JNJ-10191584 Maleate
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    WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 565275

CAS#: 869497-75-6 (maleate)

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 Maleate
CAS# 869497-75-6 (maleate)
Product data Instruction

Theoretical Analysis

MedKoo Cat#: 565275
Name: JNJ-10191584 Maleate
CAS#: 869497-75-6 (maleate)
Chemical Formula: C17H19ClN4O5
Exact Mass: 0.00
Molecular Weight: 394.812
Elemental Analysis: C, 51.72; H, 4.85; Cl, 8.98; N, 14.19; O, 20.26

Price and Availability

Size Price Availability Quantity
25mg USD 550 2 Weeks
50mg USD 950 2 Weeks
100mg USD 1650 2 Weeks
200mg USD 2950 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; JNJ-10191584 maleate

IUPAC/Chemical Name: (6-Chloro-1H-benzimidazol-2-yl)-(4-methylpiperazin-1-yl)methanone Maleate

InChi Key: KOTJFAYEELTYCZ-BTJKTKAUSA-N

InChi Code: InChI=1S/C13H15ClN4O.C4H4O4/c1-17-4-6-18(7-5-17)13(19)12-15-10-3-2-9(14)8-11(10)16-12;5-3(6)1-2-4(7)8/h2-3,8H,4-7H2,1H3,(H,15,16);1-2H,(H,5,6)(H,7,8)/b;2-1-

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

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: >3 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:

Product Data:
Product Data
Instruction:
View handling instruction
Biological target: JNJ-10191584 maleate is a highly selective histamine H4 receptor silent antagonist.
In vitro activity: Application of betahistine inhibited the evoked action potential firing starting at micromolar range, accompanied by subsequent strong neuronal depolarization at higher concentrations. Conversely, reversible inhibitory effects elicited by JNJ 10191584 and JNJ 7777120 began in the nanomolar range, without inducing neuronal depolarization. Reference: Br J Pharmacol. 2012 Oct;167(4):905-16. https://pubmed.ncbi.nlm.nih.gov/22624822/
In vivo activity: The SNI mice showed an increased spinal expression of IL‐1ß in both the ipsilateral and contralateral side that was reduced by VUF 8430 (20 μg). Pretreatment with JNJ 10151984 antagonized the H4 receptor agonist‐induced antihyperalgesic effect (Figure 2C). Reference: Br J Pharmacol. 2017 Jan;174(1):28-40. https://pubmed.ncbi.nlm.nih.gov/27714773/

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 19.7 50.00

Preparing Stock Solutions

The following data is based on the product molecular weight 394.81 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
Formulation protocol: 1. 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. PMID: 22624822; PMCID: PMC3575788. 2. Sanna MD, Lucarini L, Durante M, Ghelardini C, Masini E, Galeotti N. Histamine H4 receptor agonist-induced relief from painful peripheral neuropathy is mediated by inhibition of spinal neuroinflammation and oxidative stress. Br J Pharmacol. 2017 Jan;174(1):28-40. doi: 10.1111/bph.13644. Epub 2016 Nov 18. PMID: 27714773; PMCID: PMC5341487. 3. 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. PMID: 24787705; PMCID: PMC4128071.
In vitro protocol: 1. 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. PMID: 22624822; PMCID: PMC3575788.
In vivo protocol: 1. Sanna MD, Lucarini L, Durante M, Ghelardini C, Masini E, Galeotti N. Histamine H4 receptor agonist-induced relief from painful peripheral neuropathy is mediated by inhibition of spinal neuroinflammation and oxidative stress. Br J Pharmacol. 2017 Jan;174(1):28-40. doi: 10.1111/bph.13644. Epub 2016 Nov 18. PMID: 27714773; PMCID: PMC5341487. 2. 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. PMID: 24787705; PMCID: PMC4128071.

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