Veliflapon | CAS#128253-31-6 | Leukotriene Synthesis Inhibitor

MedKoo Cat#: 526546 | Name: Veliflapon

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Description:

WARNING: This product is for research use only, not for human or veterinary use.

Veliflapon, also known as BAY X 1005 and DG-031, is a leukotriene synthesis inhibitor. BAY x 1005 attenuates atherosclerosis in apoE/LDLR - double knockout mice. BAY-X1005 is a 5-lipoxygenase activating protein (FLAP) inhibitor. BAY-X1005 inhibits the synthesis of leukotrienes B4 and C4 in animal models and it inhibits synthesis of leukotriene B4 in A23187-stimulated leukocytes (IC50 values are 0.026, 0.039 and 0.22 μM for rat, mice and human leukocytes respectively)

Chemical Structure

Veliflapon

CAS# 128253-31-6 (acid)

Theoretical Analysis

MedKoo Cat#: 526546

Name: Veliflapon

CAS#: 128253-31-6 (acid)

Chemical Formula: C23H23NO3

Exact Mass: 361.1678

Molecular Weight: 361.44

Elemental Analysis: C, 76.43; H, 6.41; N, 3.88; O, 13.28

Price and Availability

Size	Price	Availability	Quantity
5mg	USD 500.00
10mg	USD 700.00
25mg	USD 850.00

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Related CAS #

128253-31-6 (acid)

Synonym

Bay X1005; Bay X-1005; Bay X 1005; DG 031; DG-031; DG031; Veliflapon;

IUPAC/Chemical Name

(R)-2-(4-(Quinolin-2-yl-methoxy)phenyl)-2-cyclopentylacetic acid

InChi Key

ZEYYDOLCHFETHQ-JOCHJYFZSA-N

InChi Code

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

SMILES Code

O=C(O)[C@@H](C1=CC=C(OCC2=NC3=CC=CC=C3C=C2)C=C1)C4CCCC4

Appearance

White to beige solid powder

Purity

>98% (or refer to the Certificate of Analysis)

Shipping Condition

Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition

Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility

Soluble in DMSO, not in water

Shelf Life

>2 years if stored properly

Drug Formulation

This drug may be formulated in DMSO

Stock Solution Storage

0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code

2934.99.9001

More Info

Instruction

View handling instruction

Preparing Stock Solutions

The following data is based on the product molecular weight 361.44 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

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PMID: 16033810. 6: Hakonarson H, Thorvaldsson S, Helgadottir A, Gudbjartsson D, Zink F, Andresdottir M, Manolescu A, Arnar DO, Andersen K, Sigurdsson A, Thorgeirsson G, Jonsson A, Agnarsson U, Bjornsdottir H, Gottskalksson G, Einarsson A, Gudmundsdottir H, Adalsteinsdottir AE, Gudmundsson K, Kristjansson K, Hardarson T, Kristinsson A, Topol EJ, Gulcher J, Kong A, Gurney M, Thorgeirsson G, Stefansson K. Effects of a 5-lipoxygenase-activating protein inhibitor on biomarkers associated with risk of myocardial infarction: a randomized trial. JAMA. 2005 May 11;293(18):2245-56. doi: 10.1001/jama.293.18.2245. PMID: 15886380. 7: Rotondo S, Krauze-Brzósko K, Manarini S, Evangelista V, Cerletti C. Licofelone, an inhibitor of cyclooxygenase and 5-lipoxygenase, specifically inhibits cyclooxygenase-1-dependent platelet activation. Eur J Pharmacol. 2004 Mar 19;488(1-3):79-83. doi: 10.1016/j.ejphar.2004.02.006. PMID: 15044038. 8: Titos E, Clària J, Planagumà A, López-Parra M, Villamor N, Párrizas M, Carrió A, Miquel R, Jiménez W, Arroyo V, Rivera F, Rodés J. Inhibition of 5-lipoxygenase induces cell growth arrest and apoptosis in rat Kupffer cells: implications for liver fibrosis. FASEB J. 2003 Sep;17(12):1745-7. doi: 10.1096/fj.02-1157fje. Epub 2003 Jul 3. PMID: 12958196. 9: Fiorucci S, Distrutti E, Mencarelli A, Morelli A, Laufor SA, Cirino G, Wallace JL. Evidence that 5-lipoxygenase and acetylated cyclooxygenase 2-derived eicosanoids regulate leukocyte-endothelial adherence in response to aspirin. Br J Pharmacol. 2003 Aug;139(7):1351-9. doi: 10.1038/sj.bjp.0705356. PMID: 12890715; PMCID: PMC1573955. 10: Valdivielso JM, Montero A, Munger KA, Badr KF. Inhibition of 5-LO activating protein (FLAP) activity decreases proteinuria in streptozotocin (STZ)-induced diabetic rats. Adv Exp Med Biol. 2002;507:79-83. doi: 10.1007/978-1-4615-0193-0_13. PMID: 12664568. 11: Paredes Y, Massicotte F, Pelletier JP, Martel-Pelletier J, Laufer S, Lajeunesse D. Study of the role of leukotriene B()4 in abnormal function of human subchondral osteoarthritis osteoblasts: effects of cyclooxygenase and/or 5-lipoxygenase inhibition. Arthritis Rheum. 2002 Jul;46(7):1804-12. doi: 10.1002/art.10357. PMID: 12124864. 12: Gompertz S, Stockley RA. A randomized, placebo-controlled trial of a leukotriene synthesis inhibitor in patients with COPD. Chest. 2002 Jul;122(1):289-94. doi: 10.1378/chest.122.1.289. PMID: 12114372. 13: He W, Pelletier JP, Martel-Pelletier J, Laufer S, Di Battista JA. Synthesis of interleukin 1beta, tumor necrosis factor-alpha, and interstitial collagenase (MMP-1) is eicosanoid dependent in human osteoarthritis synovial membrane explants: interactions with antiinflammatory cytokines. J Rheumatol. 2002 Mar;29(3):546-53. PMID: 11908571. 14: Roger P, Gascard JP, Bara J, de Montpreville VT, Brink C. MUC5AC mucin release from human airways in vitro: effects of indomethacin and Bay X1005. Mediators Inflamm. 2001 Feb;10(1):33-6. doi: 10.1080/09629350124329. PMID: 11324902; PMCID: PMC1781691. 15: Steinbrink K, Schönlau F, Rescher U, Henseleit U, Vogel T, Sorg C, Sunderkötter C. Ineffective elimination of Leishmania major by inflammatory (MRP14-positive) subtype of monocytic cells. Immunobiology. 2000 Nov;202(5):442-59. doi: 10.1016/s0171-2985(00)80103-5. PMID: 11205374. 16: Folco G, Rossoni G, Buccellati C, Berti F, Maclouf J, Sala A. Leukotrienes in cardiovascular diseases. Am J Respir Crit Care Med. 2000 Feb;161(2 Pt 2):S112-6. doi: 10.1164/ajrccm.161.supplement_1.ltta-22. PMID: 10673238. 17: Larsson L, Sydbom A, Dahlén SE. Selective effects of antileukotrienes on leukotriene and histamine release in human dispersed lung cells. Inflamm Res. 1999 Apr;48 Suppl 1:S9-10. doi: 10.1007/s000110050372. PMID: 10350138. 18: Burchardt ER, Müller-Peddinghaus R. Favorable combination effects of the leukotriene synthesis inhibitor BAY X 1005 and dexamethasone on edema formation in the arachidonic acid-induced mouse ear inflammation test. Prostaglandins Leukot Essent Fatty Acids. 1999 Jan;60(1):5-11. doi: 10.1054/plef.1998.0002. PMID: 10319912. 19: Boehncke WH, Kock M, Hardt-Weinelt K, Wolter M, Kaufmann R. The SCID-hu xenogeneic transplantation model allows screening of anti-psoriatic drugs. Arch Dermatol Res. 1999 Feb-Mar;291(2-3):104-6. doi: 10.1007/s004030050391. PMID: 10195398. 20: Sampson A, Holgate S. Leukotriene modifiers in the treatment of asthma. Look promising across the board of asthma severity. BMJ. 1998 Apr 25;316(7140):1257-8. doi: 10.1136/bmj.316.7140.1257. PMID: 9554892; PMCID: PMC1113026.