Powder: -20°C for 3 years | In solvent: -80°C for 1 year
JNJ-39758979是一种选择性的、高亲和力的、可口服的组胺 H4 受体拮抗剂,具有抗炎和止痒作用,对人、小鼠和猴子的组胺 H4 受体的 Ki 值分别为 12.5、5.3 和 25 nM。它对组胺诱导的 cAMP 抑制作用具有拮抗作用,pA2 为 7.9。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 738 | 现货 | ||
5 mg | ¥ 1,980 | 现货 | ||
10 mg | ¥ 3,230 | 现货 | ||
25 mg | ¥ 5,390 | 现货 | ||
50 mg | ¥ 7,580 | 现货 | ||
100 mg | ¥ 9,870 | 现货 | ||
500 mg | ¥ 19,800 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 2,220 | 现货 |
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 | H4 receptor:12.5 nM (ki)(in human), H4 receptor:188 nM (ki)(in rat), H4 receptor:25 nM (ki)(in Monkey), H4 receptor:306 nM (ki)(in Guinea pig), H4 receptor:5.3 nM (ki)(in mouse) |
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]. |
分子量 | 221.3 |
分子式 | C11H19N5 |
CAS No. | 1046447-90-8 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 30 mg/mL (135.56 mM), Sonication is recommended.
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 4.5188 mL | 22.5938 mL | 45.1875 mL | 112.9688 mL |
5 mM | 0.9038 mL | 4.5188 mL | 9.0375 mL | 22.5938 mL | |
10 mM | 0.4519 mL | 2.2594 mL | 4.5188 mL | 11.2969 mL | |
20 mM | 0.2259 mL | 1.1297 mL | 2.2594 mL | 5.6484 mL | |
50 mM | 0.0904 mL | 0.4519 mL | 0.9038 mL | 2.2594 mL | |
100 mM | 0.0452 mL | 0.2259 mL | 0.4519 mL | 1.1297 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
JNJ-39758979 1046447-90-8 GPCR/G Protein Immunology/Inflammation Neuroscience Histamine Receptor agranulocytosis histamine selective toxicity cAMP inhibit oral anti-inflammatory Inhibitor antipruritic JNJ 39758979 JNJ39758979 inhibitor