDE5
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| In vivo |
Chronic sildenafil treatment increases the detumescence phase in young and aged rats (p<0.05), although aged rats show a greater increase than young rats. Baseline cavernous PDE5 expression and activity are greater in aged vs young rats (p<0.05). After chronic sildenafil treatment cavernous PDE5 expression is increased in young (p<0.05) but not in aged rats. Chronic and acute sildenafil treatment similarly inhibits PDE5 activity in the penis of young and aged rats (p<0.05), coincident with its free plasma concentrations equivalent to clinically therapeutic ranges. |
References |
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