| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
5-lipoxygenase-activating protein (FLAP). (S)-Veliflapon is a FLAP inhibitor, which blocks the translocation of 5-lipoxygenase to the nuclear membrane, thereby inhibiting the synthesis of leukotrienes (including LTB4 and cysteinyl leukotrienes) from arachidonic acid.
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| ln Vitro |
In human whole blood, (S)-veliflapon dose-dependently decreases the synthesis of leukotriene B4 (LTB4) [1].
In vitro, (S)-Veliflapon inhibits leukotriene B4 (LTB4) formation in rat, mouse, and human leukocytes with IC50 values of 0.026 uM, 0.039 uM, and 0.22 uM, respectively. In human whole blood, (S)-Veliflapon dose-dependently decreases the synthesis of LTB4, demonstrating its effectiveness in a complex biological matrix. It exhibits enantioselectivity in human whole blood. |
| ln Vivo |
No published in vivo data. As an orally bioactive FLAP inhibitor, (S)-Veliflapon would be expected to reduce leukotriene levels in vivo and attenuate inflammation in animal models of asthma, arthritis, or cardiovascular disease, though this remains to be validated for this specific enantiomer.
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| Enzyme Assay |
Binding affinity to FLAP is typically assessed using a radioligand binding assay. Membrane preparations from cells expressing human FLAP are incubated with a radiolabeled FLAP ligand in the presence of serially diluted (S)-Veliflapon (0.1-1000 nM). Bound radioactivity is measured by filtration and scintillation counting to calculate the half-maximal inhibitory concentration (IC50).
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| Cell Assay |
Leukocytes isolated from rat, mouse, or human blood are stimulated with calcium ionophore A23187 (5 uM) in the presence of serially diluted (S)-Veliflapon (0.001-10 uM) for 10 minutes at 37degC. The reaction is terminated by centrifugation, and LTB4 levels in the supernatant are quantified by ELISA or LC-MS/MS. The half-maximal inhibitory concentration (IC50) is calculated.
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| Animal Protocol |
C57BL/6 mice are challenged with LPS to induce systemic inflammation. (S)-Veliflapon is administered orally at doses of 3-30 mg/kg, 1 hour before LPS challenge. Blood is collected 2-4 hours post-LPS, and serum LTB4 levels are measured by ELISA. Lung or peritoneal lavage fluid is collected for cell differential counts and cytokine analysis.
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| ADME/Pharmacokinetics |
(S)-Veliflapon is orally bioactive, with molecular weight 361.43 g/mol and formula C23H23NO3. LogP is 5.4, indicating high lipophilicity. DMSO solubility is 100 mg/mL. Detailed PK parameters are not fully published, but as a lipophilic small molecule, it is expected to have high plasma protein binding and moderate oral bioavailability.
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| Toxicity/Toxicokinetics |
Detailed toxicological profiles are not publicly available. As a FLAP inhibitor, potential adverse effects may include gastrointestinal disturbances, headache, or liver enzyme elevations, consistent with other leukotriene synthesis inhibitors. No severe toxicities have been reported at efficacious doses in research models.
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| References |
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| Additional Infomation |
(S)-Veliflapon is a research chemical not approved for clinical use. It is referenced in publications on in vitro pharmacology of BAY X1005 (Agents Actions. 1993 Mar;38(3-4):188-95) and in patents for leukotriene synthesis inhibitors. It is used to study the role of FLAP and leukotrienes in inflammatory and cardiovascular diseases.
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| Molecular Formula |
C23H23NO3
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|---|---|
| Molecular Weight |
361.43
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| Exact Mass |
361.167
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| CAS # |
128253-32-7
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| Related CAS # |
Veliflapon;128253-31-6
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| PubChem CID |
22860799
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| Appearance |
White to off-white solid powder
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| LogP |
5.4
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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 |
6
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| Heavy Atom Count |
27
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| Complexity |
482
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| Defined Atom Stereocenter Count |
1
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| SMILES |
[C@H](C1CCCC1)(C1C=CC(=CC=1)OCC1C=CC2C=CC=CC=2N=1)C(=O)O
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| InChi Key |
ZEYYDOLCHFETHQ-QFIPXVFZSA-N
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| InChi Code |
InChI=1S/C23H23NO3/c25-23(26)22(17-6-1-2-7-17)18-10-13-20(14-11-18)27-15-19-12-9-16-5-3-4-8-21(16)24-19/h3-5,8-14,17,22H,1-2,6-7,15H2,(H,25,26)/t22-/m0/s1
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| Chemical Name |
(2S)-2-cyclopentyl-2-[4-(quinolin-2-ylmethoxy)phenyl]acetic acid
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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 (276.68 mM)
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|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.7668 mL | 13.8339 mL | 27.6679 mL | |
| 5 mM | 0.5534 mL | 2.7668 mL | 5.5336 mL | |
| 10 mM | 0.2767 mL | 1.3834 mL | 2.7668 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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