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Psora-4_分子结构_CAS_724709-68-6)
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Psora-4

产品号 P9872 公司名称 Sigma Aldrich
CAS号 724709-68-6 公司网站 http://www.sigmaaldrich.com
分子式 C21H18O4 电 话 1-800-521-8956
分子量 334.36522 传 真
纯 度 ≥98% (HPLC) 电子邮件
保 存 protect from light Chembase数据库ID: 155006

产品价格信息

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产品别名

标题
Psora-4
IUPAC标准名
4-(4-phenylbutoxy)-7H-furo[3,2-g]chromen-7-one
IUPAC传统名
4-(4-phenylbutoxy)furo[3,2-g]chromen-7-one
别名
5-(4-Phenylbutoxy)psoralen

产品登记号

CAS号 724709-68-6
PubChem SID 24278012

产品性质

Empirical Formula (Hill Notation) C21H18O4
纯度 ≥98% (HPLC)
外观 off-white solid
溶解度 DMSO: ~16 mg/mL
溶解度 H2O: insoluble
GHS危险品标识 GHS07
GHS警示词 Warning
GHS危险声明 H315-H319-H335-H413
欧盟危险性物质标志 刺激性(Irritant) 刺激性(Irritant) (Xi)
MSDS下载 下载链接
个人保护装置 dust mask type N95 (US), Eyeshields, Gloves
GHS警示性声明 P261-P305 + P351 + P338
危险公开号 36/37/38
安全公开号 26-36
保存条件 protect from light
保存条件 under inert gas
保存温度 2-8°C
德国WGK号 3

产品详细信息

详细说明 (English)
Biochem/physiol Actions
The lymphocyte potassium channel Kv1.3 is regarded as a new target for immunosuppression. Psora-4 is the most potent small-molecule Kv1.3 blocker known. It blocked Kv1.3 in a use-dependent manner, with a Hill coefficient of 2 and an EC50 value of 3 nM, by preferentially binding to the C-type inactivated state of the channel. It exhibited 17- to 70-fold selectivity for Kv1.3 over closely related Kv1-family channels (Kv1.1, Kv1.2, Kv1.4, and Kv1.7) with the exception of Kv1.5 (EC50, 7.7 nM) and showed no effect on human ether-a-go-go-related channel, Kv3.1, the calcium-activated K+ channels (IKCa1, SK1-SK3, and BKCa), or the neuronal NaV1.2 channel. In a test of in vivo toxicity in rats, Psora-4 did not display any signs of acute toxicity after five daily subcutaneous injections at 33 mg/kg body weight. Psora-4 selectively suppressed the proliferation of human and rat myelin-specific effector memory T cells with EC50 values of 25 and 60 nM, respectively, without persistently suppressing peripheral blood naive and central memory T cells. Because autoantigen-specific effector memory T cells contribute to the pathogenesis of T cell-mediated autoimmune diseases such as multiple sclerosis, Psora-4 and other Kv1.3 blockers may be useful as immunomodulators for the therapy of autoimmune disord.
详细说明 (简体中文)
Biochem/physiol Actions
The lymphocyte potassium channel Kv1.3 is regarded as a new target for immunosuppression. Psora-4 is the most potent small-molecule Kv1.3 blocker known. It blocked Kv1.3 in a use-dependent manner, with a Hill coefficient of 2 and an EC50 value of 3 nM, by preferentially binding to the C-type inactivated state of the channel. It exhibited 17- to 70-fold selectivity for Kv1.3 over closely related Kv1-family channels (Kv1.1, Kv1.2, Kv1.4, and Kv1.7) with the exception of Kv1.5 (EC50, 7.7 nM) and showed no effect on human ether-a-go-go-related channel, Kv3.1, the calcium-activated K+ channels (IKCa1, SK1-SK3, and BKCa), or the neuronal NaV1.2 channel. In a test of in vivo toxicity in rats, Psora-4 did not display any signs of acute toxicity after five daily subcutaneous injections at 33 mg/kg body weight. Psora-4 selectively suppressed the proliferation of human and rat myelin-specific effector memory T cells with EC50 values of 25 and 60 nM, respectively, without persistently suppressing peripheral blood naive and central memory T cells. Because autoantigen-specific effector memory T cells contribute to the pathogenesis of T cell-mediated autoimmune diseases such as multiple sclerosis, Psora-4 and other Kv1.3 blockers may be useful as immunomodulators for the therapy of autoimmune disord.

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