[CAS NO. 620112-78-9] CCG-63802
PRODUCTS SPECIFICATIONS [620112-78-9]
DESCRIPTION [620112-78-9]
Overview
| MDL | MFCD04190628 |
|---|---|
| Molecular Weight | 450.51 |
| Molecular Formula | C26H18N4O2S |
| SMILES | N#C/C(C1=NC2=CC=CC=C2S1)=C\C3=C(N=C4C(C)=CC=CN4C3=O)OC5=CC=CC(C)=C5 |
1 Publications Citing Use of MCE
Summary
IC50 & Target
|
RGS4 1.9 μM (IC 50 ) |
In Vitro
CCG-63802 (5 μM) inhibits regulators of G-protein signaling (RGS) proteins in the presence of BK (bradykinin) and 8-Br-cGMP (membrane-permeable analogue of cGMP), HEK-293 cells start to depolarize again [2] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
CCG-63802 (0.05 mg/kg; intratracheal administration; once per week; 90 days) reduces RGS4 protein expression, leading to partially abrogate the attenuating effect of PGZ on airway inflammation, hyperresponsiveness (AHR), and remodeling [3] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: | Forty female BALB/c mice aged 6-8 week old [3] |
| Dosage: | 0.05 mg/kg |
| Administration: | Intratracheal administration; once per week; 90 days |
| Result: | CCG 63802 treatment in OVA +PGZ + CCG group significantly reduced RGS4 protein expression compared to OVA + PGZ group (P < 0.05) |
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 : 1.67 mg/mL ( 3.71 mM ; Need ultrasonic and warming)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.2197 mL | 11.0985 mL | 22.1971 mL |
| 5 mM | --- | --- | --- |
| 10 mM | --- | --- | --- |
-
1.
CCG-63802 is dissolved in DMSO and diluted with 0.9% NaCl [3] .
References
- [1] Levi L Blazer, et al. Reversible, allosteric small-molecule inhibitors of regulator of G protein signaling proteins. Mol Pharmacol. 2010 Sep;78(3):524-33.
- [2] Marina Dobrivojević, et al. Interaction between bradykinin and natriuretic peptides via RGS protein activation in HEK-293 cells. Am J Physiol Cell Physiol. 2012 Dec 15;303(12):C1260-8.
- [3] Xia Meng, et al. PPARγ Agonist PGZ Attenuates OVA-Induced Airway Inflammation and Airway Remodeling via RGS4 Signaling in Mouse Model. Inflammation. 2018 Dec;41(6):2079-2089.
