ORG25543 HCl | CAS#495076-64-7

ORG25543 HCl
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WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 555433

CAS#: 495076-64-7 (HCl)

Description: ORG25543 is a Potent and selective GlyT2 inhibitor (IC50 = 16 nM for hGlyT2).

Chemical Structure

ORG25543 HCl

CAS# 495076-64-7 (HCl)

Product data Instruction

Theoretical Analysis

MedKoo Cat#: 555433
Name: ORG25543 HCl
CAS#: 495076-64-7 (HCl)
Chemical Formula: C24H33ClN2O4
Exact Mass: 0.00
Molecular Weight: 448.988
Elemental Analysis: C, 64.20; H, 7.41; Cl, 7.90; N, 6.24; O, 14.25

Price and Availability

Size	Price	Availability	Quantity
10mg	USD 425
50mg	USD 1450
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.

Related CAS #: 363628-88-0 (free base) 495076-64-7 (HCl)

Synonym: ORG25543 HCl; ORG25543; ORG-25543; ORG 25543;

IUPAC/Chemical Name: N-[[1-(Dimethylamino)cyclopentyl]methyl]-3,5-dimethoxy-4-(phenylmethoxy)benzamide hydrochloride

InChi Key: NIPQJILJYQVZJR-UHFFFAOYSA-N

InChi Code: InChI=1S/C24H32N2O4.ClH/c1-26(2)24(12-8-9-13-24)17-25-23(27)19-14-20(28-3)22(21(15-19)29-4)30-16-18-10-6-5-7-11-18;/h5-7,10-11,14-15H,8-9,12-13,16-17H2,1-4H3,(H,25,27);1H

SMILES Code: O=C(NCC1(N(C)C)CCCC1)C2=CC(OC)=C(OCC3=CC=CC=C3)C(OC)=C2.[H]Cl

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: >3 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:	ORG25543 is a Potent and selective GlyT2 inhibitor (IC50 = 16 nM for hGlyT2).
In vitro activity:	TBD
In vivo activity:	TBD

Solubility Data

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	DMSO	44.9	100.00
	Water	9.0	20.00

Preparing Stock Solutions

The following data is based on the product molecular weight 448.99 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:	TBD
In vitro protocol:	TBD
In vivo protocol:	TBD

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1: Mostyn SN, Rawling T, Mohammadi S, Shimmon S, Frangos ZJ, Sarker S, Yousuf A, Vetter I, Ryan RM, Christie MJ, Vandenberg RJ. Development of an N-acyl amino acid that selectively inhibits the glycine transporter 2 to produce analgesia in a rat model of chronic pain. J Med Chem. 2019 Feb 4. doi: 10.1021/acs.jmedchem.8b01775. [Epub ahead of print] PubMed PMID: 30714733.

2: Motoyama N, Morita K, Shiraishi S, Kitayama T, Kanematsu T, Uezono Y, Dohi T. Relief of cancer pain by glycine transporter inhibitors. Anesth Analg. 2014 Oct;119(4):988-95. doi: 10.1213/ANE.0000000000000388. PubMed PMID: 25076101.

3: Mingorance-Le Meur A, Ghisdal P, Mullier B, De Ron P, Downey P, Van Der Perren C, Declercq V, Cornelis S, Famelart M, Van Asperen J, Jnoff E, Courade JP. Reversible inhibition of the glycine transporter GlyT2 circumvents acute toxicity while preserving efficacy in the treatment of pain. Br J Pharmacol. 2013 Nov;170(5):1053-63. doi: 10.1111/bph.12343. PubMed PMID: 23962079; PubMed Central PMCID: PMC3949653.

4: Apostolides PF, Trussell LO. Rapid, activity-independent turnover of vesicular transmitter content at a mixed glycine/GABA synapse. J Neurosci. 2013 Mar 13;33(11):4768-81. doi: 10.1523/JNEUROSCI.5555-12.2013. PubMed PMID: 23486948; PubMed Central PMCID: PMC3639006.

5: Romei C, Di Prisco S, Raiteri M, Raiteri L. Glycine release provoked by disturbed Na⁺, Na⁺ and Ca²⁺ homeostasis in cerebellar nerve endings: roles of Ca²⁺ channels, Na⁺/Ca²⁺ exchangers and GlyT2 transporter reversal. J Neurochem. 2011 Oct;119(1):50-63. doi: 10.1111/j.1471-4159.2011.07401.x. Epub 2011 Aug 22. PubMed PMID: 21790607.

6: Rousseau F, Aubrey KR, Supplisson S. The glycine transporter GlyT2 controls the dynamics of synaptic vesicle refilling in inhibitory spinal cord neurons. J Neurosci. 2008 Sep 24;28(39):9755-68. doi: 10.1523/JNEUROSCI.0509-08.2008. PubMed PMID: 18815261.

7: Morita K, Motoyama N, Kitayama T, Morioka N, Kifune K, Dohi T. Spinal antiallodynia action of glycine transporter inhibitors in neuropathic pain models in mice. J Pharmacol Exp Ther. 2008 Aug;326(2):633-45. doi: 10.1124/jpet.108.136267. Epub 2008 Apr 30. PubMed PMID: 18448867.

8: Luccini E, Romei C, Raiteri L. Glycinergic nerve endings in hippocampus and spinal cord release glycine by different mechanisms in response to identical depolarizing stimuli. J Neurochem. 2008 Jun 1;105(6):2179-89. doi: 10.1111/j.1471-4159.2008.05309.x. PubMed PMID: 18298662.

9: Huang H, Barakat L, Wang D, Bordey A. Bergmann glial GlyT1 mediates glycine uptake and release in mouse cerebellar slices. J Physiol. 2004 Nov 1;560(Pt 3):721-36. Epub 2004 Aug 26. PubMed PMID: 15331688; PubMed Central PMCID: PMC1665288.

10: Whitehead KJ, Pearce SM, Walker G, Sundaram H, Hill D, Bowery NG. Positive N-methyl-D-aspartate receptor modulation by selective glycine transporter-1 inhibition in the rat dorsal spinal cord in vivo. Neuroscience. 2004;126(2):381-90. PubMed PMID: 15207356.

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