883050-24-6
Chemical Structure
CCG-50014
- CAS No.: 883050-24-6
- Formula:C16H13FN2O2S
- Molecular Weight:316.35
IUPAC Name: 4-(4-fluorobenzyl)-2-(p-tolyl)-1,2,4-thiadiazolidine-3,5-dione
InChIKey: QUIIIYITNGOFEI-UHFFFAOYSA-N
SMILES: O=C(N1CC2=CC=C(F)C=C2)N(C3=CC=C(C)C=C3)SC1=O
Biological Activity: 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].
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CCG-50014 | 99.62% | 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. | ||||||||||||||||||||
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CCG-50014 (Standard) | ≥98% | CCG-50014 (Standard) is the analytical standard of CCG-50014. This product is intended for research and analytical applications. 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. | ||||||||||||||||||||
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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. [Content Brief]
- [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. [Content Brief]
