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化學(xué)性質(zhì):
規(guī)格 | 10mM (in 1mL DMSO) 10mg 50mg |
CAS | 724709-68-6 |
別名 |
|
化學(xué)名 | 4-(4-phenylbutoxy)-7H-furo[3,2-g]chromen-7-one |
分子式 | C21H18O4 |
分子量 | 334.37 |
溶解度 | ≥ 15.75mg/mL in DMSO |
儲存條件 | Store at -20°C |
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
Shipping Condition | Evaluation sample solution : ship with blue ice |
產(chǎn)品描述:
EC50: 3 nM
Psora 4 is a Kv1.3 blocker.
The voltage-gated Kv1.3 channel and the Ca2+-activated IKCa1 channel has been reported to promote and sustain Ca2+ signaling in human T cells via providing the driving force for Ca2+ entry through voltage-independent Ca2+ channels. Selective blockade of Kv1.3 and/or IKCa1 leads to membrane depolarization, reduced Ca2+ entry, as well as diminished cytokine proliferation and production.
In vitro: Psora-4 could block Kv1.3 in a dose-dependent manner. Psora-4 was found to be the most potent small-molecule Kv1.3 blocker known. Psora-4 exhibited 17- to 70-fold selectivity for Kv1.3 over Kv1-family channels including Kv1.1, Kv1.2, Kv1.4, and Kv1.7 and also showed no effect on human ether-a-go-go-related channel, Kv3.1, or the neuronal NaV1.2 channel. In addition, Psora-4 could suppress the proliferation of rat and human myelin-specific effector memory T cells with EC50 values of 60 and 25 nM, respectively, without persistently suppressing the peripheral blood naive and central memory T cells [1].
In vivo: In a study of in vivo toxicity in rats, Psora-4 was found not to show any signs of acute toxicity following five daily subcutaneous injections at 33 mg/kg body weight [1].
Clinical trial: N/A
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原創(chuàng)作者:上海莼試生物技術(shù)有限公司
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