| Bioactivity | KP136 (AL136) is an orally effective antiallergic agent. The IC50 is 76.1 μg/mL for histamine release and 63 ug/mL for degranulation[1]. |
| Target | Histamine release |
| Invitro | KP136 (0.01 μg/mL) inhibits this histamine release and degranulation in a dose-dependent manner, confirming that it is an inhibitor of mast cell activation. The IC50 is 76.1 μg/mL for histamine release and 63 ug/mL for degranulation[1]. |
| In Vivo | C4C at 0.2 mg/kg produces an equipotent effect to 1 mg/kg KP136 (KP-136) or 5 mg/kg DSCG. However, C4C is less effective by the oral route because it only produces a maximum inhibition of about 35% even at the high dose of 100 mg/kg, whereas KP136 shows an overt inhibitory effect of about 66% at the oral dose of 2 mg/kg. On the other hand, KP136 (1 mg/kg, i.v.) also remarkably inhibits 5-h homologous PCA, having an activity similar to that of C4C[1]. |
| Name | KP136 |
| CAS | 76239-32-2 |
| Formula | C16H18N4O3 |
| Molar Mass | 314.34 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Kuriyama K, et al. Antiallergic effects of 4-[2-oxo-3-(1H-tetrazol-5-yl)-2H-chromen-8-yloxy]-bu tyric acid. Jpn J Pharmacol. 1989 Jun;50(2):111-8. |