JNJ-39758979
目录号 : GC30821JNJ-39758979是一个有选择性且具有高亲和性的组胺H4受体拮抗剂,其Ki值为12.5nM。
Cas No.:1046447-90-8
Sample solution is provided at 25 µL, 10mM.
JNJ-39758979 is a selective, high-affinity histamine H4 receptor antagonist with a Ki of 12.5 nM.
JNJ-39758979 is a selective, high-affinity histamine H4 receptor antagonist with a Ki of 12.5 nM. The affinity of JNJ-39758979 for the rat (Ki=188 nM) and guinea pig H4R (Ki=306 nM) is moderate, and JNJ-39758979 has little if any affinity for the dog H4R (Ki≥10 μM). JNJ-39758979 is metabolically stable (t1/2 >120 min) when incubated in vitro with human, rat, dog, or monkey liver microsomes[1].
JNJ-39758979 shows dose-proportional pharmacokinetic (PK) in rat in the range of 2 to 500 mpK. JNJ-39758979 rapidly reaches the kidneys and liver (mean tmax=2.0 h). The elimination of JNJ-39758979 is slow from the brain, liver, and kidneys, with mean t1/2 values of 42.5, 22.3, and 20.5 h, respectively. The highest exposure (based on Cmax and AUC0-inf values) is observed in the liver followed by the kidney and brain. Tissue-to-plasma ratios for liver and kidney range from 23.2 to 95.8; the tissue-to-plasma ratios in brain increases with time from 0.256 to 22.7 up to 48 h after dosing. JNJ-39758979 is able to inhibit histamine-induced itch at doses of 5 and 20 mg/kg in mice. JNJ-39758979 exhibits dose-dependent inhibition of the clinical score in a mouse collagen-induced arthritis model[1].
[1]. Savall BM, et al. Discovery and SAR of 6-alkyl-2,4-diaminopyrimidines as histamine H? receptor antagonists. J Med Chem. 2014 Mar 27;57(6):2429-39.
Animal experiment: | The model of histamine-induced scratching in C57/bl6 mice (n=6 to 8 per group) is used to judge the antipruritic effects of JNJ-39758979. JNJ-39758979 is given p.o. in 20% hydroxypropyl-β-cyclodextran 30 min before an intradermal injection of histamine (100 μg). Bouts of scratching are calculated using an automated system. Immediately after histamine injection, mice are placed in containers above a solenoid, and magnets previously placed on the mouse ear generate scratch-specific signals that are counted over a 20 min time span[1]. |
References: [1]. Savall BM, et al. Discovery and SAR of 6-alkyl-2,4-diaminopyrimidines as histamine H receptor antagonists. J Med Chem. 2014 Mar 27;57(6):2429-39. |
Cas No. | 1046447-90-8 | SDF | |
Canonical SMILES | NC1=NC(C(C)C)=CC(N2C[C@H](N)CC2)=N1 | ||
分子式 | C11H19N5 | 分子量 | 221.3 |
溶解度 | DMSO : 33.33 mg/mL (150.61 mM) | 储存条件 | 4°C, protect from light |
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Shipping Condition | 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。 |
制备储备液 | |||
1 mg | 5 mg | 10 mg | |
1 mM | 4.5188 mL | 22.5938 mL | 45.1875 mL |
5 mM | 0.9038 mL | 4.5188 mL | 9.0375 mL |
10 mM | 0.4519 mL | 2.2594 mL | 4.5188 mL |
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2.
一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。
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- Purity: >98.00%
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