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MDL-29951

Name: MDL-29951
Brand: TargetMol
SKU: T1897
Price: 43 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T1897Cas No. 130798-51-5

MDL-29951 is a novel glycine antagonist for NMDA receptor activation.

MDL-29951

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Purity: 99.49%

Catalog No. T1897Cas No. 130798-51-5

MDL-29951 is a novel glycine antagonist for NMDA receptor activation.

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$43	In Stock	In Stock
5 mg	$106	In Stock	In Stock
10 mg	$163	In Stock	In Stock
25 mg	$293	In Stock	In Stock
50 mg	$419	In Stock	In Stock
100 mg	$673	In Stock	In Stock
1 mL x 10 mM (in DMSO)	$110	In Stock	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

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Purity:99.49%

Color:White to Yellow

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COA HNMR HPLC

Product Introduction

Bioactivity

Description	MDL-29951 is a novel glycine antagonist for NMDA receptor activation.
Targets&IC50	NMDA:0.14 μM
In vitro	MDL 100,748 and MDL 29,951 are approximately 2000-fold selective for the glycine binding site relative to the glutamate recognition sites[1]. MDL-29951 is found to inhibit the human F16Bpase under these conditions (IC50=2.5 μM). MDL-29951 inhibits the human liver (IC50=2.5 μM), porcine kidney (IC50=1.0 μM), and rabbit liver (IC50=0.21 μM) isoforms of the enzyme, but is significantly less potent against the rat liver isoform (IC50=11 μM)[2]. The MDL29951-activated receptor exhibits other activities associated with GPCR-mediated signaling, including G protein-dependent activation of extracellular signal-regulated kinase 1 and 2 (ERK1/2) and recruitment of β-arrestin. As with recombinant cell systems, MDL29951 promotes Ca2+ signaling responses and inhibition of cyclic adenosine monophosphate (cAMP) accumulation in rat oligodendrocyte precursor cells during the period of peak GPR17 abundance. Effects of MDL29951 are markedly reduced in cells with low GPR17 abundance and are blocked by pranlukast[3].
Kinase Assay	[3H]JCPP (30.7 Ci/mmol) binding assays are conducted in minivials, incubated for 15 mm at 25°C in 1 mL of 50 mM Tris-HC1 (pH 7.4) containing 10 nM [3H]JCPP, 200 g of membrane protein and unlabeled ligands as indicated. Nonspecific binding is defined using 1 mM L-glutamate. Bound ligand is separated by centrifugation. Specific binding accounted for approximately 80% of total binding.

Chemical Properties

Molecular Weight	302.11
Formula	C₁₂H₉Cl₂NO₄
Cas No.	130798-51-5
Smiles	OC(=O)CCc1c([nH]c2cc(Cl)cc(Cl)c12)C(O)=O
Relative Density.	1.657 g/cm3 (Predicted)

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 50 mg/mL (165.5 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (6.62 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	3.3101 mL	16.5503 mL	33.1005 mL	165.5026 mL
5 mM	0.6620 mL	3.3101 mL	6.6201 mL	33.1005 mL
10 mM	0.3310 mL	1.6550 mL	3.3101 mL	16.5503 mL
20 mM	0.1655 mL	0.8275 mL	1.6550 mL	8.2751 mL
50 mM	0.0662 mL	0.3310 mL	0.6620 mL	3.3101 mL
100 mM	0.0331 mL	0.1655 mL	0.3310 mL	1.6550 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc