1. Membrane Transporter/Ion Channel
    Neuronal Signaling
  2. iGluR

MDL-29951 

Cat. No.: HY-16312 Purity: 98.50%
Handling Instructions

MDL-29951 is a novel glycine antagonist of NMDA receptor activation, with Ki of 0.14 μM for [3H]glycine binding in vitro and in vivo.

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

MDL-29951 Chemical Structure

MDL-29951 Chemical Structure

CAS No. : 130798-51-5

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 238 In-stock
Stock in the United States
Estimated Time of Arrival: December 31
5 mg USD 216 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
10 mg USD 384 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
50 mg USD 1080 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
100 mg USD 1680 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

    MDL-29951 purchased from MCE. Usage Cited in: J Neurosci. 2016 Oct 12;36(41):10560-10573.

    The inhibition of Epac1 activity by ESI-09 reduces oligodendrocyte maturation.

    MDL-29951 purchased from MCE. Usage Cited in: J Neurosci. 2016 Oct 12;36(41):10560-10573.

    The inhibition of PKA signaling with PKA inhibitor H89 reduces cell viability observed after Pranlukast treatment.
    • Biological Activity

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References

    Description

    MDL-29951 is a novel glycine antagonist of NMDA receptor activation, with Ki of 0.14 μM for [3H]glycine binding in vitro and in vivo.

    IC50 & Target

    Ki: 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].

    References
    Preparing Stock Solutions
    Concentration Volume Mass 1 mg 5 mg 10 mg
    1 mM 3.3101 mL 16.5503 mL 33.1005 mL
    5 mM 0.6620 mL 3.3101 mL 6.6201 mL
    10 mM 0.3310 mL 1.6550 mL 3.3101 mL
    Please refer to the solubility information to select the appropriate solvent.
    Kinase Assay
    [1]

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

    References
    Molecular Weight

    302.11

    Formula

    C₁₂H₉Cl₂NO₄

    CAS No.

    130798-51-5

    SMILES

    O=C(O)CCC1=C(C(O)=O)NC2=C1C(Cl)=CC(Cl)=C2

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Shipping

    Room temperature in continental US; may vary elsewhere

    Solvent & Solubility

    10 mM in DMSO

    * "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

    Inquiry Online

    Your information is safe with us. * Required Fields.

    Product name

     

    Salutation

    Applicant name *

     

    Email address *

    Phone number *

     

    Organization name *

    Country or Region *

     

    Requested quantity *

    Remarks

    Bulk Inquiry

    Inquiry Information

    Product Name:
    MDL-29951
    Cat. No.:
    HY-16312
    Quantity: