| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| 25mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| Other Sizes |
Purity: ≥98%
| Targets |
CGS 15943 targets adenosine receptors, specifically the A₁, A₂A, and A₂B subtypes. Adenosine receptors are G protein-coupled receptors involved in numerous physiological processes including neurotransmission, cardiovascular function, and inflammation. By blocking adenosine receptors, CGS 15943 inhibits adenosine-mediated effects such as vasodilation, neurotransmitter release modulation, and immune suppression. The compound is a non-xanthine antagonist with high affinity for all three receptor subtypes.
|
|---|---|
| ln Vitro |
CGS 15943 slightly inhibits p110δ with an IC50 of 8.47 μM and suppresses the intermittent activity of class IB PI3K isoform p110γ with an IC50 of 1.1 μM [3]. HLF and SK-Hep are inhibited by CGS 15943 (0–20 μM; 72 hours). CGS 15943 (0 -20 μM; 24 hours) inhibits the development of HepG2 and PLC-PRF-5 cells [3] as well as the phosphorylation of Akt residues Ser473 and Thr308 in HLF and Sk-Hep-1 cells [3].
In vitro, CGS 15943 demonstrates potent adenosine receptor antagonism with high affinity for A₁, A₂A, and A₂B receptors. Specific Ki values for each receptor subtype are documented in the literature. The compound shows activity in receptor binding assays and functional assays measuring cAMP accumulation or other second messenger responses. It is soluble in DMSO and other organic solvents. The compound's potency and selectivity have been characterized in various cell-based and biochemical assays. |
| ln Vivo |
In vivo, CGS 15943 has been studied in animal models of neurological and cardiovascular disorders. Adenosine receptor antagonists like CGS 15943 have been investigated for their potential to enhance cognition, improve motor function, and modulate cardiovascular responses. The compound's effects are mediated through blockade of adenosine-mediated inhibition of neurotransmitter release and modulation of vascular tone. Further studies are needed to fully characterize its therapeutic potential.
|
| Enzyme Assay |
Adenosine receptor binding assays are performed using membrane preparations from cells expressing human adenosine receptors or from brain tissue. Radioligand displacement assays use [³H]-DPCPX (A₁), [³H]-CGS21680 (A₂A), or other appropriate radiolabeled ligands. CGS 15943 is tested at various concentrations, and Ki values are calculated from competition binding curves. Functional assays measure inhibition of adenosine-induced cAMP accumulation or calcium flux.
|
| Cell Assay |
Cell viability assay [3]
Cell Types: HLF, SK-Hep-1, HepG2 and PLC-PRF-5 Cell Tested Concentrations: 0 μM; ]. 1μM; 5μM; 10μM; 20 μM Incubation Duration: 24 hrs (hours) Experimental Results: Inhibited the growth of four different HCC cell lines. Western Blot Analysis[3] Cell Types: HLF and Sk-Hep-1 cells Tested Concentrations: 0 μM; 1μM; 5μM; 10μM; 20 μM Incubation Duration: 24 hrs (hours) Experimental Results: Inhibition of PI3K/ in HLF and Sk-Hep-1 cells Akt pathway In vitro cellular assays use cell lines expressing adenosine receptors. Cells are treated with CGS 15943 at various concentrations. Receptor activation is measured by second messenger assays (cAMP accumulation, calcium flux). Antagonist activity is assessed by measuring inhibition of agonist-induced responses. Cell viability is assessed by MTT assay. The compound is dissolved in DMSO for stock solutions and diluted in culture media for cellular experiments. |
| Animal Protocol |
In vivo efficacy is evaluated in animal models of neurological disorders (e.g., Parkinson's disease, Alzheimer's disease, epilepsy) and cardiovascular disorders. CGS 15943 is administered orally or intraperitoneally. Behavioral assessments include motor function, cognition tests, and seizure susceptibility. Cardiovascular parameters include blood pressure, heart rate, and vascular responses. Pharmacokinetic studies are conducted to determine plasma concentrations and tissue distribution.
|
| ADME/Pharmacokinetics |
CGS 15943 is a non-xanthine adenosine receptor antagonist. Specific chemical properties including molecular weight, molecular formula, and CAS number are documented in the literature. The compound is typically stored at -20°C and protected from light. It is soluble in DMSO and other organic solvents. Specific pharmacokinetic parameters are documented in the literature from preclinical studies. The compound is metabolized in the liver and excreted primarily in urine.
|
| Toxicity/Toxicokinetics |
Specific toxicity data for CGS 15943 are documented in preclinical studies. As an adenosine receptor antagonist, its safety profile has been characterized in animal models. Common adverse effects may include cardiovascular effects (tachycardia, hypertension) and central nervous system effects (insomnia, anxiety) due to adenosine receptor blockade. Standard laboratory safety precautions should be followed when handling this compound. It is intended for research use only and not for human therapeutic applications.
|
| References |
|
| Additional Infomation |
CGS 15943 belongs to the triazoloquinazoline class of compounds, with the structure [1,2,4]triazolo[1,5-c]quinazoline, substituted at positions 2, 5, and 9 with furan-2-yl, amino, and chlorine groups, respectively. It is a potent antagonist of adenosine A1 and adenosine A2A receptors. It functions as an adenosine A1 receptor antagonist, an adenosine A2A receptor antagonist, a central nervous system stimulant, and an antitumor drug. It is a triazoloquinazoline compound, an organochlorine compound, a furan compound, a biaryl compound, an aromatic amine compound, and a primary amino compound.
CGS 15943 is a potent, non-xanthine adenosine receptor antagonist with high affinity for A₁, A₂A, and A₂B adenosine receptors. It is used as a research tool to study adenosine receptor function and the role of adenosine in various physiological and pathological processes including neurotransmission, cardiovascular function, and inflammation. The compound has been investigated for potential therapeutic applications in neurological and cardiovascular disorders. It is commercially available for research purposes only. |
| Molecular Formula |
C13H8CLN5O
|
|---|---|
| Molecular Weight |
285.68852
|
| Exact Mass |
285.042
|
| CAS # |
104615-18-1
|
| PubChem CID |
2690
|
| Appearance |
White to off-white solid powder
|
| Density |
1.72 g/cm3
|
| Boiling Point |
566.6ºC at 760 mmHg
|
| Melting Point |
278-279 °C
|
| Flash Point |
296.5ºC
|
| Vapour Pressure |
7.4E-13mmHg at 25°C
|
| Index of Refraction |
1.84
|
| LogP |
3.354
|
| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
5
|
| Rotatable Bond Count |
1
|
| Heavy Atom Count |
20
|
| Complexity |
373
|
| Defined Atom Stereocenter Count |
0
|
| InChi Key |
MSJODEOZODDVGW-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C13H8ClN5O/c14-7-3-4-9-8(6-7)12-17-11(10-2-1-5-20-10)18-19(12)13(15)16-9/h1-6H,(H2,15,16)
|
| Chemical Name |
9-chloro-2-furan-2-yl-[1,2,4]triazolo[1,5-c]quinazolin-5-amine
|
| Synonyms |
CGS 15943 CGS15943 CGS-15943.
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| Solubility (In Vitro) |
DMSO : ~12.22 mg/mL (~42.77 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 1.22 mg/mL (4.27 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 12.2 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 1.22 mg/mL (4.27 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 12.2 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 1.22 mg/mL (4.27 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.5003 mL | 17.5015 mL | 35.0030 mL | |
| 5 mM | 0.7001 mL | 3.5003 mL | 7.0006 mL | |
| 10 mM | 0.3500 mL | 1.7501 mL | 3.5003 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
COA