2. Membrane Transporter/Ion Channel Neuronal Signaling
  3. iGluR
  4. MDL 105519

MDL 105519 is a potent and selective antagonist of glycine binding to the NMDA receptor.

For research use only. We do not sell to patients.

MDL 105519 Chemical Structure

MDL 105519 Chemical Structure

CAS No. : 161230-88-2

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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of MDL 105519:

MDL 105519 Related Antibodies

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Description

MDL 105519 is a potent and selective antagonist of glycine binding to the NMDA receptor.

IC50 & Target

NMDA Receptor

 

In Vitro

MDL 105519 is a potent and selective ligand for the glycine recognition site that completely inhibit the binding of [3H]glycine to rat brain membranes with a Ki value of 10.9 nM. MDL 105519 is approximately 10,000-fold selective for the glycine recognition site relative to the other receptor types investigated. MDL 105519 inhibits NMDA-dependent responses, such as elevations of [3H]TCP binding in brain membranes, cyclic GMP accumulation in brain slices, and alterations in cytosolic Ca2+ and Na+-Ca2+ currents in cultured neurons. Inhibition is non-competitive with respect to NMDA and could be nullified with D-serine[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

MDL 105519 Related Antibodies
In Vivo

MDL 105519 is an NMDA receptor antagonist in vivo. Intravenously administration of MDL 105519 prevents harmaline-stimulated increases in cerebellar cyclic GMP content, providing biochemical evidence of NMDA receptor antagonism in vivo. This antagonism is associated with anticonvulsant activity in genetically based, chemically induced, and electrically mediated seizure models. Anxiolytic activity is observed in the rat separation-induced vocalization model, but muscle-relaxant activity is apparent at lower doses. Higher doses impair rotorod performance, but are without effect on mesolimbic dopamine turnover or prepulse inhibition of the startle reflex[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Molecular Weight

376.19

Formula

C18H11Cl2NO4
CAS No.
Appearance

Solid

Color

Off-white to yellow

SMILES

O=C(O)C(N1)=C(/C=C(C2=CC=CC=C2)/C(O)=O)C3=C1C=C(Cl)C=C3Cl
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 17 mg/mL (45.19 mM; Need ultrasonic and warming; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.6582 mL 13.2912 mL 26.5823 mL
5 mM 0.5316 mL 2.6582 mL 5.3165 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation

Purity: 99.67%

SDS (251 KB)

COA (257 KB) LCMS (93 KB)

Handling Instructions (2659 KB)
References
Animal Administration
[1]

Adult, male, CD rats are administered MK-801 (n=4, 2 mg/kg, i.p.) or MDL 105519 (n=4, 2 mg/kg, i.p.) and extracellular dopamine concentrations are measured using in vivo microdialysis[1].

Mice: Mice adult male CD-1 are injected with various doses of MDL 105519 (8, 16, 32, 64, 128 mg/kg) intraperitoneally and 30 min later are administered harmaline 50 mg/kg. Sixty minutes after the first injection, the mice are killed and cerebellar cGMP content is measured by radioimmunoassay[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.6582 mL 13.2912 mL 26.5823 mL 66.4558 mL
5 mM 0.5316 mL 2.6582 mL 5.3165 mL 13.2912 mL
10 mM 0.2658 mL 1.3291 mL 2.6582 mL 6.6456 mL
15 mM 0.1772 mL 0.8861 mL 1.7722 mL 4.4304 mL
20 mM 0.1329 mL 0.6646 mL 1.3291 mL 3.3228 mL
25 mM 0.1063 mL 0.5316 mL 1.0633 mL 2.6582 mL
30 mM 0.0886 mL 0.4430 mL 0.8861 mL 2.2152 mL
40 mM 0.0665 mL 0.3323 mL 0.6646 mL 1.6614 mL
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MDL 105519 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

MDL 105519161230-88-2MDL105519MDL-105519iGluRIonotropic glutamate receptorsInhibitorinhibitorinhibit

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