| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 5mg |
|
||
| 10mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| 250mg | |||
| Other Sizes |
Purity: ≥98%
| Targets |
Difamilast targets phosphodiesterase 4 (PDE4), an enzyme that hydrolyzes cyclic adenosine monophosphate (cAMP). By inhibiting PDE4, it increases intracellular cAMP levels, leading to the suppression of pro-inflammatory cytokine production and the reduction of inflammation.
|
|---|---|
| ln Vitro |
PDE4 B isoform (IC50=11.2 nM) is highly selectively inhibited by OPA-15406, while PDE2 is likewise inhibited by OPA-15406 [2].
In vitro, difamilast is a potent and selective inhibitor of PDE4. It inhibits PDE4 activity with high potency. Its selectivity for PDE4 over other PDE isoforms has been characterized. |
| ln Vivo |
In animal models of AD, OPA-1540 ameliorates skin problems [1].
In vivo, difamilast is a topical anti-inflammatory agent. It has been shown to reduce inflammation and improve skin lesions in animal models of atopic dermatitis. It is being developed as a treatment for inflammatory skin conditions. |
| Enzyme Assay |
In vitro enzyme assays for difamilast typically measure its ability to inhibit PDE4 activity. The enzyme is incubated with its substrate (cAMP) in the presence of increasing concentrations of the compound. The hydrolysis of cAMP is measured. IC₅₀ values are calculated.
|
| Cell Assay |
Cell-based assays for difamilast involve treating immune cells with the compound and measuring cytokine production and cAMP levels. The compound's ability to suppress pro-inflammatory cytokine production is assessed.
|
| Animal Protocol |
In vivo animal studies for difamilast typically involve topical administration to animal models of atopic dermatitis. The compound's ability to reduce inflammation, skin lesions, and pruritus is assessed.
|
| ADME/Pharmacokinetics |
Pharmacokinetic properties of difamilast have been characterized in preclinical and clinical studies. The compound is administered topically and has low systemic absorption.
|
| Toxicity/Toxicokinetics |
Difamilast is generally well-tolerated. Common side effects include local skin irritation. It has a favorable safety profile.
|
| References |
|
| Additional Infomation |
Difamilast is being investigated in the clinical trial NCT01702181 (a safety study evaluating the use and efficacy of a topical ointment for the treatment of atopic dermatitis in adults).
Difamilast is a PDE4 inhibitor being developed for the treatment of atopic dermatitis. It is not currently approved for clinical use. It is a valuable research tool for studying PDE4 and inflammation. |
| Molecular Formula |
C23H24F2N2O5
|
|---|---|
| Molecular Weight |
446.4439
|
| Exact Mass |
446.165
|
| CAS # |
937782-05-3
|
| PubChem CID |
57855696
|
| Appearance |
White to off-white solid powder
|
| Density |
1.2±0.1 g/cm3
|
| Index of Refraction |
1.534
|
| LogP |
4.73
|
| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
8
|
| Rotatable Bond Count |
10
|
| Heavy Atom Count |
32
|
| Complexity |
583
|
| Defined Atom Stereocenter Count |
0
|
| InChi Key |
VFBILHPIHUPBPZ-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C23H24F2N2O5/c1-4-29-18-8-6-5-7-17(18)21(28)26-12-16-13-30-22(27-16)15-9-10-19(32-23(24)25)20(11-15)31-14(2)3/h5-11,13-14,23H,4,12H2,1-3H3,(H,26,28)
|
| Chemical Name |
N-[[2-[4-(difluoromethoxy)-3-propan-2-yloxyphenyl]-1,3-oxazol-4-yl]methyl]-2-ethoxybenzamide
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~223.99 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (5.60 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
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 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.60 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 | 2.2399 mL | 11.1997 mL | 22.3994 mL | |
| 5 mM | 0.4480 mL | 2.2399 mL | 4.4799 mL | |
| 10 mM | 0.2240 mL | 1.1200 mL | 2.2399 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
COA