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Submit ReviewJNJ 39758979 dihydrochloride is a high affinity and selective histamine H4 antagonist (Ki = 12.5 nM). Exhibits >80-fold selectivity for H4 over other histamine receptors and no significant activity at a range of other targets. Inhibits histamine-induced eosinophil shape change in whole blood in vitro and ovalbumin-induced inflammation in ovalbumin-sensitized mice in vivo. Orally bioavailable.
Sold with the permission of Janssen Pharmaceutica N.V.
JNJ 39758979 dihydrochloride is also offered as part of the Tocriscreen 2.0 Max. 了解 Tocris 化合物库的更多信息。
分子量 | 294.22 |
公式 | C11H19N5.2HCl |
储存 | Desiccate at RT |
纯度 | ≥98% (HPLC) |
PubChem ID | 129628806 |
InChI Key | KXPWYAVIFCXPRW-YCBDHFTFSA-N |
Smiles | CC(C1=CC(N2CC[C@H](C2)N)=NC(N)=N1)C.Cl.Cl |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
water | 22.13 | 100 | |
DMSO | 22.13 | 100 |
以下数据基于产品分子量 294.22。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 3.4 mL | 16.99 mL | 33.99 mL |
5 mM | 0.68 mL | 3.4 mL | 6.8 mL |
10 mM | 0.34 mL | 1.7 mL | 3.4 mL |
50 mM | 0.07 mL | 0.34 mL | 0.68 mL |
参考文献是支持产品生物活性的出版物。
Thurmond et al (2014) Clinical and preclinical characterization of the histamine H4 receptor antagonist JNJ-39758979. J.Pharmacol.Exp.Ther. 349 176 PMID: 24549371
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关键词: JNJ 39758979 dihydrochloride, JNJ 39758979 dihydrochloride supplier, JNJ39758979, 2HCl, 1046447-90-8, high, affinity, selective, histamine, H4, antagonists, antagonism, anti-inflammatory, orally, bioavailable, Histamine, Receptors, 6279, Tocris Bioscience
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