| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| Other Sizes |
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Purity: ≥98%
Diflapolin is reported to be the first potent dual soluble epoxide hydrolase (sEH)/5-lipoxygenase-activating protein (FLAP) inhibitor with anti-inflammatory effects. Whereas 5-LOX (5-lipoxygenase) activating protein facilitates 5-LOX-mediated conversion of arachidonic acid to pro-inflammatory leukotrienes, soluble epoxide hydrolase (sEH) degrades anti-inflammatory epoxyeicosatrienoic acids (EETs). Dual inhibition might therefore offer increased efficacy as an anti-inflammatory intervention compared to single target agents. Accordingly, dual FLAP/sEH inhibition might be advantageous drugs for intervention of inflammation.
| ln Vivo |
In vivo investigations have shown that diflapolin (1–10 mg/kg; intraperitoneally; 30 minutes before zymosan administration) displays strong anti-inflammatory effects [1].
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|---|---|
| Animal Protocol |
Animal/Disease Models: Male CD-1 mouse (Zymosan-induced peritonitis mouse model) [1]
Doses: 1, 3 and 10 mg/kg Route of Administration: intraperitoneal (ip) injection; 30 minutes before injection of zymosan Experimental Results: from 1 mg/kg dose initiated a significant reduction in peritoneal levels of LTC4 and LTB4, which was comparable to the effect of MK886. |
| References |
| Molecular Formula |
C22H17CL2N3O2S
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|---|---|
| Molecular Weight |
458.360281705856
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| Exact Mass |
457.041
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| Elemental Analysis |
C, 57.65; H, 3.74; Cl, 15.47; N, 9.17; O, 6.98; S, 6.99
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| CAS # |
724453-98-9
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| PubChem CID |
4560409
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| Appearance |
White to off-white solid powder
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| Density |
1.5±0.1 g/cm3
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| Boiling Point |
543.0±50.0 °C at 760 mmHg
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| Flash Point |
282.2±30.1 °C
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| Vapour Pressure |
0.0±1.5 mmHg at 25°C
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| Index of Refraction |
1.736
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| LogP |
7.05
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
30
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| Complexity |
587
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| Defined Atom Stereocenter Count |
0
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| SMILES |
ClC1=C(C=CC(=C1)NC(NC1C=CC(=CC=1C)OCC1=NC2C=CC=CC=2S1)=O)Cl
|
| InChi Key |
FGXLEECGXSDIMM-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C22H17Cl2N3O2S/c1-13-10-15(29-12-21-26-19-4-2-3-5-20(19)30-21)7-9-18(13)27-22(28)25-14-6-8-16(23)17(24)11-14/h2-11H,12H2,1H3,(H2,25,27,28)
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| Chemical Name |
1-(4-(benzo[d]thiazol-2-ylmethoxy)-2-methylphenyl)-3-(3,4-dichlorophenyl)urea
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| Synonyms |
Diflapolin
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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 : ~83.33 mg/mL (~181.80 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 2.08 mg/mL (4.54 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 20.8 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: ≥ 2.08 mg/mL (4.54 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 20.8 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 | 2.1817 mL | 10.9085 mL | 21.8169 mL | |
| 5 mM | 0.4363 mL | 2.1817 mL | 4.3634 mL | |
| 10 mM | 0.2182 mL | 1.0908 mL | 2.1817 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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