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MedKoo Cat#: 329512 | Name: Rislenemdaz

Description:

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

Rislenemdaz, also known as MK-0657, is a NR2B-selective NMDA antagonist potentially for the treatment of Parkinson's disease.

Chemical Structure

Rislenemdaz
Rislenemdaz
CAS#808732-98-1 (free base)

Theoretical Analysis

MedKoo Cat#: 329512

Name: Rislenemdaz

CAS#: 808732-98-1 (free base)

Chemical Formula: C19H23FN4O2

Exact Mass: 358.1805

Molecular Weight: 358.42

Elemental Analysis: C, 63.67; H, 6.47; F, 5.30; N, 15.63; O, 8.93

Price and Availability

This product is currently not in stock but may be available through custom synthesis. To ensure cost efficiency, the minimum order quantity is 1 gram. The estimated lead time is 2 to 4 months, with pricing dependent on the complexity of the synthesis (typically high for intricate chemistries). Quotes for quantities below 1 gram will not be provided. To request a quote, please click the button below. Note: If this product becomes available in stock in the future, pricing will be listed accordingly.
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Related CAS #
808733-06-4 (HCl) 808732-98-1 (free base) 1893392-76-1 (mesylate)
Synonym
Rislenemdaz; MK-0657; MK 0657; MK0657; CERC-301; CERC301; CERC 301;
IUPAC/Chemical Name
4-methylbenzyl (3S,4R)-3-fluoro-4-((pyrimidin-2-ylamino)methyl)piperidine-1-carboxylate
InChi Key
RECBFDWSXWAXHY-IAGOWNOFSA-N
InChi Code
InChI=1S/C19H23FN4O2/c1-14-3-5-15(6-4-14)13-26-19(25)24-10-7-16(17(20)12-24)11-23-18-21-8-2-9-22-18/h2-6,8-9,16-17H,7,10-13H2,1H3,(H,21,22,23)/t16-,17-/m1/s1
SMILES Code
O=C(N1C[C@@H](F)[C@@H](CNC2=NC=CC=N2)CC1)OCC3=CC=C(C)C=C3
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

Preparing Stock Solutions

The following data is based on the product molecular weight 358.42 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
1: Ibrahim L, Diaz Granados N, Jolkovsky L, Brutsche N, Luckenbaugh DA, Herring WJ, Potter WZ, Zarate CA Jr. A Randomized, placebo-controlled, crossover pilot trial of the oral selective NR2B antagonist MK-0657 in patients with treatment-resistant major depressive disorder. J Clin Psychopharmacol. 2012 Aug;32(4):551-7. doi: 10.1097/JCP.0b013e31825d70d6. PubMed PMID: 22722512; PubMed Central PMCID: PMC3438886. 2: Addy C, Assaid C, Hreniuk D, Stroh M, Xu Y, Herring WJ, Ellenbogen A, Jinnah HA, Kirby L, Leibowitz MT, Stewart RM, Tarsy D, Tetrud J, Stoch SA, Gottesdiener K, Wagner J. Single-dose administration of MK-0657, an NR2B-selective NMDA antagonist, does not result in clinically meaningful improvement in motor function in patients with moderate Parkinson's disease. J Clin Pharmacol. 2009 Jul;49(7):856-64. doi: 10.1177/0091270009336735. PubMed PMID: 19491335. 3: Skolnick P, Kos T, Czekaj J, Popik P. Effect of NMDAR antagonists in the tetrabenazine test for antidepressants: comparison with the tail suspension test. Acta Neuropsychiatr. 2015 Aug;27(4):228-34. doi: 10.1017/neu.2015.14. PubMed PMID: 25858023. 4: Jaso BA, Niciu MJ, Iadarola ND, Lally N, Richards EM, Park M, Ballard ED, Nugent AC, Machado-Vieira R, Zarate CA Jr. THERAPEUTIC MODULATION OF GLUTAMATE RECEPTORS IN MAJOR DEPRESSIVE DISORDER. Curr Neuropharmacol. 2016 Mar 21. [Epub ahead of print] PubMed PMID: 26997505. 5: Deutschenbaur L, Beck J, Kiyhankhadiv A, Mühlhauser M, Borgwardt S, Walter M, Hasler G, Sollberger D, Lang UE. Role of calcium, glutamate and NMDA in major depression and therapeutic application. Prog Neuropsychopharmacol Biol Psychiatry. 2016 Jan 4;64:325-33. doi: 10.1016/j.pnpbp.2015.02.015. Review. PubMed PMID: 25747801. 6: Machado-Vieira R, Henter ID, Zarate CA Jr. New targets for rapid antidepressant action. Prog Neurobiol. 2015 Dec 23. pii: S0301-0082(15)30038-1. doi: 10.1016/j.pneurobio.2015.12.001. [Epub ahead of print] Review. PubMed PMID: 26724279; PubMed Central PMCID: PMC4919246. 7: Fernandes A, Wojcik T, Baireddy P, Pieschl R, Newton A, Tian Y, Hong Y, Bristow L, Li YW. Inhibition of in vivo [(3)H]MK-801 binding by NMDA receptor open channel blockers and GluN2B antagonists in rats and mice. Eur J Pharmacol. 2015 Nov 5;766:1-8. doi: 10.1016/j.ejphar.2015.08.044. PubMed PMID: 26325093. 8: Caddy C, Amit BH, McCloud TL, Rendell JM, Furukawa TA, McShane R, Hawton K, Cipriani A. Ketamine and other glutamate receptor modulators for depression in adults. Cochrane Database Syst Rev. 2015 Sep 23;(9):CD011612. doi: 10.1002/14651858.CD011612.pub2. Review. PubMed PMID: 26395901. 9: Dutta A, McKie S, Deakin JF. Ketamine and other potential glutamate antidepressants. Psychiatry Res. 2015 Jan 30;225(1-2):1-13. doi: 10.1016/j.psychres.2014.10.028. Review. PubMed PMID: 25467702. 10: Pochwat B, Pałucha-Poniewiera A, Szewczyk B, Pilc A, Nowak G. NMDA antagonists under investigation for the treatment of major depressive disorder. Expert Opin Investig Drugs. 2014 Sep;23(9):1181-92. doi: 10.1517/13543784.2014.918951. Review. Erratum in: Expert Opin Investig Drugs. 2014 Oct;23(10):1457. PubMed PMID: 24818801. 11: Dang YH, Ma XC, Zhang JC, Ren Q, Wu J, Gao CG, Hashimoto K. Targeting of NMDA receptors in the treatment of major depression. Curr Pharm Des. 2014;20(32):5151-9. Review. PubMed PMID: 24410564. 12: Hashimoto K, Malchow B, Falkai P, Schmitt A. Glutamate modulators as potential therapeutic drugs in schizophrenia and affective disorders. Eur Arch Psychiatry Clin Neurosci. 2013 Aug;263(5):367-77. doi: 10.1007/s00406-013-0399-y. Review. PubMed PMID: 23455590. 13: Tomillero A, Moral MA. Gateways to clinical trials. Methods Find Exp Clin Pharmacol. 2010 Jan-Feb;32(1):47-86. PubMed PMID: 20383346.

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