KP136

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

KP136 (AL136) 是一种有效的，具有口服活性的抗过敏剂。抑制组胺释放和细胞脱粒，IC50 分别为 76.1 μg/mL 和 63 μg/mL。

KP136 (AL136) 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.

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.

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GPCR/G Protein

Histamine Receptor

Histamine Receptor

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76239-32-2

314.34

C16H18N4O3

>98% (HPLC)

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O=C1OC=2C(OCCCCCC)=CC=CC2C=C1C3=NN=NN3

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(-20℃)

With Ice Pack

≥ 2 years