[CAS NO. 883050-24-6] CCG-50014
PRODUCTS SPECIFICATIONS [883050-24-6]
DESCRIPTION [883050-24-6]
Overview
| MDL | MFCD00113783 |
|---|---|
| Molecular Weight | 316.35 |
| Molecular Formula | C16H13FN2O2S |
| SMILES | O=C(N1CC2=CC=C(F)C=C2)N(C3=CC=C(C)C=C3)SC1=O |
1 Publications Citing Use of MCE
Summary
CCG-50014 is the most potent against the regulator of G-protein signaling protein type 4 (RGS4) ( IC 50 =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] .
IC50 & Target
|
RGS4 30 nM (IC 50 ) |
RGS8 11 μM (IC 50 ) |
RGS16 3.5 μM (IC 50 ) |
RGS19 0.12 μM (IC 50 ) |
In Vivo
CCG50014 (10, 30, or 100 nM) attenuates the nociceptive responses during the late phase in a dose-dependent manner
[2]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 62.5 mg/mL ( 197.57 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 3.1611 mL | 15.8053 mL | 31.6106 mL |
| 5 mM | 0.6322 mL | 3.1611 mL | 6.3221 mL |
| 10 mM | 0.3161 mL | 1.5805 mL | 3.1611 mL |
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.