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

CAS: 130798-51-5 Cat. No.: M654998 Fórmula: C₁₂H₉Cl₂NO₄ Peso molecular: 302.11 PubChem CID: 446916

GRAU & PUREZA 10mM in DMSO

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Visão geral

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

Especificações

Especificações e pureza

10mM in DMSO

Mecanismos bioquímicos e fisiológicos

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.

Condições de armazenamento de armazenamento

Store at -80°C

Enviado em

Dry ice packs + Cold packs

Este produto requer transporte de cadeia fria. Serviços terrestres e outros serviços econômicos não estão disponíveis.

Tipo de ação

ANTAGONIST

Nomes e identificadores

SMILES isoméricas

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

CAS alternativo

101861-63-6

PubChem CID

446916

Termos de entrada MeSH

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

Peso molecular

302.11

Alvos associados (humanos)

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)