JNJ-40411813 | ADX71149 | CAS#1127498-03-6 | PAM mGlu2

JNJ-40411813
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WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 526853

CAS#: 1127498-03-6

Description: JNJ-40411813, also known as ADX71149, is a positive allosteric modulator of the mGlu2 receptor. JNJ-40411813 acts as a PAM at the cloned mGlu2 receptor: EC50 = 147 ± 42 nmol/L in a [(35)S]GTPγS binding assay with human metabotropic glutamate type 2 (hmGlu2) CHO cells and EC50 = 64 ± 29 nmol/L in a Ca(2+) mobilization assay with hmGlu2 G α16 cotransfected HEK293 cells. JNJ-40411813 displaced [(3)H]JNJ-40068782 and [(3)H]JNJ-46281222 (mGlu2 receptor PAMs), while it failed to displace [(3)H]LY341495 (a competitive mGlu2/3 receptor antagonist). JNJ-40411813 is an interesting candidate to explore the therapeutic potential of mGlu2 PAMs, in in vivo rodents experiments as well as in clinical studies.

Chemical Structure

JNJ-40411813

CAS# 1127498-03-6

Product data Instruction

Theoretical Analysis

MedKoo Cat#: 526853
Name: JNJ-40411813
CAS#: 1127498-03-6
Chemical Formula: C20H25ClN2O
Exact Mass: 344.17
Molecular Weight: 344.883
Elemental Analysis: C, 69.65; H, 7.31; Cl, 10.28; N, 8.12; O, 4.64

Price and Availability

Size	Price	Availability
5mg	USD 90	Ready to ship
10mg	USD 150	Ready to ship
25mg	USD 250	Ready to ship
50mg	USD 450	Ready to ship
100mg	USD 800	Ready to ship
200mg	USD 1450	Ready to ship
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-40411813; JNJ 40411813; JNJ40411813; ADX71149; ADX 71149; ADX-71149.

IUPAC/Chemical Name: 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone

InChi Key: HYOGJHCDLQSAHX-UHFFFAOYSA-N

InChi Code: InChI=1S/C20H25ClN2O/c1-2-3-12-23-15-11-18(19(21)20(23)24)22-13-9-17(10-14-22)16-7-5-4-6-8-16/h4-8,11,15,17H,2-3,9-10,12-14H2,1H3

SMILES Code: ClC1=C(N2CCC(C3=CC=CC=C3)CC2)C=CN(CCCC)C1=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: >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

Certificate of Analysis:

View CoA: current batch, Lot#A22T08K29

QC Data:

View QC data: current batch, Lot#A22T08K29

Safety Data Sheet (SDS):

View Safety Data Sheet (SDS)

Instruction:

View handling instruction

Biological target:	JNJ-40411813 (ADX-71149) is a novel positive allosteric modulator of the metabotropic Glutamate 2 receptor (mGlu2R) with EC50 of 147 nM.
In vitro activity:	JNJ-40411813 acts as a PAM at the cloned mGlu2 receptor: EC50 = 147 ± 42 nmol/L in a [(35)S]GTPγS binding assay with human metabotropic glutamate type 2 (hmGlu2) CHO cells and EC50 = 64 ± 29 nmol/L in a Ca(2+) mobilization assay with hmGlu2 G α16 cotransfected HEK293 cells. Reference: Pharmacol Res Perspect. 2015 Feb;3(1):e00096. https://pubmed.ncbi.nlm.nih.gov/25692015/
In vivo activity:	In mice, JNJ-40411813, JNJ-42153605, and LY404039 inhibited spontaneous locomotion and phencyclidine- and scopolamine-induced but not d-amphetamine-induced hyperlocomotion; the 5HT2A antagonist ritanserin inhibited only spontaneous locomotion and phencyclidine-induced hyperlocomotion. Reference: Pharmacol Res Perspect. 2015 Mar;3(2):e00097. https://pubmed.ncbi.nlm.nih.gov/25692027/

Solubility Data

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	DMSO	25.0	72.49

Preparing Stock Solutions

The following data is based on the product molecular weight 344.88 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. Lavreysen H, Langlois X, Donck LV, Nuñez JM, Pype S, Lütjens R, Megens A. Preclinical evaluation of the antipsychotic potential of the mGlu2-positive allosteric modulator JNJ-40411813. Pharmacol Res Perspect. 2015 Mar;3(2):e00097. doi: 10.1002/prp2.97. Epub 2015 Jan 30. PMID: 25692027; PMCID: PMC4324682. 2. Lavreysen H, Ahnaou A, Drinkenburg W, Langlois X, Mackie C, Pype S, Lütjens R, Le Poul E, Trabanco AA, Nuñez JM. Pharmacological and pharmacokinetic properties of JNJ-40411813, a positive allosteric modulator of the mGlu2 receptor. Pharmacol Res Perspect. 2015 Feb;3(1):e00096. doi: 10.1002/prp2.96. Epub 2014 Dec 9. PMID: 25692015; PMCID: PMC4317228.
In vitro protocol:	1. Lavreysen H, Ahnaou A, Drinkenburg W, Langlois X, Mackie C, Pype S, Lütjens R, Le Poul E, Trabanco AA, Nuñez JM. Pharmacological and pharmacokinetic properties of JNJ-40411813, a positive allosteric modulator of the mGlu2 receptor. Pharmacol Res Perspect. 2015 Feb;3(1):e00096. doi: 10.1002/prp2.96. Epub 2014 Dec 9. PMID: 25692015; PMCID: PMC4317228.
In vivo protocol:	1. Lavreysen H, Langlois X, Donck LV, Nuñez JM, Pype S, Lütjens R, Megens A. Preclinical evaluation of the antipsychotic potential of the mGlu2-positive allosteric modulator JNJ-40411813. Pharmacol Res Perspect. 2015 Mar;3(2):e00097. doi: 10.1002/prp2.97. Epub 2015 Jan 30. PMID: 25692027; PMCID: PMC4324682. 2. Lavreysen H, Ahnaou A, Drinkenburg W, Langlois X, Mackie C, Pype S, Lütjens R, Le Poul E, Trabanco AA, Nuñez JM. Pharmacological and pharmacokinetic properties of JNJ-40411813, a positive allosteric modulator of the mGlu2 receptor. Pharmacol Res Perspect. 2015 Feb;3(1):e00096. doi: 10.1002/prp2.96. Epub 2014 Dec 9. PMID: 25692015; PMCID: PMC4317228.

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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: Kent JM, Daly E, Kezic I, Lane R, Lim P, De Smedt H, De Boer P, Van Nueten L, Drevets WC, Ceusters M. Efficacy and safety of an adjunctive mGlu2 receptor positive allosteric modulator to a SSRI/SNRI in anxious depression. Prog Neuropsychopharmacol Biol Psychiatry. 2016 Jun 3;67:66-73. doi: 10.1016/j.pnpbp.2016.01.009. Epub 2016 Jan 20. PubMed PMID: 26804646.

2: Ahnaou A, de Boer P, Lavreysen H, Huysmans H, Sinha V, Raeymaekers L, Van De Casteele T, Cid JM, Van Nueten L, Macdonald GJ, Kemp JA, Drinkenburg WH. Translational neurophysiological markers for activity of the metabotropic glutamate receptor (mGluR2) modulator JNJ-40411813: Sleep EEG correlates in rodents and healthy men. Neuropharmacology. 2016 Apr;103:290-305. doi: 10.1016/j.neuropharm.2015.11.031. Epub 2015 Dec 12. PubMed PMID: 26686390.

3: Salih H, Anghelescu I, Kezic I, Sinha V, Hoeben E, Van Nueten L, De Smedt H, De Boer P. Pharmacokinetic and pharmacodynamic characterisation of JNJ-40411813, a positive allosteric modulator of mGluR2, in two randomised, double-blind phase-I studies. J Psychopharmacol. 2015 Apr;29(4):414-25. doi: 10.1177/0269881115573403. Epub 2015 Mar 3. PubMed PMID: 25735992.

4: Lavreysen H, Langlois X, Donck LV, Nuñez JM, Pype S, Lütjens R, Megens A. Preclinical evaluation of the antipsychotic potential of the mGlu2-positive allosteric modulator JNJ-40411813. Pharmacol Res Perspect. 2015 Mar;3(2):e00097. doi: 10.1002/prp2.97. Epub 2015 Jan 30. PubMed PMID: 25692027; PubMed Central PMCID: PMC4324682.

5: Lavreysen H, Ahnaou A, Drinkenburg W, Langlois X, Mackie C, Pype S, Lütjens R, Le Poul E, Trabanco AA, Nuñez JM. Pharmacological and pharmacokinetic properties of JNJ-40411813, a positive allosteric modulator of the mGlu2 receptor. Pharmacol Res Perspect. 2015 Feb;3(1):e00096. doi: 10.1002/prp2.96. Epub 2014 Dec 9. PubMed PMID: 25692015; PubMed Central PMCID: PMC4317228.

6: Cid JM, Tresadern G, Duvey G, Lütjens R, Finn T, Rocher JP, Poli S, Vega JA, de Lucas AI, Matesanz E, Linares ML, Andrés JI, Alcazar J, Alonso JM, Macdonald GJ, Oehlrich D, Lavreysen H, Ahnaou A, Drinkenburg W, Mackie C, Pype S, Gallacher D, Trabanco AA. Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor. J Med Chem. 2014 Aug 14;57(15):6495-512. doi: 10.1021/jm500496m. Epub 2014 Jul 28. PubMed PMID: 25032784.

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