MDL-105519

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

MedKoo CAT#: 522402

CAS#: 161230-88-2

Description: MDL-105519 is a high affinity NMDA glutamate receptor antagonist at the glycine site. MDL 105,519 prevented harmaline-stimulated increases in cerebellar cyclic GMP content, providing biochemical evidence of NMDA receptor antagonism in vivo. This antagonism was associated with anticonvulsant activity in genetically based, chemically induced, and electrically mediated seizure models.

Chemical Structure

MDL-105519

CAS# 161230-88-2

Instruction

Theoretical Analysis

MedKoo Cat#: 522402
Name: MDL-105519
CAS#: 161230-88-2
Chemical Formula: C18H11Cl2NO4
Exact Mass: 375.01
Molecular Weight: 376.180
Elemental Analysis: C, 57.47; H, 2.95; Cl, 18.85; N, 3.72; O, 17.01

Price and Availability

Size	Price	Availability	Quantity
1g	USD -1
2g	USD -1
5g	USD -1
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: MDL-105519; MDL 105519; MDL105519; MDL105,519; MDL-105,519; MDL 105,519

IUPAC/Chemical Name: (E)-3-(2-carboxy-2-phenylvinyl)-4,6-dichloro-1H-indole-2-carboxylic acid

InChi Key: LPWVUDLZUVBQGP-DHZHZOJOSA-N

InChi Code: InChI=1S/C18H11Cl2NO4/c19-10-6-13(20)15-12(16(18(24)25)21-14(15)7-10)8-11(17(22)23)9-4-2-1-3-5-9/h1-8,21H,(H,22,23)(H,24,25)/b11-8+

SMILES Code: ClC1=C2C(NC(C(O)=O)=C2/C=C(C3=CC=CC=C3)/C(O)=O)=CC(Cl)=C1

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:

Instruction:

View handling instruction

Biological target:
In vitro activity:
In vivo activity:

Preparing Stock Solutions

The following data is based on the product molecular weight 376.18 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:
In vitro protocol:
In vivo protocol:

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1: Kakuda T, Nozawa A, Sugimoto A, Niino H. Inhibition by theanine of binding of [3H]AMPA, [3H]kainate, and [3H]MDL 105,519 to glutamate receptors. Biosci Biotechnol Biochem. 2002 Dec;66(12):2683-6. PubMed PMID: 12596867.

2: Sharma TA, Reynolds IJ. Complex polyamine effects on [3H]MDL 105,519 binding to the NMDA receptor glycine site. Neurochem Int. 1998 Aug;33(2):155-9. PubMed PMID: 9761459.

3: Chazot PL, Reiss C, Chopra B, Stephenson FA. [3H]MDL 105,519 binds with equal high affinity to both assembled and unassembled NR1 subunits of the NMDA receptor. Eur J Pharmacol. 1998 Jul 17;353(1):137-40. PubMed PMID: 9721050.

4: Höfner G, Wanner KT. Characterisation of the binding of [3H]MDL 105,519, a radiolabelled antagonist for the N-methyl-D-aspartate-associated glycine site, to pig cortical brain membranes. Neurosci Lett. 1997 Apr 25;226(2):79-82. PubMed PMID: 9159494.

5: Baron BM, Harrison BL, Kehne JH, Schmidt CJ, van Giersbergen PL, White HS, Siegel BW, Senyah Y, McCloskey TC, Fadayel GM, Taylor VL, Murawsky MK, Nyce P, Salituro FG. Pharmacological characterization of MDL 105,519, an NMDA receptor glycine site antagonist. Eur J Pharmacol. 1997 Apr 4;323(2-3):181-92. PubMed PMID: 9128837.

6: Siegel BW, Sreekrishna K, Baron BM. Binding of the radiolabeled glycine site antagonist [3H]MDL 105,519 to homomeric NMDA-NR1a receptors. Eur J Pharmacol. 1996 Oct 3;312(3):357-65. PubMed PMID: 8894619.

7: Baron BM, Siegel BW, Harrison BL, Gross RS, Hawes C, Towers P. [3H]MDL 105,519, a high-affinity radioligand for the N-methyl-D-aspartate receptor-associated glycine recognition site. J Pharmacol Exp Ther. 1996 Oct;279(1):62-8. PubMed PMID: 8858976.

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