JNJ-47965567 | CAS#1428327-31-4

MedKoo Cat#: 531988 | Name: JNJ-47965567

Description:

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

JNJ-47965567 is a selective antagonist of the purinergic receptor P2X subtype 7 (P2X7), a ligand-gated ion channel.

Chemical Structure

JNJ-47965567

CAS#1428327-31-4

Theoretical Analysis

MedKoo Cat#: 531988

Name: JNJ-47965567

CAS#: 1428327-31-4

Chemical Formula: C28H32N4O2S

Exact Mass: 488.2246

Molecular Weight: 488.65

Elemental Analysis: C, 68.82; H, 6.60; N, 11.47; O, 6.55; S, 6.56

Price and Availability

Size	Price	Availability
50mg	USD 450.00	2 Weeks
100mg	USD 750.00	2 Weeks
200mg	USD 1,250.00	2 Weeks
500mg	USD 2,050.00	2 Weeks
1g	USD 2,950.00	2 Weeks
2g	USD 5,250.00	2 Weeks

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Synonym

JNJ-47965567; JNJ 47965567; JNJ47965567.

IUPAC/Chemical Name

N-[[4-(4-phenylpiperazin-1-yl)oxan-4-yl]methyl]-2-phenylsulfanylpyridine-3-carboxamide

InChi Key

XREFXUCWSYMIOG-UHFFFAOYSA-N

InChi Code

InChI=1S/C28H32N4O2S/c33-26(25-12-7-15-29-27(25)35-24-10-5-2-6-11-24)30-22-28(13-20-34-21-14-28)32-18-16-31(17-19-32)23-8-3-1-4-9-23/h1-12,15H,13-14,16-22H2,(H,30,33)

SMILES Code

O=C(C1=CC=CN=C1SC2=CC=CC=C2)NCC3(N4CCN(C5=CC=CC=C5)CC4)CCOCC3

Appearance

Solid powder

Purity

>97% (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

Product Data

Product Data

Instruction

View handling instruction

Biological target:

JNJ-47965567 is a centrally permeable, high-affinity, selective P2X7 antagonist, with pKis of 7.9 and 8.7 for human and rat P2X7, respectively.

In vitro activity:

JNJ-47965567 is a potent P2X7 antagonist across all species tested. These results demonstrate that JNJ-47965567 displaced the binding of [3H]-A-804598 in a concentration dependent manner (Figure 2) both at the human and rat P2X7 cell membranes (other species were not tested routinely in the binding assay as rat was the in vivo species of choice). Reference: Br J Pharmacol. 2013 Oct;170(3):624-40. https://pubmed.ncbi.nlm.nih.gov/23889535/

In vivo activity:

Electrographic seizure-suppressive effects were also observed with a second P2X7R antagonist, JNJ-47965567, in the same mouse model. Reference: Neuropharmacology. 2017 Apr;116:351-363. https://pubmed.ncbi.nlm.nih.gov/28082183/

	Solvent	mg/mL	mM
Solubility
	DMF	30.0	61.39
	DMSO	59.6	122.01
	DMSO:PBS (pH 7.2) (1:3)	0.3	0.51
	Ethanol	12.5	25.58

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 488.65 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.

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. Dutta SS, Andonova AA, Wöellert T, Hewett SJ, Hewett JA. P2X7-dependent constitutive Interleukin-1β release from pyramidal neurons of the normal mouse hippocampus: Evidence for a role in maintenance of the innate seizure threshold. Neurobiol Dis. 2022 Jun 15;168:105689. doi: 10.1016/j.nbd.2022.105689. Epub 2022 Mar 11. PMID: 35288304; PMCID: PMC9067394. 2. Bhattacharya A, Wang Q, Ao H, Shoblock JR, Lord B, Aluisio L, Fraser I, Nepomuceno D, Neff RA, Welty N, Lovenberg TW, Bonaventure P, Wickenden AD, Letavic MA. Pharmacological characterization of a novel centrally permeable P2X7 receptor antagonist: JNJ-47965567. Br J Pharmacol. 2013 Oct;170(3):624-40. doi: 10.1111/bph.12314. PMID: 23889535; PMCID: PMC3792000. 3. Rodriguez-Alvarez N, Jimenez-Mateos EM, Engel T, Quinlan S, Reschke CR, Conroy RM, Bhattacharya A, Boylan GB, Henshall DC. Effects of P2X7 receptor antagonists on hypoxia-induced neonatal seizures in mice. Neuropharmacology. 2017 Apr;116:351-363. doi: 10.1016/j.neuropharm.2017.01.005. Epub 2017 Jan 10. PMID: 28082183. 4. Jimenez-Pacheco A, Diaz-Hernandez M, Arribas-Blázquez M, Sanz-Rodriguez A, Olivos-Oré LA, Artalejo AR, Alves M, Letavic M, Miras-Portugal MT, Conroy RM, Delanty N, Farrell MA, O'Brien DF, Bhattacharya A, Engel T, Henshall DC. Transient P2X7 Receptor Antagonism Produces Lasting Reductions in Spontaneous Seizures and Gliosis in Experimental Temporal Lobe Epilepsy. J Neurosci. 2016 Jun 1;36(22):5920-32. doi: 10.1523/JNEUROSCI.4009-15.2016. PMID: 27251615; PMCID: PMC6601816.

In vitro protocol:

In vivo protocol:

1. Rodriguez-Alvarez N, Jimenez-Mateos EM, Engel T, Quinlan S, Reschke CR, Conroy RM, Bhattacharya A, Boylan GB, Henshall DC. Effects of P2X7 receptor antagonists on hypoxia-induced neonatal seizures in mice. Neuropharmacology. 2017 Apr;116:351-363. doi: 10.1016/j.neuropharm.2017.01.005. Epub 2017 Jan 10. PMID: 28082183. 2. Jimenez-Pacheco A, Diaz-Hernandez M, Arribas-Blázquez M, Sanz-Rodriguez A, Olivos-Oré LA, Artalejo AR, Alves M, Letavic M, Miras-Portugal MT, Conroy RM, Delanty N, Farrell MA, O'Brien DF, Bhattacharya A, Engel T, Henshall DC. Transient P2X7 Receptor Antagonism Produces Lasting Reductions in Spontaneous Seizures and Gliosis in Experimental Temporal Lobe Epilepsy. J Neurosci. 2016 Jun 1;36(22):5920-32. doi: 10.1523/JNEUROSCI.4009-15.2016. PMID: 27251615; PMCID: PMC6601816.

1: Ly D, Dongol A, Cuthbertson P, Guy TV, Geraghty NJ, Sophocleous RA, Sin L, Turner BJ, Watson D, Yerbury JJ, Sluyter R. The P2X7 receptor antagonist JNJ-47965567 administered thrice weekly from disease onset does not alter progression of amyotrophic lateral sclerosis in SOD1^G93A mice. Purinergic Signal. 2020 Mar;16(1):109-122. doi: 10.1007/s11302-020-09692-4. Epub 2020 Mar 13. PMID: 32170537; PMCID: PMC7166237. 2: Ruiz-Ruiz C, García-Magro N, Negredo P, Avendaño C, Bhattacharya A, Ceusters M, García AG. Chronic administration of P2X7 receptor antagonist JNJ-47965567 delays disease onset and progression, and improves motor performance in ALS SOD1^G93A female mice. Dis Model Mech. 2020 Oct 30;13(10):dmm045732. doi: 10.1242/dmm.045732. PMID: 33174532; PMCID: PMC7648608. 3: Bhattacharya A, Wang Q, Ao H, Shoblock JR, Lord B, Aluisio L, Fraser I, Nepomuceno D, Neff RA, Welty N, Lovenberg TW, Bonaventure P, Wickenden AD, Letavic MA. Pharmacological characterization of a novel centrally permeable P2X7 receptor antagonist: JNJ-47965567. Br J Pharmacol. 2013 Oct;170(3):624-40. doi: 10.1111/bph.12314. PMID: 23889535; PMCID: PMC3792000.