JNJ-39758979 NEW
| Price | $68 | $163 | $263 |
| Package | 1mg | 5mg | 10mg |
| Min. Order: | |
| Supply Ability: | 10g |
| Update Time: | 2024-11-18 |
Product Details
| Product Name: JNJ-39758979 | CAS No.: 1046447-90-8 |
| Purity: 98.3% | Supply Ability: 10g |
| Release date: 2024/11/18 |
Product Introduction
Bioactivity
| 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]. |
| 存儲條件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| 溶解度 | DMSO : 55 mg/mL (248.53 mM), Sonication is recommended. |
| 關鍵字 | agranulocytosis | histamine | selective | toxicity | JNJ-39758979 | cAMP | inhibit | oral | Histamine Receptor | anti-inflammatory | Inhibitor | antipruritic | JNJ 39758979 | JNJ39758979 |
| 相關產(chǎn)品 | Chlorphenesin | Meclizine dihydrochloride | Mirtazapine | Lidocaine | Famotidine | Mebhydrolin napadisylate | Sodium butanoate | Amitriptyline hydrochloride | Nizatidine | Alginic acid | Trazodone hydrochloride | Mianserin hydrochloride |
| 相關庫 | 經(jīng)典已知活性庫 | 疼痛相關化合物庫 | 神經(jīng)退行性疾病化合物庫 | 膜蛋白靶向化合物庫 | 抗癌臨床化合物庫 | 藥物功能重定位化合物庫 | 抑制劑庫 | 抗衰老化合物庫 | 已知活性化合物庫 | 抗癌藥物庫 |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
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United States- Since: 2011-01-07
- Address: 36?Washington?Street, Wellesley?Hills
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