BAY-X1005

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

MedKoo CAT#: 531567

CAS#: 128253-31-6

Description: 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).


Price and Availability

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BAY-X1005 , is not in stock, may be available through custom synthesis. For cost-effective reason, minimum 1 gram order is requested. The product will be characterized by NMR, HPLC and MS analysis. Purity (HPLC) is usually >98%. CoA, QC data, MSDS will be provided when product is successfully made. The estimated lead time is 2-3 months. Please send email to sales@medkoo.com to inquire quote.


Chemical Structure

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Theoretical Analysis

MedKoo Cat#: 531567
Name: BAY-X1005
CAS#: 128253-31-6
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


Synonym: BAY-X1005; BAYX1005; BAY X1005; DG-031; veliflapon.

IUPAC/Chemical Name: (2R)-2-cyclopentyl-2-[4-(quinolin-2-ylmethoxy)phenyl]acetic 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](C1CCCC1)C2=CC=C(OCC3=NC4=CC=CC=C4C=C3)C=C2


Technical Data

Appearance:
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

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).

Harmonized System Code:
293490


References

1: 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. PubMed PMID: 11324902; PubMed Central PMCID: PMC1781691.

2: Nagai H, Takeda H, Uno T, Tanaka H, Matsuo A. Effect of a novel leukotoriene synthesis inhibitor, BAY x1005, on the antigen-and LPS-induced airway hyperresponsiveness in guinea pigs. Prostaglandins. 1996 Feb;51(2):139-48. PubMed PMID: 8711135.

3: Rossoni G, Sala A, Berti F, Testa T, Buccellati C, Molta C, Muller-Peddinghaus R, Maclouf J, Folco GC. Myocardial protection by the leukotriene synthesis inhibitor BAY X1005: importance of transcellular biosynthesis of cysteinyl-leukotrienes. J Pharmacol Exp Ther. 1996 Jan;276(1):335-41. PubMed PMID: 8558451.

4: Hatzelmann A, Goossens J, Fruchtmann R, Mohrs KH, Raddatz S, Müller-Peddinghaus R. Inversely-correlated inhibition of human 5-lipoxygenase activity by BAY X1005 and other quinoline derivatives in intact cells and a cell-free system--implications for the function of 5-lipoxygenase activating protein. Biochem Pharmacol. 1994 Jun 15;47(12):2259-68. PubMed PMID: 8031320.

5: Gardiner PJ, Cuthbert NJ, Francis HP, Fitzgerald MF, Thompson AM, Carpenter TG, Patel UP, Newton BB, Mohrs K, Müller-Peddinghaus R, et al. Inhibition of antigen-induced contraction of guinea-pig airways by a leukotriene synthesis inhibitor, BAY x1005. Eur J Pharmacol. 1994 Jun 2;258(1-2):95-102. PubMed PMID: 7925604.

6: Gorenne I, Labat C, Gascard JP, Norel X, Müller-Peddinghaus R, Mohrs KH, Taylor WA, Gardiner PJ, Brink C. (R)-2-[4-(quinolin-2-yl-methoxy)phenyl]-2-cyclopentyl] acetic acid (BAY x1005), a potent leukotriene synthesis inhibitor: effects on anti-IgE challenge in human airways. J Pharmacol Exp Ther. 1994 Feb;268(2):868-72. PubMed PMID: 8114000.

7: Hatzelmann A, Fruchtmann R, Mohrs KH, Raddatz S, Matzke M, Pleiss U, Keldenich J, Müller-Peddinghaus R. Mode of action of the leukotriene synthesis (FLAP) inhibitor BAY X1005. Implications for biological regulation of 5-lipoxygenase. Adv Prostaglandin Thromboxane Leukot Res. 1994;22:23-31. Review. PubMed PMID: 7771337.

8: Müller-Peddinghaus R, Kohlsdorfer C, Theisen-Popp P, Fruchtmann R, Perzborn E, Beckermann B, Bühner K, Ahr HJ, Mohrs KH. BAY X1005, a new inhibitor of leukotriene synthesis: in vivo inflammation pharmacology and pharmacokinetics. J Pharmacol Exp Ther. 1993 Oct;267(1):51-7. PubMed PMID: 8229782.

9: Müller-Peddinghaus R, Fruchtmann R, Ahr HJ, Beckermann B, Bühner K, Fugmann B, Junge B, Matzke M, Kohlsdorfer C, Raddatz S, et al. BAY X1005, a new selective inhibitor of leukotriene synthesis: pharmacology and pharmacokinetics. J Lipid Mediat. 1993 Mar-Apr;6(1-3):245-8. PubMed PMID: 8395246.

10: Fruchtmann R, Mohrs KH, Hatzelmann A, Raddatz S, Fugmann B, Junge B, Horstmann H, Müller-Peddinghaus R. In vitro pharmacology of BAY X1005, a new inhibitor of leukotriene synthesis. Agents Actions. 1993 Mar;38(3-4):188-95. PubMed PMID: 8213345.