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CCG-50014

  Cat. No.:  DC22819   Featured
Chemical Structure
883050-24-6
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Field of application
CCG-50014 is the most potent against the regulator of G-protein signaling protein type 4 (RGS4) (IC50 =30 nM) and is >20-fold selective for RGS4 over other RGS proteins. CCG-50014 binds covalently to the RGS, forming an adduct on two cysteine residues located in an allosteric regulatory site. CCG50014, reduces nociceptive responses and enhances opioid-mediated analgesic effects in the mouse formalin test.
Chemicals PropertiesBiological activity COA & MSDSRelated productsDatasheet
Cas No.: 883050-24-6
Chemical Name: 4-[(4-Fluorophenyl)methyl]-2-(4-methylphenyl)-1,2,4-thiadiazolidine-3,5-dione
Synonyms: CCG50014;CCG 50014
SMILES: FC1C=CC(CN2C(=O)SN(C3C=CC(C)=CC=3)C2=O)=CC=1
Formula: C16H13FN2O2S
M.Wt: 316.35
Purity: >98%
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description: CCG-50014 is the most potent against the regulator of G-protein signaling protein type 4 (RGS4) (IC50 =30 nM) and is >20-fold selective for RGS4 over other RGS proteins. CCG-50014 binds covalently to the RGS, forming an adduct on two cysteine residues located in an allosteric regulatory site[1]. CCG50014, reduces nociceptive responses and enhances opioid-mediated analgesic effects in the mouse formalin test[2].
Target: RGS4:30 nM (IC50) RGS8:11 μM (IC50) RGS16:3.5 μM (IC50) RGS19:0.12 μM (IC50)
In Vivo: CCG50014 (10, 30, or 100 nM) attenuates the nociceptive responses during the late phase in a dose-dependent manner[2].
References: [1]. Blazer LL, et al. A nanomolar-potency small molecule inhibitor of regulator of G-protein signaling proteins. Biochemistry. 2011 Apr 19;50(15):3181-92. [2]. Yoon SY, et al. Intrathecal RGS4 inhibitor, CCG50014, reduces nociceptive responses and enhances opioid-mediated analgesic effects in the mouse formalin test. Anesth Analg. 2015 Mar;120(3):671-7.
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
2018-0101
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