3-(2-carboxy-4,6-dichloroindol-3-yl)propionic acid

Name	2-Carboxy-4,6-dichloro-1H-indole-3-propionic acid
Synonyms	CS-1105 MDL29951 MDL-29951 2-Carboxy-4,6-dichloro-1H-indole-3-propionic acid 2-Carboxy-4,6-dichloro-1H-indole-3-propanoic acid 3-(2-carboxy-4,6-dichloroindol-3-yl)propionic acid 3-(2-carboxyethyl)-4,6-dichloro-1H-indole-2-carboxylic acid MDL-29951 2-Carboxy-4,6-dichloro-1H-indole-3-propanoic acid
CAS	130798-51-5
EINECS	200-256-5

Molecular Formula	C12H9Cl2NO4
Molar Mass	302.11
Density	1.657±0.06 g/cm3(Predicted)
Melting Point	273-280℃
Boling Point	582.5±45.0 °C(Predicted)
Solubility	Soluble in DMSO (up to 15 mg/ml with warming) or in Ethanol (up to 10 mg/ml).
Appearance	solid
Color	Off-white
pKa	4.04±0.30(Predicted)
Storage Condition	2-8°C(protect from light)
Stability	Stable for 2 years from date of pruchase as supplied. Solutions in DMSO or ethanol may be stored at -20° for up to 3 months.
In vitro study	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.

Last Update：2024-01-02 23:10:35

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