CCG 50014

Names

[ Name ]:
CCG 50014

[Synonym ]:
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

Biological Activity

[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]:

Research Areas >> Inflammation/Immunology

Signaling Pathways >> GPCR/G Protein >> RGS Protein

[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.

Chemical & Physical Properties

[ Molecular Formula ]:
C₁₆H₁₃FN₂O₂S

[ Molecular Weight ]:
316.35000

[ Exact Mass ]:
316.06800

[ PSA ]:
72.24000

[ LogP ]:
2.55650

[ Storage condition ]:
-20℃

MSDS

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Safety Information

[ RIDADR ]:
NONH for all modes of transport

Synthetic Route

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Precursor & DownStream

Precursor

DownStream

Related Compounds

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