AS-35

Modify Date: 2024-01-13 17:11:39

AS-35 Structure
AS-35 structure
Common Name AS-35
CAS Number 108427-72-1 Molecular Weight 420.42100
Density 1.46g/cm3 Boiling Point 678.8ºC at 760mmHg
Molecular Formula C21H20N6O4 Melting Point N/A
MSDS N/A Flash Point 364.4ºC

 Use of AS-35


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.

 Names

Name 9-[(4-acetyl-3-hydroxy-2-propylphenoxy)methyl]-3-(2H-tetrazol-5-yl)pyrido[1,2-a]pyrimidin-4-one
Synonym More Synonyms

 AS-35 Biological Activity

Description 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.
Related Catalog
Target

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)

In Vitro In isolated guinea pig preparations, AS-35 antagonizes LTC4-, LTD4 and LTE4-induced contractions of the ileum with IC50 values of 8 nM, 4 nM and 3 nM, respectively. In the trachea, the agent also antagonizes LTD4 and LTE4-induced con tractions with IC50 values of 10 nM and 20 nM, respectively. However, AS-35 does not antagonize LTC4-induced tracheal contraction in the presence of L-serine borate[1].
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].
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.

 Chemical & Physical Properties

Density 1.46g/cm3
Boiling Point 678.8ºC at 760mmHg
Molecular Formula C21H20N6O4
Molecular Weight 420.42100
Flash Point 364.4ºC
Exact Mass 420.15500
PSA 135.36000
LogP 2.31430
Vapour Pressure 4.74E-19mmHg at 25°C
Index of Refraction 1.707
Storage condition 2-8℃

 Synthetic Route

~98%

AS-35 Structure

AS-35

CAS#:108427-72-1

Literature: Tokyo Tanabe Co. Ltd. Patent: US4816459 A1, 1989 ;

~65%

AS-35 Structure

AS-35

CAS#:108427-72-1

Literature: Tokyo Tanabe Co. Ltd. Patent: US4816459 A1, 1989 ;

 Precursor & DownStream

Precursor  2

DownStream  0

 Synonyms

as-35