KP136是一种口服有效的抗过敏剂。抑制组胺释放和细胞脱粒，IC50分别为76.1μg/mL和63μg/mL。
CAS：76239-32-2
分子式：C16H18N4O3
分子量：314.34
纯度：98%
存储：Store at -20°C

Background:

KP136 is an orally effective antiallergic agent. The IC50 is 76.1 μg/mL for histamine release and 63 ug/mL for degranulation.

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].

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].

[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.