[CAS NO. 128253-31-6] Veliflapon
PRODUCTS SPECIFICATIONS [128253-31-6]
DESCRIPTION [128253-31-6]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 361.43 |
| Molecular Formula | C23H23NO3 |
| SMILES | O=C(O)[C@H](C1CCCC1)C(C=C2)=CC=C2OCC3=NC4=CC=CC=C4C=C3 |
Summary
IC50 & Target
|
LTB 4 |
LTC 4 |
In Vitro
Veliflapon (BAY X 1005; DG-031) effectively inhibits the synthesis of LTB4 in A23187-stimulated leukocytes from rats, mice and humans (IC
50
s of 0.026, 0.039 and 0.22 μM, respectively) as well as the formation of LTC4 (IC
50
of 0.021 μM) in mouse peritoneal macrophages stimulated with opsonized zymosan
[3]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Veliflapon (BAY X 1005; DG-031; diet; 18.8 mg/kg/day for 16 weeks ) inhibits atherogenesis
[4]
.
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 (ED
40
of 16 hours, 70 mg/kg p.o.) in the rat whole blood ex vivo leukotriene B4 inhibition assay
[4]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: | Female apoE/LDLR-DKO mouse model [4] |
| Dosage: | 18.8 mg/kg |
| Administration: | Diet; per day during 16 weeks |
| Result: | Inhibited atherogenesis. |
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date | Phase |
|---|---|---|---|---|
| NCT00353067 | deCODE genetics|Henry Ford Health System|Duke University |
Acute Coronary Syndrome
|
May 2006 | Phase 3 |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
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)
Stock Solutions
| Concentration Solvent Mass | 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 |
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.
- [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.
- [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.
- [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.