JNJ-10191584

    WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 525297

CAS#: 73903-17-0

Description: JNJ-10191584 is a drug which acts as a potent and selective antagonist at the histamine H4 receptor. It has antiinflammatory and analgesic effects in animal studies of acute inflammation.


Price and Availability

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JNJ-10191584 is not in stock, but may be available through custom synthesis. For cost-effective reason, minimum 1 gram order is requested. The product will be characterized by NMR, HPLC and MS analysis. Purity (HPLC) is usually >98%. CoA, QC data, MSDS will be provided when product is successfully made. The estimated lead time is 2-3 months. Please send email to sales@medkoo.com to inquire quote.


Chemical Structure

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Theoretical Analysis

MedKoo Cat#: 525297
Name: JNJ-10191584
CAS#: 73903-17-0
Chemical Formula: C13H15ClN4O
Exact Mass: 278.09344
Molecular Weight: 278.74
Elemental Analysis: C, 56.02; H, 5.42; Cl, 12.72; N, 20.10; O, 5.74


Synonym: JNJ-10191584; JNJ10191584; JNJ 10191584; VUF-6002.

IUPAC/Chemical Name: (5-Chloro-1H-benzimidazol-2-yl)(4-methylpiperazin-1-yl)methanone

InChi Key: MOIWSUQWIOVGRH-UHFFFAOYSA-N

InChi Code: InChI=1S/C13H15ClN4O/c1-17-4-6-18(7-5-17)13(19)12-15-10-3-2-9(14)8-11(10)16-12/h2-3,8H,4-7H2,1H3,(H,15,16)

SMILES Code: O=C(C1=NC2=CC(Cl)=CC=C2N1)N3CCN(C)CC3


Technical Data

Appearance:
Solid powder

Purity:
>98% (or refer to the Certificate of Analysis)

Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition:
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility:
Soluble in DMSO

Shelf Life:
>2 years if stored properly

Drug Formulation:
This drug may be formulated in DMSO

Stock Solution Storage:
0 - 4 C for short term (days to weeks), or -20 C for long term (months).

Harmonized System Code:
293490


References

1: Jochem J, Altinbas B, Yalcin M, Ottani A, Giuliani D, Savci V, Kasperska-Zajac A, Guarini S. Involvement of the histaminergic system in the resuscitating effect of centrally acting leptin in haemorrhagic shock in rats. J Physiol Pharmacol. 2016 Feb;67(1):67-74. PubMed PMID: 27010896.

2: Sanna MD, Stark H, Lucarini L, Ghelardini C, Masini E, Galeotti N. Histamine H4 receptor activation alleviates neuropathic pain through differential regulation of ERK, JNK, and P38 MAPK phosphorylation. Pain. 2015 Dec;156(12):2492-504. doi: 10.1097/j.pain.0000000000000319. PubMed PMID: 26270581.

3: Nosáľ R, Jančinová V, Drábiková K, Perečko T. Molecular pharmacology of antihistamines in inhibition of oxidative burst of professional phagocytes. Gen Physiol Biophys. 2015 Apr;34(2):209-16. doi: 10.4149/gpb_2014040. Epub 2015 Mar 2. PubMed PMID: 25730898.

4: Kaneko H, Ye F, Ijima R, Kachi S, Kato S, Nagaya M, Higuchi A, Terasaki H. Histamine H4 receptor as a new therapeutic target for choroidal neovascularization in age-related macular degeneration. Br J Pharmacol. 2014 Aug;171(15):3754-63. doi: 10.1111/bph.12737. PubMed PMID: 24787705; PubMed Central PMCID: PMC4128071.

5: Vasicek O, Lojek A, Jancinova V, Nosal R, Ciz M. Role of histamine receptors in the effects of histamine on the production of reactive oxygen species by whole blood phagocytes. Life Sci. 2014 Mar 28;100(1):67-72. doi: 10.1016/j.lfs.2014.01.082. Epub 2014 Feb 12. PubMed PMID: 24530738.

6: Galeotti N, Sanna MD, Ghelardini C. Pleiotropic effect of histamine H4 receptor modulation in the central nervous system. Neuropharmacology. 2013 Aug;71:141-7. doi: 10.1016/j.neuropharm.2013.03.026. Epub 2013 Apr 11. PubMed PMID: 23583928.

7: Desmadryl G, Gaboyard-Niay S, Brugeaud A, Travo C, Broussy A, Saleur A, Dyhrfjeld-Johnsen J, Wersinger E, Chabbert C. Histamine H4 receptor antagonists as potent modulators of mammalian vestibular primary neuron excitability. Br J Pharmacol. 2012 Oct;167(4):905-16. doi: 10.1111/j.1476-5381.2012.02049.x. PubMed PMID: 22624822; PubMed Central PMCID: PMC3575788.

8: Connelly WM, Shenton FC, Lethbridge N, Leurs R, Waldvogel HJ, Faull RL, Lees G, Chazot PL. The histamine H4 receptor is functionally expressed on neurons in the mammalian CNS. Br J Pharmacol. 2009 May;157(1):55-63. doi: 10.1111/j.1476-5381.2009.00227.x. PubMed PMID: 19413571; PubMed Central PMCID: PMC2697783.

9: Michel I, Borck H, McElligott S, Krieg C, Diel F. Histamine receptor H4R-selective ligands influence the STAT6 Transcription Activation Domain (TAD) and the DNA-binding. Inflamm Res. 2008;57 Suppl 1:S47-8. doi: 10.1007/s00011-007-0623-1. PubMed PMID: 18345495.

10: Zhang M, Thurmond RL, Dunford PJ. The histamine H(4) receptor: a novel modulator of inflammatory and immune disorders. Pharmacol Ther. 2007 Mar;113(3):594-606. Epub 2006 Dec 28. Review. PubMed PMID: 17275092.

11: Dunford PJ, O'Donnell N, Riley JP, Williams KN, Karlsson L, Thurmond RL. The histamine H4 receptor mediates allergic airway inflammation by regulating the activation of CD4+ T cells. J Immunol. 2006 Jun 1;176(11):7062-70. PubMed PMID: 16709868.

12: Varga C, Horvath K, Berko A, Thurmond RL, Dunford PJ, Whittle BJ. Inhibitory effects of histamine H4 receptor antagonists on experimental colitis in the rat. Eur J Pharmacol. 2005 Oct 17;522(1-3):130-8. Epub 2005 Oct 6. PubMed PMID: 16213481.