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

JNJ-5207852
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WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 526662

CAS#: 98473-34-2

Description: 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

Product data Instruction

Theoretical Analysis

MedKoo Cat#: 526662
Name: JNJ-5207852
CAS#: 98473-34-2
Chemical Formula: C20H32N2O
Exact Mass: 316.25
Molecular Weight: 316.489
Elemental Analysis: C, 75.90; H, 10.19; N, 8.85; O, 5.06

Price and Availability

Size	Price	Availability
100mg	USD 650	2 Weeks
200mg	USD 950	2 Weeks
500mg	USD 1850	2 Weeks
1g	USD 2850	2 Weeks
Bulk inquiry Welcome, Customer: Please do not inquire quote if your intended use is for a patient since our products are for research use and for chemical synthesis use, not for human use . For in-stock products, we listed price in the web page. You may inquire prices for which sizes were not listed. If no price is listed, this means the product is not in stock at the moment, which may be available via custom synthesis. For cost-effective reason, minimum order of 1g is requested (typically very expensive). The lead time is usually 2-4 months. Quote of less than 1g will not be provided. MedKoo may not offer quote for below reasons: (1) current available synthetic method appears to be extremely expensive which is obviously not affordable to most customers; (2) Key raw material to make the product is temporally not available; (3) DEA controlled substances; (4) the product is under patent protection in customer’s country.

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

More Info:

Product Data:

Product Data

Instruction:

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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:	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 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.

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*When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and SDS / CoA (available online).

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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.

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