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MedKoo Cat#: 565275 | Name: JNJ-10191584 Maleate
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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 Maleate
JNJ-10191584 Maleate
CAS#869497-75-6 (maleate)

Theoretical Analysis

MedKoo Cat#: 565275

Name: JNJ-10191584 Maleate

CAS#: 869497-75-6 (maleate)

Chemical Formula: C17H19ClN4O5

Exact Mass:

Molecular Weight: 394.81

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 550.00 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; 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/
Solvent mg/mL mM
Solubility
DMSO 19.7 50.00
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

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.

View History

RP-101075

RP-101075