| Size | Price | Stock | Qty |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
Purity: ≥98%
| Targets |
CCG-63808 targets RGS proteins, specifically RGS4 and other members of the RGS family. It acts as a reversible inhibitor with an IC50 of 1.4 μM for RGS4. By inhibiting RGS proteins, the compound prolongs the GTP-bound state of Gα subunits, thereby enhancing G protein-coupled receptor signaling.
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| ln Vitro |
In vitro, CCG-63808 inhibits RGS protein function. The compound reversibly binds to RGS4 and other RGS family members, blocking their GTPase-accelerating activity. This results in enhanced and prolonged signaling through G protein-coupled receptors that are normally desensitized by RGS proteins.
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| ln Vivo |
Cellular assays are used to evaluate the compound's ability to enhance GPCR signaling by inhibiting RGS proteins. In cells expressing GPCRs and RGS proteins, CCG-63808 treatment leads to enhanced and prolonged receptor-mediated signaling.
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| Enzyme Assay |
For in vitro enzyme assays, recombinant RGS4 protein is incubated with Gα subunits and GTP. GTPase activity is measured by monitoring the hydrolysis of GTP to GDP using radioactive or fluorescence-based assays. CCG-63808 is tested at various concentrations to determine its IC50 for RGS4 inhibition.
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| Cell Assay |
Cellular assays are performed in HEK-293 cells or other cell lines expressing GPCRs and RGS proteins. Cells are treated with CCG-63808, and GPCR-mediated signaling is assessed by measuring downstream effectors such as calcium mobilization, cAMP accumulation, or MAPK activation. Enhanced signaling in the presence of the inhibitor confirms RGS inhibition.
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| Animal Protocol |
In vivo studies of CCG-63808 are limited as the compound is primarily used as a research tool. Animal models may be used to evaluate the effects of RGS inhibition on GPCR-mediated physiological responses. The compound's ability to modulate signaling pathways in vivo has been characterized in pharmacological studies.
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| ADME/Pharmacokinetics |
CCG-63808 (molecular weight 454.48) is a small-molecule RGS inhibitor. It is soluble in DMSO (1 mg/mL, 2.20 mM) with sonication. The compound is typically stored at -20°C or -80°C and formulated in DMSO for in vitro studies.
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| Toxicity/Toxicokinetics |
Preclinical toxicity studies of CCG-63808 have been limited as the compound is used primarily for research purposes. No significant toxicity has been reported. The compound's safety profile supports its use as a research tool for studying RGS protein function and GPCR signaling.
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| References | |
| Additional Infomation |
CCG-63808 is a reversible, allosteric small-molecule inhibitor of regulator of G protein signaling proteins. Its mechanism involves binding to RGS proteins and blocking their GTPase-accelerating activity, thereby prolonging the GTP-bound state of Gα subunits and enhancing GPCR signaling. The compound is used as a research tool to study the role of RGS proteins in GPCR signaling and to explore the therapeutic potential of RGS inhibitors.
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| Molecular Formula |
C25H15N4O2FS
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|---|---|
| Molecular Weight |
454.4756
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| Exact Mass |
454.09
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| Elemental Analysis |
C, 66.07; H, 3.33; F, 4.18; N, 12.33; O, 7.04; S, 7.05
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| CAS # |
620113-73-7
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| PubChem CID |
5948316
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| Appearance |
Pink to red solid powder
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| Density |
1.37
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| Boiling Point |
534.5ºC at 760 mmHg
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| Flash Point |
277ºC
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| Index of Refraction |
1.695
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| LogP |
5.608
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
33
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| Complexity |
1030
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| Defined Atom Stereocenter Count |
0
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| SMILES |
N#C/C(C1=NC2=CC=CC=C2S1)=C\C3=C(N=C4C(C)=CC=CN4C3=O)OC5=CC=C(C=C5)F
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| InChi Key |
IPZHFKHGSYRBNT-DTQAZKPQSA-N
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| InChi Code |
InChI=1S/C25H15FN4O2S/c1-15-5-4-12-30-22(15)29-23(32-18-10-8-17(26)9-11-18)19(25(30)31)13-16(14-27)24-28-20-6-2-3-7-21(20)33-24/h2-13H,1H3/b16-13+
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| Chemical Name |
(E)-2-(1,3-benzothiazol-2-yl)-3-[2-(4-fluorophenoxy)-9-methyl-4-oxopyrido[1,2-a]pyrimidin-3-yl]prop-2-enenitrile
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| Synonyms |
CCG-63808; CCG63808; CCG 63808
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: ~1 mg/mL (~2.2 mM)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.2003 mL | 11.0016 mL | 22.0032 mL | |
| 5 mM | 0.4401 mL | 2.2003 mL | 4.4006 mL | |
| 10 mM | 0.2200 mL | 1.1002 mL | 2.2003 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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