A 78773

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

MedKoo CAT#: 571191

CAS#: 141579-67-1

Description: A 78773 is a potent, selective, direct, and reversible 5-lipoxygenase inhibitor. It has activity in a variety of purified cells and in more complex biological systems such as whole blood, lung fragments, and tracheal tissues. A 78773 acts against inflammation and allergy, edema, inflammatory cell influx, and bronchospasm. It may treat asthma and inflammatory bowel disease.


Price and Availability

Size
Price

Size
Price

Size
Price

A 78773 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

img

Theoretical Analysis

MedKoo Cat#: 571191
Name: A 78773
CAS#: 141579-67-1
Chemical Formula: C15H13FN2O4
Exact Mass: 304.0859
Molecular Weight: 304.28
Elemental Analysis: C, 59.21; H, 4.31; F, 6.24; N, 9.21; O, 21.03


Synonym: A 78773; A-78773; A78773

IUPAC/Chemical Name: Urea, N-(3-(5-(4-fluorophenoxy)-2-furanyl)-1-methyl-2-propynyl)-N-hydroxy-

InChi Key: OLZHFFKRBCZHHT-UHFFFAOYSA-N

InChi Code: InChI=1S/C15H13FN2O4/c1-10(18(20)15(17)19)2-5-12-8-9-14(21-12)22-13-6-3-11(16)4-7-13/h3-4,6-10,20H,1H3,(H2,17,19)

SMILES Code: O=C(N)N(C(C)C#CC1=CC=C(OC2=CC=C(F)C=C2)O1)O


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: Bell RL, Lanni C, Malo PE, Brooks DW, Stewart AO, Hansen R, Rubin P, Carter GW. Preclinical and clinical activity of zileuton and A-78773. Ann N Y Acad Sci. 1993 Nov 30;696:205-15. PubMed PMID: 8109828.

2: Rao TS, Currie JL, Shaffer AF, Isakson PC. Evaluation of 5-lipoxygenase inhibitors, zileuton, A-78773 and ICI-D-2138 in an ionophore (A-23187)-induced pleural inflammation model in the rat. Life Sci. 1993;53(9):PL147-52. PubMed PMID: 8394967.

3: Bell RL, Brooks DW, Young PR, Lanni C, Stewart AO, Bouska J, Malo PE, Carter GW. A-78773: a selective, potent 5-lipoxygenase inhibitor. J Lipid Mediat. 1993 Mar-Apr;6(1-3):259-64. PubMed PMID: 8395248.

4: Carter GW, Bell RL, Marsh K, Lanni C, Awni WM, Bouska J, Stewart AO, Hansen R, Dubé L, Brooks DW. Stereoselective metabolism of the 5-lipoxygenase inhibitor A-78773. Ann N Y Acad Sci. 1994 Nov 15;744:262-73. PubMed PMID: 7825849.

5: Smith WG, Shaffer AF, Currie JL, Thompson JM, Kim S, Rao T, Isakson PC. Characterization of 5-lipoxygenase inhibitors in biochemical and functional in vivo assays. J Pharmacol Exp Ther. 1995 Dec;275(3):1332-8. PubMed PMID: 8531100.

6: Nair DG, Funk CD. A cell-based assay for screening lipoxygenase inhibitors. Prostaglandins Other Lipid Mediat. 2009 Dec;90(3-4):98-104. doi: 10.1016/j.prostaglandins.2009.09.006. Epub 2009 Oct 3. PubMed PMID: 19804839.

7: Li R, Mayer PT, Trivedi JS, Fort JJ. Polymorphism and crystallization behavior of Abbott-79175, a second-generation 5-lipoxygenase inhibitor. J Pharm Sci. 1996 Jul;85(7):773-80. PubMed PMID: 8819005.

8: Negro JM, Miralles JC, Ortiz JL, Funes E, García A. Biosynthesis inhibitors for leukotrienes in bronchial asthma. Allergol Immunopathol (Madr). 1997 Jul-Aug;25(4):209-16. Review. PubMed PMID: 9269512.

9: Bell RL, Bouska JB, Malo PE, Lanni C, Harris RR, Otis ER, Stewart AO, Brooks DW, Carter GW. Optimization of the potency and duration of action of N-hydroxyurea 5-lipoxygenase inhibitors. J Pharmacol Exp Ther. 1995 Feb;272(2):724-31. PubMed PMID: 7853186.

10: Anderson GD, Keys KL, De Ciechi PA, Masferrer JL. Combination therapies that inhibit cyclooxygenase-2 and leukotriene synthesis prevent disease in murine collagen induced arthritis. Inflamm Res. 2009 Feb;58(2):109-17. doi: 10.1007/s00011-009-8149-3. PubMed PMID: 19184362.

11: McLoughlin M, Kearney AS, Palepu NR. Aqueous stability of SB 210661: kinetics and primary degradation mechanisms of an N-hydroxyurea-containing 5-lipoxygenase inhibitor. J Pharm Pharmacol. 1998 Feb;50(2):127-32. PubMed PMID: 9530978.

12: Harris RR, Wilcox D, Bell RL, Carter GW. The role of tissue mast cells in polyacrylamide gel-induced inflammation in mice. Inflamm Res. 1998 Mar;47(3):104-8. PubMed PMID: 9562335.

13: Rioux N, Castonguay A. Inhibitors of lipoxygenase: a new class of cancer chemopreventive agents. Carcinogenesis. 1998 Aug;19(8):1393-400. PubMed PMID: 9744535.

14: Hulkower KI, Pollock JS, Walsh RE, Huang R, Otis ER, Brooks CD, Bell RL. Leukotrienes do not regulate nitric oxide production in RAW 264.7 macrophages. Prostaglandins Leukot Essent Fatty Acids. 1996 Sep;55(3):145-9. PubMed PMID: 8931110.

15: Howarth PH, Harrison K, Lau L. The influence of 5-lipoxygenase inhibition in allergic rhinitis. Int Arch Allergy Immunol. 1995 May-Jun;107(1-3):423-4. PubMed PMID: 7613199.