128253-31-6
128253-31-6 structure
- Name: BAY-X 1005
- Chemical Name: (2R)-2-cyclopentyl-2-[4-(quinolin-2-ylmethoxy)phenyl]acetic acid
- CAS Number: 128253-31-6
- Molecular Formula: C23H23NO3
- Molecular Weight: 361.43400
- Catalog: Signaling Pathways GPCR/G Protein Leukotriene Receptor
- Create Date: 2016-04-04 14:54:01
- Modify Date: 2024-01-10 20:56:27
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Veliflapon (BAY X 1005; DG-031) is an orally active inhibitor of the synthesis of the leukotrienes B4 and C4[1]. Veliflapon is shown to be a selective inhibitor of the formation of 5-lipoxygenase-derived metabolites in vitro, without effects on other routes of arachidonic acid metabolism[2].
| Name | (2R)-2-cyclopentyl-2-[4-(quinolin-2-ylmethoxy)phenyl]acetic acid |
|---|---|
| Synonyms |
DG-031
Veliflapon Bayx-1005 |
| Description | Veliflapon (BAY X 1005; DG-031) is an orally active inhibitor of the synthesis of the leukotrienes B4 and C4[1]. Veliflapon is shown to be a selective inhibitor of the formation of 5-lipoxygenase-derived metabolites in vitro, without effects on other routes of arachidonic acid metabolism[2]. |
|---|---|
| Related Catalog | |
| Target |
LTB4 LTC4 5-Lipoxygenase |
| In Vitro | 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[2]. |
| In Vivo | Veliflapon (BAY X 1005; DG-031; diet; 18.8 mg/kg/day for 16 weeks ) inhibits atherogenesis[3]. 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[3]. 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[3]. Animal Model: Female apoE/LDLR-DKO mouse model[3] Dosage: 18.8 mg/kg Administration: Diet; per day during 16 weeks Result: Inhibited atherogenesis. |
| References |
| Density | 1.242g/cm3 |
|---|---|
| Boiling Point | 555.4ºC at 760mmHg |
| Molecular Formula | C23H23NO3 |
| Molecular Weight | 361.43400 |
| Flash Point | 289.7ºC |
| Exact Mass | 361.16800 |
| PSA | 59.42000 |
| LogP | 5.17220 |
| Vapour Pressure | 0mmHg at 25°C |
| Index of Refraction | 1.645 |
| Symbol |
GHS07 |
|---|---|
| Signal Word | Warning |
| Hazard Statements | H302 |
| Hazard Codes | Xi |
| RIDADR | NONH for all modes of transport |
|
~87%
128253-31-6 |
| Literature: Xie, Jian-Hua; Zhou, Zhang-Tao; Kong, Wei-Ling; Zhou, Qi-Lin Journal of the American Chemical Society, 2007 , vol. 129, # 7 p. 1868 - 1869 |
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128253-31-6 |
| Literature: Journal of the American Chemical Society, , vol. 129, # 7 p. 1868 - 1869 |
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128253-31-6 |
| Literature: Journal of the American Chemical Society, , vol. 129, # 7 p. 1868 - 1869 |
