MDL-29951 - 10mM in DMSO , CAS No.130798-51-5

CAS: 130798-51-5 Cat. No.: M654998 Summenformel: C₁₂H₉Cl₂NO₄ Molekulargewicht: 302.11 PubChem CID: 446916

QUALITÄT & REINHEIT 10mM in DMSO

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Übersicht

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

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. MDL-29951 is found to inhibit the human F16Bpase under these conditions (IC 50 =2.5 μM). MDL-29951 inhibits the human liver (IC 50 =2.5 μM), porcine kidney (IC 50 =1.0 μM), and rabbit liver (IC 50 =0.21 μM) isoforms of the enzyme, but is significantly less potent against the rat liver isoform (IC 50 =11 μM). 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 Ca 2+ 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

IC50& Target:NMDA Receptor

Spezifikationen

Spezifikationen & Reinheit

10mM in DMSO

Biochemische und physiologische Mechanismen

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

Storage

Store at -80°C

Verschickt in

Dry ice packs + Cold packs

Dieses Produkt erfordert Kühlkettenversand. Grundversand und andere Economy-Optionen sind nicht verfügbar.

Aktionsart

ANTAGONIST

Namen und Kennungen

Isomere SMILES

C1=C(C=C(C2=C1NC(=C2CCC(=O)O)C(=O)O)Cl)Cl

Alternative CAS-Nummer

101861-63-6

PubChem CID

446916

MeSH-Eintrag

2-carboxy-4,6-dichloro-(1H)-indole-3-propanoic acid;3-(4,6-dichloro-2-carboxyindol-3-yl)propionic acid;3-DCCIP;MDL 29951;MDL-29951;MDL29,951

Molekulargewicht

302.11

Zugehörige Ziele (menschlich)

GPR17 Tchem Uracil nucleotide/cysteinyl leukotriene receptor (2 Activities)

Discover Target: GPR17

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)