产品
编 号：F019801
分子式：C11H19N5
分子量：221.3
分子式：C11H19N5
分子量：221.3
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
3200
In-stock
1mg
1100
In-stock
5mg
2970
In-stock
10mg
4850
In-stock
结构图
CAS No: 1046447-90-8
产品详情
生物活性：
JNJ-39758979 is a selective, orally active, and high-affinity histamine H4 receptor antagonist with Kis of 12.5, 5.3, and 25 nM for human, mouse, and monkey histamine H4 receptor, respectively. JNJ-39758979 functionally antagonizes histamine-induced cAMP inhibition with a pA2 of 7.9 in transfected cells. JNJ-39758979 shows good anti-inflammatory and antipruritic activity.
体内研究：
JNJ-39758979 (10 mg/kg; p.o.) treatment shows that the Cmax, t1/2 and F values are 0.3 μM, 7.5 hours, and 36%, respectively.JNJ-39758979 (2 mg/kg; i.v.) treatment shows that the Vss, AUC, CL and t1/2 were 19.9 L/kg, 1.4 μM*h, 2.2 L/h, and 2.1 hours, respectively .Animal Model:Sprague-Dawley rats
Dosage:10 mg/kg
Administration:Oral administration (Pharmacokinetic Analysis)
Result:The Cmax, t1/2 and F values were 0.3 μM, 7.5 hours, and 36%, respectively.
体外研究：
JNJ 39758979 is a selective, high-affinity histamine H4 receptor antagonist with a Ki of 12.5 nM versus the human H4 receptor 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 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 H3 receptors.JNJ-39758979 is metabolically stable (t1/2 >120 min) when incubated in vitro with human, rat, dog, or monkey liver microsomes.
JNJ-39758979 is a selective, orally active, and high-affinity histamine H4 receptor antagonist with Kis of 12.5, 5.3, and 25 nM for human, mouse, and monkey histamine H4 receptor, respectively. JNJ-39758979 functionally antagonizes histamine-induced cAMP inhibition with a pA2 of 7.9 in transfected cells. JNJ-39758979 shows good anti-inflammatory and antipruritic activity.
体内研究：
JNJ-39758979 (10 mg/kg; p.o.) treatment shows that the Cmax, t1/2 and F values are 0.3 μM, 7.5 hours, and 36%, respectively.JNJ-39758979 (2 mg/kg; i.v.) treatment shows that the Vss, AUC, CL and t1/2 were 19.9 L/kg, 1.4 μM*h, 2.2 L/h, and 2.1 hours, respectively .Animal Model:Sprague-Dawley rats
Dosage:10 mg/kg
Administration:Oral administration (Pharmacokinetic Analysis)
Result:The Cmax, t1/2 and F values were 0.3 μM, 7.5 hours, and 36%, respectively.
体外研究：
JNJ 39758979 is a selective, high-affinity histamine H4 receptor antagonist with a Ki of 12.5 nM versus the human H4 receptor 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 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 H3 receptors.JNJ-39758979 is metabolically stable (t1/2 >120 min) when incubated in vitro with human, rat, dog, or monkey liver microsomes.
产品资料
Copyright©2015-2024 沪ICP备2022026524号-1
沪公网安备