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Submit ReviewJNJ 39758979 dihydrochloride
Description: High affinity and selective histamine H4 antagonist; orally bioavailable
Chemical Name: 4-[(3R)-3-Amino-1-pyrrolidinyl]-6-(1-methylethyl)-2-pyridinamine dihydrochloride
Purity: ≥98% (HPLC)
Biological Activity for JNJ 39758979 dihydrochloride
JNJ 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.
Licensing Information
Sold with the permission of Janssen Pharmaceutica N.V.
Compound Libraries for JNJ 39758979 dihydrochloride
JNJ 39758979 dihydrochloride is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
Technical Data for JNJ 39758979 dihydrochloride
| M. Wt | 294.22 |
| Formula | C11H19N5.2HCl |
| Storage | Desiccate at RT |
| Purity | ≥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 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for JNJ 39758979 dihydrochloride
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| water | 22.13 | 100 | |
| DMSO | 22.13 | 100 |
Preparing Stock Solutions for JNJ 39758979 dihydrochloride
The following data is based on the product molecular weight 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.
| Concentration / Solvent Volume / Mass | 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 |
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Product Datasheets for JNJ 39758979 dihydrochloride
References for JNJ 39758979 dihydrochloride
References are publications that support the biological activity of the product.
Thurmond et al (2014) Clinical and preclinical characterization of the histamine H4 receptor antagonist JNJ-39758979. J.Pharmacol.Exp.Ther. 349 176 PMID: 24549371
If you know of a relevant reference for JNJ 39758979 dihydrochloride, please let us know.
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Keywords: 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
Citations for JNJ 39758979 dihydrochloride
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Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
Histamine Receptors Scientific Review
Written by Iwan de Esch and Rob Leurs, this review provides a synopsis of the different histamine receptor subtypes and the ligands that act upon them; compounds available from Tocris are listed.