| 名稱 | JNJ-39758979 |
| 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. |
| 體外活性 | 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]. |
| 體內(nèi)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]. |
| 存儲(chǔ)條件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Shipping with blue ice/Shipping at ambient temperature. |
| 溶解度 | 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 3.3 mg/mL (14.91 mM), Sonication is recommended.
DMSO : 55 mg/mL (248.53 mM), Sonication is recommended.
|
| 關(guān)鍵字 | toxicity | selective | Rat H4 receptor | oral | Mouse H4 Receptor | Monkey H4 receptor | JNJ-39758979 | JNJ39758979 | JNJ 39758979 | Inhibitor | inhibit | Human H4 Receptor | HistamineReceptor | Histamine Receptor | histamine | H4 receptor | Guinea pig H4 receptor | cAMP | antipruritic | anti-inflammatory | agranulocytosis |
| 相關(guān)產(chǎn)品 | Famotidine | Meclizine dihydrochloride | Nizatidine | Lidocaine | Betahistine mesylate | Alginic acid | Sodium butanoate | Mianserin hydrochloride | Trazodone hydrochloride | Undecane | Doxepin hydrochloride | Histamine dihydrochloride |
| 相關(guān)庫 | 抑制劑庫 | 經(jīng)典已知活性庫 | 已知活性化合物庫 | 臨床失敗化合物庫 | 抗衰老化合物庫 | GPCR靶點(diǎn)分子庫 | 免疫/炎癥分子化合物庫 | 膜蛋白靶向化合物庫 | 神經(jīng)退行性疾病化合物庫 | 疼痛相關(guān)化合物庫 | 抗癌臨床化合物庫 | 抗癌藥物庫 |