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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。
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 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 662 | 现货 | |
5 mg | ¥ 1,650 | 现货 | |
10 mg | ¥ 2,650 | 现货 | |
25 mg | ¥ 4,480 | 现货 | |
50 mg | ¥ 6,490 | 现货 | |
100 mg | ¥ 8,770 | 现货 | |
500 mg | ¥ 17,500 | 现货 | |
1 mL x 10 mM (in DMSO) | ¥ 1,820 | 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 |
Smiles | CC(C)c1cc(nc(N)n1)N1CC[C@@H](N)C1 |
密度 | no data available |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
溶解度信息 | DMSO: 55 mg/mL (248.53 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
溶液配制表 | ||||||||||||||||||||||||||||||||||||
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