BAY-X 1005

Modify Date: 2024-01-10 20:56:27

BAY-X 1005 structure	Common Name	BAY-X 1005
	CAS Number	128253-31-6	Molecular Weight	361.43400
	Density	1.242g/cm3	Boiling Point	555.4ºC at 760mmHg
	Molecular Formula	C₂₃H₂₃NO₃	Melting Point	N/A
	MSDS	Chinese USA	Flash Point	289.7ºC
	Symbol	GHS07	Signal Word	Warning

Use of BAY-X 1005

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
Synonym	More Synonyms

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	Research Areas >> Cardiovascular Disease Signaling Pathways >> GPCR/G Protein >> Leukotriene Receptor Research Areas >> Inflammation/Immunology Signaling Pathways >> Metabolic Enzyme/Protease >> 5-Lipoxygenase
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	[1]. 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. [2]. 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. [3]. Jawień J, et al. BAY x 1005 attenuates atherosclerosis in apoE/LDLR - double knockout mice. J Physiol Pharmacol. 2007 Sep;58(3):583-8.

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

N/A

CAS#:177275-24-0

~87%

BAY-X 1005

CAS#: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

2-cyclopentyl-2...

CAS#:931583-38-9

BAY-X 1005

CAS#:128253-31-6

Literature: Journal of the American Chemical Society, , vol. 129, # 7 p. 1868 - 1869

N/A

CAS#:931583-40-3

BAY-X 1005

CAS#:128253-31-6

Literature: Journal of the American Chemical Society, , vol. 129, # 7 p. 1868 - 1869

Leukotriene modifiers in the treatment of asthma. Look promising across the board of asthma severity.

BMJ 316(7140) , 1257-8, (1998)

BAY x 1005 attenuates atherosclerosis in apoE/LDLR - double knockout mice.

J. Physiol. Pharmacol. 58(3) , 583-8, (2007)

Recently, we have shown that MK-886 - an inhibitor of five lipoxygenase activating protein (FLAP) inhibits atherosclerosis in apolipoprotein E / LDL receptor - double knockout mice. We, therefore, wan...

Inhibition of 5-LO activating protein (FLAP) activity decreases proteinuria in streptozotocin (STZ)-induced diabetic rats.

Adv. Exp. Med. Biol. 507 , 79-83, (2002)

DG-031

Veliflapon

Bayx-1005