BAY-X-1005 - CAS 128253-31-6
Catalog number:
128253-31-6
Category:
Inhibitor
Not Intended for Therapeutic Use. For research use only.
Molecular Formula:
C23H23NO3
Molecular Weight:
361.43
COA:
Inquire
Targets:
FLAP
Description:
BAY-X 1005 is a potent and selective FLAP (5-lipoxygenase-activating protein) inhibitor. BAY-X 1005 is also a selective inhibitor of leukotriene synthesis. BAY-X1005 inhibited LTB4 synthesis with IC50 values of 220 nM for isolated PMNL of human and inhibited LTC4 synthesis with IC50 value of 210 nM in mouse macrophages. Phase-III for Myocardial infarction in USA was suspended in 2006.
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Purity:
>98 %
Appearance:
white to beige powder
Synonyms:
Veliflapon;DG-031;(2R)-2-cyclopentyl-2-[4-(quinolin-2-ylmethoxy)phenyl]acetic acid
Solubility:
DMSO: soluble5 mg/mL (clear solution)
Storage:
-20°C Freezer
MSDS:
Inquire
Application:
Myocardial infarction
Quality Standard:
In-house standard
Shelf Life:
2 month in rt, long time
Quantity:
Milligrams-Grams
Boiling Point:
555.4ºC at 760mmHg
Density:
1.242g/cm3
InChIKey:
ZEYYDOLCHFETHQ-JOCHJYFZSA-N
InChI:
InChI=1S/C23H23NO3/c25-23(26)22(17-6-1-2-7-17)18-10-13-20(14-11-18)27-15-19-12-9-16-5-3-4-8-21(16)24-19/h3-5,8-14,17,22H,1-2,6-7,15H2,(H,25,26)/t22-/m1/s1
Canonical SMILES:
C1CCC(C1)C(C2=CC=C(C=C2)OCC3=NC4=CC=CC=C4C=C3)C(=O)O
Current Developer:
deCODE genetics
1.Study of the role of leukotriene B()4 in abnormal function of human subchondral osteoarthritis osteoblasts: effects of cyclooxygenase and/or 5-lipoxygenase inhibition.
Paredes Y1, Massicotte F, Pelletier JP, Martel-Pelletier J, Laufer S, Lajeunesse D. Arthritis Rheum. 2002 Jul;46(7):1804-12.
OBJECTIVE: To compare the effect of licofelone, NS-398 (an inhibitor of cyclooxygenase 2 [COX-2]), and BayX-1005 (an inhibitor of 5-lipoxygenase activating protein) on the production of leukotriene B(4) (LTB(4)) and prostaglandin E(2) (PGE(2)), and on cell biomarkers by human osteoarthritis (OA) subchondral osteoblasts.
2.Inhibition of 5-lipoxygenase-activating protein abrogates experimental liver injury: role of Kupffer cells.
Titos E1, Clària J, Planagumà A, López-Parra M, González-Périz A, Gaya J, Miquel R, Arroyo V, Rodés J. J Leukoc Biol. 2005 Oct;78(4):871-8. Epub 2005 Jul 20.
Activation of Kupffer cells is a prominent feature of necro-inflammatory liver injury. We have recently demonstrated that 5-lipoxygenase (5-LO) and its accessory protein, 5-LO-activating protein (FLAP), are essential for the survival of Kupffer cells in culture, as their inhibition drives these liver resident macrophages to programmed cell death. In the current study, we explored whether the potent FLAP inhibitor, Bay-X-1005, reduces the number of Kupffer cells in vivo and whether this pharmacological intervention protects the liver from carbon tetrachloride (CCl(4))-induced damage. Rats treated with CCl(4) showed an increased number of Kupffer cells, an effect that was abrogated by the administration of Bay-X-1005 (100 mg/Kg body weight, per oral, daily). Consistent with a role for Kupffer cells in necro-inflammatory liver injury, partial depletion of Kupffer cells following FLAP inhibition was associated with a remarkable hepatoprotective action.
3.FLAP inhibitors for the treatment of inflammatory diseases.
Sampson AP1. Curr Opin Investig Drugs. 2009 Nov;10(11):1163-72.
Leukotrienes are lipid inflammatory mediators that are implicated in asthma, COPD, arthritis, cardiovascular disease and cancer. Leukotriene synthesis requires 5-lipoxygenase activating protein (FLAP), which acts as a scaffolding protein for the assembly of other enzymes involved in the leukotriene synthetic pathway occurring at the nuclear envelope of leukocytes. By blocking the formation of both leukotriene B4 and the cysteinyl leukotrienes (ie, LTC4 , LTD4 and LTE4), FLAP inhibitors act as broad-spectrum leukotriene-modifier drugs that may have a wide range of therapeutic applications. FLAP inhibitors such as MK-886, MK-0591 and veliflapon (BAY-X-1005, DG-031) demonstrated promise in clinical trials with patients with inflammatory diseases in the mid 1990 s, but, unlike the 'lukast' class of cysteinyl-leukotriene receptor antagonists, these compounds were not brought to market. The elucidation of the 3D structure of FLAP has enabled novel compound development, and several FLAP inhibitors including 2190914 (AM-103) and GSK-2190915 (both under development by GlaxoSmithKline plc) have entered phase II trials for the treatment of inflammatory disease, including asthma.
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CAS 128253-31-6 BAY-X-1005

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