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Psora 4

现货
Catalog No.
B7659
Kv1.3阻断剂
组合的产品项目
规格价格库存 数量
10mM (in 1mL DMSO)
¥ 1,800.00
现货
10mg
¥ 1,580.00
现货
50mg
¥ 6,430.00
现货

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Background

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

Reference:
[1] Vennekamp J,Wulff H,Beeton C,Calabresi PA,Grissmer S,Hnsel W,Chandy KG.  Kv1.3-blocking 5-phenylalkoxypsoralens: a new class of immunomodulators. Mol Pharmacol.2004 Jun;65(6):1364-74.

文献引用

1. Admasu TD, Chaithanya Batchu K, et al. "Drug Synergy Slows Aging and Improves Healthspan through IGF and SREBP Lipid Signaling." Dev Cell. 2018 Oct 8;47(1):67-79.e5. PMID:30269951

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt334.37
Cas No.724709-68-6
FormulaC21H18O4
Solubility≥15.75mg/mL in DMSO
Chemical Name4-(4-phenylbutoxy)-7H-furo[3,2-g]chromen-7-one
SDFDownload SDF
Canonical SMILESO=C1OC2=C(C=C1)C(OCCCCC3=CC=CC=C3)=C4C(OC=C4)=C2
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

试验操作

细胞实验[1]:

细胞系

人和大鼠TEM细胞

溶解方法

在DMSO中的溶解度>15.75mg/mL。为了获得更高的浓度,可以将离心管在37℃加热10分钟和/或在超声波浴中震荡一段时间。原液可以在-20℃以下储存几个月。

反应条件

0-1000 nM; 30 min

应用

Psora-4优先抑制人和大鼠TEM细胞的增殖,EC50值分别为25和60nM。

动物实验[2]:

动物模型

抗肾小球基底膜肾小球肾炎(抗GBM GN)大鼠

剂量

0.3 ml,溶于25%CremophorEL和75%PBS的混合物中以制备9mg / ml的浓度,从第0天到第21天,腹腔注射

应用

在抗肾小球基底膜肾小球肾炎(抗GBM GN)的大鼠中,Psora 4显著降低尿蛋白排泄,肾脏重量增加明显小于载体组。 Psora4恢复了肌酐清除率,减少新月体肾小球的比例,以及ED-1 +巨噬细胞和CD3 + T细胞的数量。

注意事项

请测试所有化合物在室内的溶解度,实际溶解度和理论值可能略有不同,这是由实验系统的误差引起的,属于正常现象。

References:

[1] Vennekamp J,Wulff H,Beeton C,Calabresi PA,Grissmer S,Hnsel W,Chandy KG. Kv1.3-blocking 5-phenylalkoxypsoralens: a new class of immunomodulators. Mol Pharmacol.2004 Jun;65(6):1364-74.

[2]. Hyodo T1, Oda T, Kikuchi Y, et al. Voltage-gated potassium channel Kv1.3 blocker as a potential treatment for rat anti-glomerular basement membrane glomerulonephritis. Am J Physiol Renal Physiol. 2010 Dec;299(6):F1258-69.

质量控制

化学结构

Psora 4

相关生物数据

Psora 4