JNJ-10191584
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MedKoo CAT#: 525297

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

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. 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

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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: 278.09344
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
25.0mg USD 550.0 2 Weeks
50.0mg USD 950.0 2 Weeks
100.0mg USD 1650.0 2 Weeks
200.0mg USD 2950.0 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

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

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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.

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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.

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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.