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MedKoo Cat#: 525297 | Name: JNJ-10191584
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Description:

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

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. JNJ-10191584 binds with high affinity to the human H4 receptor (Ki = 26 nM). > 540-fold selective over the H3 receptor (Ki = 14.1 μM).

Chemical Structure

JNJ-10191584
JNJ-10191584
CAS#73903-17-0 (free base)

Theoretical Analysis

MedKoo Cat#: 525297

Name: JNJ-10191584

CAS#: 73903-17-0 (free base)

Chemical Formula: C13H15ClN4O

Exact Mass: 278.0934

Molecular Weight: 278.74

Elemental Analysis: C, 56.02; H, 5.42; Cl, 12.72; N, 20.10; O, 5.74

Price and Availability

Size Price Availability Quantity
25mg USD 550.00 2 Weeks
50mg USD 950.00 2 Weeks
100mg USD 1,650.00 2 Weeks
200mg USD 2,950.00 2 Weeks
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Related CAS #
73903-17-0 (free base) 869497-75-6 (maleate)
Synonym
VUF6002; VUF 6002; VUF-6002; JNJ-10191584; JNJ 10191584; JNJ10191584;
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
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).
HS Tariff Code
2934.99.9001
More Info

Preparing Stock Solutions

The following data is based on the product molecular weight 278.74 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.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
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.

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