| Identification | Back Directory | [Name]
(2R)-2-cyclopentyl-2-[4-(quinolin-2-ylmethoxy)phenyl]acetic acid | [CAS]
128253-31-6 | [Synonyms]
DG 031
BAY 1005
Velifapon
VELIFLAPON
BAY-X 1005
BAY-X-1005 >=98% (HPLC)
ZEYYDOLCHFETHQ-JOCHJYFZSA-N
2-(4-(quinolin-2-yl-methoxy)phenyl)-2-cyclopentylacetic acid
α-Cyclopentyl-4-(2-quinolinylmethoxy)-(R)-benzeneacetic acid
(αR)-α-Cyclopentyl-4-(2-quinolinylmethoxy)-benzeneacetic acid
(2R)-2-cyclopentyl-2-[4-(quinolin-2-ylmethoxy)phenyl]acetic acid
Benzeneacetic acid, α-cyclopentyl-4-(2-quinolinylmethoxy)-, (αR)- | [Molecular Formula]
C23H23NO3 | [MDL Number]
MFCD00870329 | [MOL File]
128253-31-6.mol | [Molecular Weight]
361.43 |
| Chemical Properties | Back Directory | [Melting point ]
169-171 °C | [Boiling point ]
555.4±40.0 °C(Predicted) | [density ]
1.242±0.06 g/cm3(Predicted) | [storage temp. ]
2-8°C | [solubility ]
DMSO: soluble5mg/mL (clear solution) | [form ]
powder | [pka]
4.47±0.10(Predicted) | [color ]
white to beige |
| Hazard Information | Back Directory | [Uses]
Prevention of acute cardiovascular events. | [Biological Activity]
bay-x 1005 is a selective inhibitor of 5-lipoxygenase-activating protein [1].5-lipoxygenase-activating protein (flap) is an integral protein and plays an important role in the activation of 5-lipoxygenase (5-lox) and the synthesis of leukotrienes, which regulating immune responses.bay-x 1005 is a selective inhibitor of leukotriene synthesis. bay x 1005 binds to flap and inhibits 5-lox translocation from the cytosol to membranes [1]. bay-x1005 inhibited ltb4 synthesis with ic50 values of 0.22, 0.026 and 0.039 μm for isolated pmnl of human, rat and mouse respectively and inhibited ltc4 synthesis with ic50 value of 0.021 μm in mouse macrophages [2].in the arachidonate-induced mouse ear inflammation test, bay-x 1005 inhibited myeloperoxidase activity and edema formation with ed50 values of 7.9 and 48.7, respectively [2].also, bay-x 1005 (100 mg/kg) reduced platelet-activating factor-induced death of mice by 51% in a dose-dependent way. in animal models, bay-x 1005 inhibited the synthesis of ltb4 and ltc4, which reduced edema formation, the vascular phenomena of inflammation and leukocyte immigration [3]. | [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 (ED40 of 16 hours, 70 mg/kg p.o.) in the rat whole blood ex vivo leukotriene B4 inhibition assay[4].
| Animal Model: | Female apoE/LDLR-DKO mouse model[4] | | Dosage: | 18.8 mg/kg | | Administration: | Diet; per day during 16 weeks | | Result: | Inhibited atherogenesis.
|
| [IC 50]
LTB4; LTC4 | [References]
[1]. hatzelmann a, fruchtmann r, mohrs kh, et al. mode of action of the leukotriene synthesis (flap) inhibitor bay x 1005: implications for biological regulation of 5-lipoxygenase. agents actions, 1994, 43(1-2): 64-68.
[2]. müller-peddinghaus r, fruchtmann r, ahr hj, et al. bay x1005, a new selective inhibitor of leukotriene synthesis: pharmacology and pharmacokinetics. j lipid mediat, 1993, 6(1-3): 245-248.
[3]. müller-peddinghaus r, kohlsdorfer c, theisen-popp p, et al. bay x1005, a new inhibitor of leukotriene synthesis: in vivo inflammation pharmacology and pharmacokinetics. j pharmacol exp ther, 1993, 267(1): 51-57. |
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