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883050-24-6

883050-24-6 structure
883050-24-6 structure
  • Name: CCG 50014
  • Chemical Name: 4-[(4-fluorophenyl)methyl]-2-(4-methylphenyl)-1,2,4-thiadiazolidine-3,5-dione
  • CAS Number: 883050-24-6
  • Molecular Formula: C16H13FN2O2S
  • Molecular Weight: 316.35000
  • Catalog: Signaling Pathways GPCR/G Protein RGS Protein
  • Create Date: 2017-03-02 04:16:37
  • Modify Date: 2024-04-05 11:36:35
  • 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].

Name 4-[(4-fluorophenyl)methyl]-2-(4-methylphenyl)-1,2,4-thiadiazolidine-3,5-dione
Synonyms 2-p-tolyl-4-(4-fluorobenzyl)-1,2,4-thiadiazolidine-3,5-dione
UNII-RA72G28VE9
4-((4-fluorophenyl)methyl)-2-(4-methylphenyl)-1,2,4-thiadiazolidine-3,5-dione
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].
Related Catalog
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.

Molecular Formula C16H13FN2O2S
Molecular Weight 316.35000
Exact Mass 316.06800
PSA 72.24000
LogP 2.55650
Storage condition -20℃
RIDADR NONH for all modes of transport

~39%

883050-24-6 structure

883050-24-6

Literature: THE REGENTS OF THE UNIVERSITY OF MICHIGAN; Neubig, Richard; Blazer, Levi; Husbands, Stephen; Larsen, Scott; Traynor, John Patent: US2012/277273 A1, 2012 ; Location in patent: Page/Page column 22-23 ;
Precursor  2

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