L 2-401
- CAS No.
- 883050-24-6
- Chemical Name:
- L 2-401
- Synonyms
- CS-563;L 2-401;CCG 50014;CCG50014;CCG 50014;CCG-50014 >=98% (HPLC);CCG-50014, 10 mM in DMSO;4-(4-Fluorobenzyl)-2-p-tolyl-1,2,4-thiadiazolidine-3,5-dione;4-[(4-Fluorophenyl)methyl]-2-(4-methylphenyl)-1,2,4-thiadiazolidine-3,5-dione;1,2,4-Thiadiazolidine-3,5-dione, 4-[(4-fluorophenyl)methyl]-2-(4-methylphenyl)-;Regulators of G-protein Signaling,Regulator of G-protein Signaling,RGS Protein,CCG-50014,inhibit,CCG50014,Inhibitor
- CBNumber:
- CB82657938
- Molecular Formula:
- C16H13FN2O2S
- Molecular Weight:
- 316.35
- MDL Number:
- MFCD00113783
- MOL File:
- 883050-24-6.mol
Density | 1.398±0.06 g/cm3 (20 ºC 760 Torr) |
---|---|
storage temp. | 2-8°C |
solubility | DMSO: soluble5mg/mL, clear (warmed) |
form | powder |
color | white to beige |
FDA UNII | RA72G28VE9 |
UNSPSC Code | 12352200 |
NACRES | NA.77 |
L 2-401 price More Price(23)
Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
---|---|---|---|---|---|---|---|
Sigma-Aldrich | SML0908 | CCG-50014 ≥98% (HPLC) | 883050-24-6 | 5mg | $122 | 2024-03-01 | Buy |
Sigma-Aldrich | SML0908 | CCG-50014 ≥98% (HPLC) | 883050-24-6 | 25mg | $382 | 2024-03-01 | Buy |
Cayman Chemical | 10802 | CCG-50014 ≥98% | 883050-24-6 | 1mg | $27 | 2024-03-01 | Buy |
Cayman Chemical | 10802 | CCG-50014 ≥98% | 883050-24-6 | 5mg | $93 | 2024-03-01 | Buy |
Cayman Chemical | 10802 | CCG-50014 ≥98% | 883050-24-6 | 10mg | $146 | 2024-03-01 | Buy |
L 2-401 Chemical Properties,Uses,Production
Description
CCG-50014 is an inhibitor of regulator of G protein signaling 4 (RGS4) (IC50 = 30 nM) and is > 20-fold selective for RGS4 over other RGS proteins. RGS proteins bind to the Gα subunits of activated heterotrimeric G proteins and accelerate the rate of GTP hydrolysis, acting as GTPase-activating proteins. CCG-50014 irreversibly binds and destabilizes RGS4 with no effect on Gα0, while blocking GTPase activity and Gα0-dependent translocation of RGS4 to the membrane.
Uses
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].
in vivo
CCG50014 (10, 30, or 100 nM) attenuates the nociceptive responses during the late phase in a dose-dependent manner[2].
IC 50
RGS4: 30 nM (IC50); RGS8: 11 μM (IC50); RGS16: 3.5 μM (IC50); RGS19: 0.12 μM (IC50)
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. DOI:10.1021/bi1019622
[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. DOI:10.1213/ANE.0000000000000607
L 2-401 Preparation Products And Raw materials
Raw materials
Preparation Products
Supplier | Tel | Country | ProdList | Advantage | |
---|---|---|---|---|---|
ATK CHEMICAL COMPANY LIMITED | +undefined-21-51877795 | ivan@atkchemical.com | China | 33024 | 60 |
BOC Sciences | +1-631-485-4226 | inquiry@bocsci.com | United States | 19552 | 58 |
TargetMol Chemicals Inc. | +1-781-999-5354 +1-00000000000 | marketing@targetmol.com | United States | 32159 | 58 |
Career Henan Chemica Co | +86-0371-86658258 +8613203830695 | laboratory@coreychem.com | China | 30231 | 58 |
InvivoChem | +1-708-310-1919 +1-13798911105 | sales@invivochem.cn | United States | 6391 | 58 |
TargetMol Chemicals Inc. | support@targetmol.com | United States | 38630 | 58 | |
Aladdin Scientific | tp@aladdinsci.com | United States | 57505 | 58 | |
Amadis Chemical Company Limited | 571-89925085 | sales@amadischem.com | China | 131957 | 58 |
Shanghai Aladdin Bio-Chem Technology Co.,LTD | 400-6206333 1316706386 | anhua.mao@aladdin-e.com | China | 25003 | 65 |
Shanghai Lollane Biological Technology Co.,Ltd. | 021-52996696,15000506266 15000506266 | China | 4601 | 55 |