您好,欢迎来到化工原料网! [登录] [免费注册]
化工原料网
位置:首页 > 产品库 > JNJ-39758979 dihydrochloride
立即咨询
咨询类型:
     
*姓名:
*电话:
*单位:
Email:
*留言内容:
请详细说明您的需求。
*验证码:
 
JNJ-39758979 dihydrochloride
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
JNJ-39758979 dihydrochloride图片
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品介绍
JNJ-39758979 dihydrochloride 是一种选择性的、具有口服活性的、高亲和力的组胺 H4受体 (histamine H4receptor) 拮抗剂,对人,小鼠,猴子的组胺 H4受体的Ki值分别为12.5、5.3 和 25 nM。JNJ-39758979 dihydrochloride 对组胺诱导的 cAMP 抑制作用具有拮抗作用,pA2 为 7.9。JNJ-39758979 dihydrochloride 具有良好的抗炎、止痒作用。
生物活性

JNJ-39758979 dihydrochloride is a selective, orally active, and high-affinityhistamineH4receptorantagonist, withKis of 12.5, 5.3, and 25 nM for human, mouse, and monkey histamineH4receptor, respectively. JNJ-39758979 dihydrochloride functionally antagonizes histamine-induced cAMP inhibition with a pA2 of 7.9 in transfected cells. JNJ-39758979 dihydrochloride shows good anti-inflammatory and antipruritic activity[1][2].

IC50& Target[1]

Human H4Receptor

12.5 nM (Ki)

Mouse H4Receptor

5.3 nM (Ki)

Monkey H4receptor

25 nM (Ki)

Rat H4receptor

188 nM (Ki)

Guinea pig H4receptor

306 nM (Ki)

体外研究
(In Vitro)

JNJ-39758979 dihydrochloride is a selective, high-affinity histamine H4receptor antagonist with a Kiof 12.5 nM versus the human H4receptor and functionally antagonizes histamine-induced cAMP inhibition with a pA2 of 7.9 in transfected cells. At the mouse H4R, the Ki=5.3 nM and the pA2=8.3. At the monkey H4R, the Ki=25 nM and the pA2=7.5. The affinity for the rat (Ki=188 nM, pA2 = 7.2) and guinea pig H4R (Ki=306 nM) is moderate, and JNJ-39758979 dihydrochloride has little if any affinity for the dog H4R (Ki≥10 μM). The compound is highly selective for H4R, as it exhibits low affinity for the H1, H2, and H3receptors[1].
JNJ-39758979 dihydrochloride is metabolically stable (t1/2>120 min) when incubatedin vitrowith human, rat, dog, or monkey liver microsomes[1].

体内研究
(In Vivo)

JNJ-39758979 dihydrochloride (10 mg/kg; p.o.) treatment shows that the Cmax, t1/2and F values are 0.3 μM, 7.5 hours, 36%, respectively[1].
JNJ-39758979 dihydrochloride (2 mg/kg; i.v.) treatment shows that the Vss, AUC, CL and t1/2were 19.9 L/kg, 1.4 μM*h, 2.2 L/h, and 2.1 hours, respectively[1].

Animal Model:Sprague-Dawley rats[1]
Dosage:10 mg/kg
Administration:Oral administration (Pharmacokinetic Analysis)
Result:The Cmax, t1/2and F values were 0.3 μM, 7.5 hours, and 36%, respectively.
分子量

294.22

Formula

C11H21Cl2N5

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.