WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H526546
CAS#: 128253-31-6 (acid)
Description: 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)
Hodoodo Cat#: H526546
Name: Veliflapon
CAS#: 128253-31-6 (acid)
Chemical Formula: C23H23NO3
Exact Mass: 361.17
Molecular Weight: 361.441
Elemental Analysis: C, 76.43; H, 6.41; N, 3.88; O, 13.28
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:
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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 |
| Formulation protocol: | |
| In vitro protocol: | |
| In vivo protocol: |
1: Müller-Peddinghaus R. Potential anti-inflammatory effects of 5-lipoxygenase inhibition--exemplified by the leukotriene synthesis inhibitor BAY X 1005. J Physiol Pharmacol. 1997 Dec;48(4):529-36. Review. PubMed PMID: 9444606.
2: Burchardt ER, Müller-Peddinghaus R. Antiedematous effects of combination therapies with the leukotriene synthesis inhibitor BAY X 1005 in the archidonic acid-induced mouse ear inflammation test. Prostaglandins Leukot Essent Fatty Acids. 1997 Apr;56(4):301-6. PubMed PMID: 9150376.
3: Jawień J, Gajda M, Olszanecki R, Korbut R. BAY x 1005 attenuates atherosclerosis in apoE/LDLR - double knockout mice. J Physiol Pharmacol. 2007 Sep;58(3):583-8. PubMed PMID: 17928652.
4: 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. PubMed PMID: 10319912.
5: Cunningham FM, Andrews M, Landoni MF, Lees P. Pharmacology of the 5-lipoxygenase inhibitors BAY Y 1015 and BAY X 1005 in the horse. J Vet Pharmacol Ther. 1997 Aug;20(4):296-307. PubMed PMID: 9280370.
6: Groen H, Moesker HL, Leeuwenkamp OR, Sollie FA, Jonkman JH. No pharmacokinetic or pharmacodynamic interaction between theophylline and the leukotriene biosynthesis inhibitor BAY x 1005. J Clin Pharmacol. 1996 Jul;36(7):639-46. PubMed PMID: 8844447.
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 X 1005: implications for biological regulation of 5-lipoxygenase. Agents Actions. 1994 Nov;43(1-2):64-8. Review. PubMed PMID: 7741044.
8: Hatzelmann A, Fruchtmann R, Mohrs KH, Raddatz S, Müller-Peddinghaus R. Mode of action of the new selective leukotriene synthesis inhibitor BAY X 1005 ((R)-2-[4-(quinolin-2-yl-methoxy)phenyl]-2-cyclopentyl acetic acid) and structurally related compounds. Biochem Pharmacol. 1993 Jan 7;45(1):101-11. PubMed PMID: 8381000.
