108427-72-1
108427-72-1 structure
- Name: AS-35
- Chemical Name: 9-[(4-acetyl-3-hydroxy-2-propylphenoxy)methyl]-3-(2H-tetrazol-5-yl)pyrido[1,2-a]pyrimidin-4-one
- CAS Number: 108427-72-1
- Molecular Formula: C21H20N6O4
- Molecular Weight: 420.42100
- Catalog: Signaling Pathways GPCR/G Protein Leukotriene Receptor
- Create Date: 2017-11-01 13:15:23
- Modify Date: 2024-01-13 17:11:39
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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.
| Name | 9-[(4-acetyl-3-hydroxy-2-propylphenoxy)methyl]-3-(2H-tetrazol-5-yl)pyrido[1,2-a]pyrimidin-4-one |
|---|---|
| Synonyms | as-35 |
| 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. |
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| 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 |
| 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℃ |
|
~98%
108427-72-1 |
| Literature: Tokyo Tanabe Co. Ltd. Patent: US4816459 A1, 1989 ; |
|
~65%
108427-72-1 |
| Literature: Tokyo Tanabe Co. Ltd. Patent: US4816459 A1, 1989 ; |
| Precursor 2 | |
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| DownStream 0 | |