JNJ-5207852 | CAS#98473-34-2 | H3 antagonist

MedKoo Cat#: 526662 | Name: JNJ-5207852

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Description:

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

JNJ-5207852 is a potent and selective H3 antagonist with high affinity at the rat (pKi=8.9) and human (pKi=9.24) H3 receptor. JNJ-5207852 is selective for the H3 receptor, with negligible binding to other receptors, transporters and ion channels at 1 microm. JNJ-5207852 readily penetrates the brain tissue after subcutaneous (s.c.) administration, as determined by ex vivo autoradiography (ED50 of 0.13 mg kg(-1) in mice).

Chemical Structure

JNJ-5207852

CAS#98473-34-2

Theoretical Analysis

MedKoo Cat#: 526662

Name: JNJ-5207852

CAS#: 98473-34-2

Chemical Formula: C20H32N2O

Exact Mass: 316.2515

Molecular Weight: 316.49

Elemental Analysis: C, 75.90; H, 10.19; N, 8.85; O, 5.06

Price and Availability

Size	Price	Availability
100mg	USD 650.00	2 Weeks
200mg	USD 950.00	2 Weeks
500mg	USD 1,850.00	2 Weeks
1g	USD 2,850.00	2 Weeks

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Synonym

JNJ-5207852; JNJ 5207852; JNJ5207852.

IUPAC/Chemical Name

1-(4-(3-(piperidin-1-yl)propoxy)benzyl)piperidine

InChi Key

PTKHFRNHJULJKT-UHFFFAOYSA-N

InChi Code

InChI=1S/C20H32N2O/c1-3-12-21(13-4-1)16-7-17-23-20-10-8-19(9-11-20)18-22-14-5-2-6-15-22/h8-11H,1-7,12-18H2

SMILES Code

N1(CC2=CC=C(OCCCN3CCCCC3)C=C2)CCCCC1

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, not in water

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

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Product Data

Product Data

Instruction

View handling instruction

Biological target:

JNJ-5207852 is a potent and selective H3 antagonist.

In vitro activity:

JNJ-5207852 increased GIIS (glucose-induced insulin secretion) in a dose-dependent manner, with an EC50 of 13.8 μM and an Emax of 103% (Figure 3D). Reference: Br J Pharmacol. 2014 Jan;171(1):171-85. https://pubmed.ncbi.nlm.nih.gov/24117016/

In vivo activity:

JNJ-5207852 elicited a dose-dependent increase in the total time spent awake (Figure 4a). This wake-promoting effect was most noticeable at the higher dose, where 10 mg kg−1 JNJ-5207852 caused an increase in time spent awake that manifested within the first 30 min after dosing and remained present throughout the observation period (1580±103 vs 640±122 s in the vehicle-treated rats in the 30–60 min post-dosing interval, P<0.05; 1525±241 vs 577±184 s in the vehicle-treated animals in the 60–90 min post-dosing observation interval, P<0.05). Reference: Br J Pharmacol. 2004 Nov;143(5):649-61. https://pubmed.ncbi.nlm.nih.gov/15466448/

Preparing Stock Solutions

The following data is based on the product molecular weight 316.49 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. Nakamura T, Yoshikawa T, Noguchi N, Sugawara A, Kasajima A, Sasano H, Yanai K. The expression and function of histamine H₃ receptors in pancreatic beta cells. Br J Pharmacol. 2014 Jan;171(1):171-85. doi: 10.1111/bph.12429. PMID: 24117016; PMCID: PMC3874705. 2. Barbier AJ, Berridge C, Dugovic C, Laposky AD, Wilson SJ, Boggs J, Aluisio L, Lord B, Mazur C, Pudiak CM, Langlois X, Xiao W, Apodaca R, Carruthers NI, Lovenberg TW. Acute wake-promoting actions of JNJ-5207852, a novel, diamine-based H3 antagonist. Br J Pharmacol. 2004 Nov;143(5):649-61. doi: 10.1038/sj.bjp.0705964. Epub 2004 Oct 4. Erratum in: Br J Pharmacol. 2005 Jan;144(1):145. PMID: 15466448; PMCID: PMC1575430.

In vitro protocol:

In vivo protocol:

1. Barbier AJ, Berridge C, Dugovic C, Laposky AD, Wilson SJ, Boggs J, Aluisio L, Lord B, Mazur C, Pudiak CM, Langlois X, Xiao W, Apodaca R, Carruthers NI, Lovenberg TW. Acute wake-promoting actions of JNJ-5207852, a novel, diamine-based H3 antagonist. Br J Pharmacol. 2004 Nov;143(5):649-61. doi: 10.1038/sj.bjp.0705964. Epub 2004 Oct 4. Erratum in: Br J Pharmacol. 2005 Jan;144(1):145. PMID: 15466448; PMCID: PMC1575430.

1: Nakamura T, Yoshikawa T, Noguchi N, Sugawara A, Kasajima A, Sasano H, Yanai K. The expression and function of histamine H₃ receptors in pancreatic beta cells. Br J Pharmacol. 2014 Jan;171(1):171-85. doi: 10.1111/bph.12429. PubMed PMID: 24117016; PubMed Central PMCID: PMC3874705. 2: Neumann D, Beermann S, Burhenne H, Glage S, Hartwig C, Seifert R. The dual H3/4R antagonist thioperamide does not fully mimic the effects of the 'standard' H4R antagonist JNJ 7777120 in experimental murine asthma. Naunyn Schmiedebergs Arch Pharmacol. 2013 Nov;386(11):983-90. doi: 10.1007/s00210-013-0898-4. Epub 2013 Jul 3. PubMed PMID: 23820873. 3: Abuhamdah RM, van Rensburg R, Lethbridge NL, Ennaceur A, Chazot PL. Effects of methimepip and JNJ-5207852 in Wistar rats exposed to an open-field with and without object and in Balb/c mice exposed to a radial-arm maze. Front Syst Neurosci. 2012 Jul 16;6:54. doi: 10.3389/fnsys.2012.00054. eCollection 2012. PubMed PMID: 22811660; PubMed Central PMCID: PMC3397409. 4: Bonaventure P, Letavic M, Dugovic C, Wilson S, Aluisio L, Pudiak C, Lord B, Mazur C, Kamme F, Nishino S, Carruthers N, Lovenberg T. Histamine H3 receptor antagonists: from target identification to drug leads. Biochem Pharmacol. 2007 Apr 15;73(8):1084-96. Epub 2006 Nov 3. PubMed PMID: 17129577. 5: Airaksinen AJ, Jablonowski JA, van der Mey M, Barbier AJ, Klok RP, Verbeek J, Schuit R, Herscheid JD, Leysen JE, Carruthers NI, Lammertsma AA, Windhorst AD. Radiosynthesis and biodistribution of a histamine H3 receptor antagonist 4-[3-(4-piperidin-1-yl-but-1-ynyl)-[11C]benzyl]-morpholine: evaluation of a potential PET ligand. Nucl Med Biol. 2006 Aug;33(6):801-10. PubMed PMID: 16934699. 6: Jia F, Kato M, Dai H, Xu A, Okuda T, Sakurai E, Okamura N, Lovenberg TW, Barbier A, Carruthers NI, Iinuma K, Yanai K. Effects of histamine H(3) antagonists and donepezil on learning and mnemonic deficits induced by pentylenetetrazol kindling in weanling mice. Neuropharmacology. 2006 Mar;50(4):404-11. Epub 2005 Nov 28. PubMed PMID: 16310812. 7: Barbier AJ, Berridge C, Dugovic C, Laposky AD, Wilson SJ, Boggs J, Aluisio L, Lord B, Mazur C, Pudiak CM, Langlois X, Xiao W, Apodaca R, Carruthers NI, Lovenberg TW. Acute wake-promoting actions of JNJ-5207852, a novel, diamine-based H3 antagonist. Br J Pharmacol. 2004 Nov;143(5):649-61. Epub 2004 Oct 4. Erratum in: Br J Pharmacol. 2005 Jan;144(1):145. PubMed PMID: 15466448; PubMed Central PMCID: PMC1575430. 8: Apodaca R, Dvorak CA, Xiao W, Barbier AJ, Boggs JD, Wilson SJ, Lovenberg TW, Carruthers NI. A new class of diamine-based human histamine H3 receptor antagonists: 4-(aminoalkoxy)benzylamines. J Med Chem. 2003 Aug 28;46(18):3938-44. PubMed PMID: 12930154.