| Identification | Back Directory | [Name]
AS 35 | [CAS]
108427-72-1 | [Synonyms]
AS 35
4H-Pyrido[1,2-a]pyrimidin-4-one, 9-[(4-acetyl-3-hydroxy-2-propylphenoxy)methyl]-3-(2H-tetrazol-5-yl)-
3-(1H-Tetrazol-5-yl)-9-[[[2-propyl-3-hydroxy-4-(methylcarbonyl)phenyl]oxy]methyl]-4H-pyrido[1,2-a]pyrimidin-4-one | [Molecular Formula]
C21H20N6O4 | [MDL Number]
MFCD00892239 | [MOL File]
108427-72-1.mol | [Molecular Weight]
420.42 |
| Chemical Properties | Back Directory | [Melting point ]
269-271 °C | [Boiling point ]
678.8±65.0 °C(Predicted) | [density ]
1.46±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
Soluble in DMSO | [pka]
3?+-.0.10(Predicted) |
| Hazard Information | Back Directory | [Uses]
AS-35 is an orally effective, potent and selective antagonist of leukotrienes, antagonizes LTC4-, LTD4 and LTE4-induced contractions of the ileum with IC50 values of 8 nM, 4 nM and 3 nM, respectively, and has antiallergic activities. | [in vivo]
AS-35 (0.0375 to 0.3 mg/kg, i.v.) dose-dependently antagonizes bronchoconstriction induced by i.v.-injection of LTC4 and LTD4 in anesthetized guinea pigs, but does not inhibit histamine-induced bronchoconstriction. Oral administration of AS-35 also antagonizes LTD4 as well as antigen-induced LT-mediated bronchoconstriction. AS-35 (p.o.) inhibits LTD4-induced increase in the cutaneous vascular permeability of guinea pig[1]. | [IC 50]
LTE4: 3 nM (IC50, In isolated guinea pig ileum); LTD4: 4 nM (IC50, In isolated guinea pig ileum); LTC4: 8 nM (IC50, In isolated guinea pig ileum) | [References]
[1] Kasai H, et al. Peptide leukotriene antagonistic activity of AS-35, a new antiallergic drug. Jpn J Pharmacol. 1992 Apr;58(4):347-55. DOI:10.1254/jjp.58.347 |
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