Veliflapon
Based on 1 Customer Validation
Veliflapon (BAY X 1005; DG-031) is an orally active and selective 5-lipoxygenase activating protein (FLAP) inhibitor. Veliflapon inhibits the synthesis of the leukotrienes B4 and C4.
For research use only. We do not sell to patients.
- Purity: 99.31%
- CAS No.: 128253-31-6
- Formula: C23H23NO3
- Molecular Weight:361.43
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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All Leukotriene Receptor Isoforms
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Biological Activity
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LTB4 |
LTC4 |
Veliflapon (BAY X 1005; DG-031) effectively inhibits the synthesis of LTB4 in A23187-stimulated leukocytes from rats, mice and humans (IC50s of 0.026, 0.039 and 0.22 μM, respectively) as well as the formation of LTC4 (IC50 of 0.021 μM) in mouse peritoneal macrophages stimulated with opsonized zymosan[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Veliflapon after topical (18 μg/ear) and oral (48.7 mg/kg) administration has antiedematous effects in the arachidonic acid-induced mouse ear inflammation test[4].
Veliflapon is potent (11.8 and 6.7 mg/kg p.o. at 1 and 5 hours, respectively) and has a long duration of action (ED40 of 16 hours, 70 mg/kg p.o.) in the rat whole blood ex vivo leukotriene B4 inhibition assay[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female apoE/LDLR-DKO mouse model[4]
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Dosage:18.8 mg/kg
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Administration:Diet; per day during 16 weeks
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Result:Inhibited atherogenesis.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 128253-31-6
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Appearance Solid
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Molecular Weight 361.43
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Formula C23H23NO3
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Color White to light yellow
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SMILES
O=C(O)[C@H](C1CCCC1)C(C=C2)=CC=C2OCC3=NC4=CC=CC=C4C=C3
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Synonyms
BAY X 1005; DG-031
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 100 mg/mL (276.68 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (274 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[1]. Hatzelmann A, et al. Mode of action of the leukotriene synthesis (FLAP) inhibitor BAY X 1005: implications for biological regulation of 5-lipoxygenase. Agents Actions. 1994 Nov;43(1-2):64-8. [Content Brief]
[2]. Müller-Peddinghaus R, et al. BAY X1005, a new inhibitor of leukotriene synthesis: in vivo inflammation pharmacology and pharmacokinetics. J Pharmacol Exp Ther. 1993 Oct;267(1):51-7. [Content Brief]
[3]. Fruchtmann R, et al. In vitro pharmacology of BAY X1005, a new inhibitor of leukotriene synthesis. Agents Actions. 1993 Mar;38(3-4):188-95. [Content Brief]
[4]. Jawień J, et al. BAY x 1005 attenuates atherosclerosis in apoE/LDLR - double knockout mice. J Physiol Pharmacol. 2007 Sep;58(3):583-8. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.7668 mL | 13.8339 mL | 27.6679 mL | 69.1697 mL |
| 5 mM | 0.5534 mL | 2.7668 mL | 5.5336 mL | 13.8339 mL | |
| 10 mM | 0.2767 mL | 1.3834 mL | 2.7668 mL | 6.9170 mL | |
| 15 mM | 0.1845 mL | 0.9223 mL | 1.8445 mL | 4.6113 mL | |
| 20 mM | 0.1383 mL | 0.6917 mL | 1.3834 mL | 3.4585 mL | |
| 25 mM | 0.1107 mL | 0.5534 mL | 1.1067 mL | 2.7668 mL | |
| 30 mM | 0.0922 mL | 0.4611 mL | 0.9223 mL | 2.3057 mL | |
| 40 mM | 0.0692 mL | 0.3458 mL | 0.6917 mL | 1.7292 mL | |
| 50 mM | 0.0553 mL | 0.2767 mL | 0.5534 mL | 1.3834 mL | |
| 60 mM | 0.0461 mL | 0.2306 mL | 0.4611 mL | 1.1528 mL | |
| 80 mM | 0.0346 mL | 0.1729 mL | 0.3458 mL | 0.8646 mL | |
| 100 mM | 0.0277 mL | 0.1383 mL | 0.2767 mL | 0.6917 mL |
Veliflapon Related Classifications
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