首页 GPCR/G Protein Histamine Receptor JNJ-39758979
JNJ-39758979
编号 T11723L    
CAS 1046447-90-8     分子式 C11H19N5     分子量 221.3
靶点: Human H4 Receptor; Mouse H4 Receptor; Monkey H4 receptor; Rat H4 receptor; Guinea pig H4 receptor;
JNJ-39758979 is a selective and high-affinity histamine H4 receptor antagonist (Kis: 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.
选择批次  
纯度 98.00%
规格 库存 单价 数量
1 mg 待询 970.00
5 mg 待询 2840.00
10 mg 待询 4285.00
50 mg 待询 12785.00
100 mg 待询 17885.00
200 mg 待询 待询
500 mg 待询 待询
1 mL * 10 mM (in DMSO) 待询 2310.00
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生物活性

产品描述

JNJ-39758979 is a selective and high-affinity histamine H4 receptor antagonist (Kis: 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.

靶点活性

Human H4 Receptor,12.5 nM (ki)

Mouse H4 Receptor,5.3 nM (ki)

Monkey H4 receptor,25 nM (ki)

Rat H4 receptor,188 nM (ki)

Guinea pig H4 receptor,306 nM (ki)

体外活性

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 and high-affinity histamine H4 receptor antagonist (Ki: 12.5 nM versus the human H4 receptor). In transfected cells, functionally antagonizes histamine-induced cAMP inhibition ( pA2: 7.9). 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 [1].

体内活性

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. JNJ-39758979 (10 mg/kg; p.o.) treatment displays that the Cmax, t1/2, and F values are 0.3 μM, 7.5 hours, and 36%, respectively [1].

化学信息

分子量

221.3

分子式

C11H19N5

CAS

1046447-90-8

溶解度

DMSO: 33.33 mg/mL (150.61 mM), Need ultrasonic

( < 1 mg/ml refers to the product slightly soluble or insoluble )

储存条件

store at -80°C

备注

For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

配制溶液

1 mg 5 mg 10 mg
1 mM 4.519 ml 22.594 ml 45.188 ml
5 mM 0.904 ml 4.519 ml 9.038 ml
10 mM 0.452 ml 2.259 ml 4.519 ml
50 mM 0.09 ml 0.452 ml 0.904 ml
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