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| Targets |
The primary target of 0990CL is the heterotrimeric Gαi subunit of G proteins. The compound directly interacts with Gαi in its GDP-bound state, inhibiting its function. By blocking Gαi activity, 0990CL prevents the inhibition of adenylyl cyclase, thereby blocking α2AR-mediated regulation of cAMP levels. This mechanism makes the compound a valuable tool for studying GPCR signaling pathways that involve Gαi-mediated inhibition of cAMP production.
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| ln Vitro |
In HEK293 GloSensor cells, 0990CL (100 nM-1 μM; 24 hours) increases α2AR/Gαi-mediated cAMP levels that are induced by Fsk and UK14304. A restoration of 31% of the cAMP decrease is possible at a dose of 100 nM[1]. 0990CL (30 μM; 30 minutes pretreatment) demonstrated higher Gαi1 selectivity than Gαq. It has a maximal endpoint fluorescence decrease of 38±8% and 10%, respectively, and shows selectivity for Gαi and Gαq [1].
In vitro, 0990CL demonstrates specific inhibition of Gαi subunits. The compound directly interacts with purified Gαi in its GDP-bound state. In cellular models, low concentrations of 0990CL partially restore cAMP levels that are suppressed by Gαi-mediated signaling. However, at higher concentrations (10 μM), the compound begins to have a negative impact on cell viability. The compound's specificity for Gαi over other G protein subunits is a key feature of its pharmacological profile. |
| ln Vivo |
In vivo data for 0990CL are not extensively reported in the available literature. As a specific inhibitor of Gαi subunits, the compound has potential for in vivo applications in studying the role of Gαi-mediated signaling in various physiological and pathophysiological processes. However, specific in vivo efficacy data, including animal models, dosing regimens, and pharmacokinetic-pharmacodynamic relationships, are not detailed in the available sources.
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| Enzyme Assay |
In vitro receptor binding assays for 0990CL are not typically performed, as the compound targets the Gαi protein rather than a cell surface receptor. Instead, the compound's activity is assessed in biochemical assays measuring its interaction with purified Gαi proteins. For example, the compound is incubated with purified Gαi in its GDP-bound state, and binding is assessed using techniques such as surface plasmon resonance or fluorescence-based assays. The compound's ability to inhibit Gαi function is also assessed in functional assays.
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| Cell Assay |
Cellular assays for 0990CL are performed in cells expressing Gαi-coupled receptors, such as the α2-adrenergic receptor. Cells are treated with 0990CL, and the effects on cAMP levels are measured. The compound's ability to block α2AR-mediated regulation of cAMP is assessed by measuring cAMP levels in the presence of an α2AR agonist. At low concentrations, 0990CL partially restores cAMP levels, while at high concentrations (10 μM), it begins to negatively affect cell viability.
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| Animal Protocol |
In vivo animal studies with 0990CL are not extensively documented in the available literature. Based on its inhibition of Gαi signaling, potential in vivo models could include studies of GPCR-mediated physiological responses, such as cardiovascular function, pain, or neurological processes. However, specific protocols are not detailed in the available sources. The compound is intended for laboratory research use only.
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| ADME/Pharmacokinetics |
0990CL has a molecular weight of 343.42. It is typically dissolved in DMSO for in vitro studies. The compound is stable when stored as a powder at -20°C. However, detailed pharmacokinetic parameters such as absorption, distribution, metabolism, excretion, half-life, and bioavailability are not available in the literature for this research compound.
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| Toxicity/Toxicokinetics |
At higher concentrations (10 μM), 0990CL begins to have a negative impact on cell viability, indicating potential cytotoxicity. However, comprehensive toxicology data for this compound are not extensively reported. The compound is classified as a research-use-only chemical and is not intended for human consumption. Specific toxicological data, including acute toxicity, genotoxicity, and target organ effects, are not reported in the available literature.
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| References | |
| Additional Infomation |
0990CL is a research-grade compound not approved for clinical use. Its primary application is as a pharmacological tool for studying G protein-coupled receptor (GPCR) signaling, particularly the role of Gαi subunits in cAMP regulation. The compound is used to investigate the mechanisms of Gαi-mediated signaling and to study the function of Gαi-coupled receptors such as the α2-adrenergic receptor. It is also used as a tool to validate the role of Gαi in various cellular processes.
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| Molecular Formula |
C21H21N5
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| Molecular Weight |
343.424943685532
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| Exact Mass |
343.179
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| CAS # |
511514-03-7
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| PubChem CID |
950615
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| Appearance |
Light yellow to yellow solid powder
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| LogP |
3.7
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
26
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| Complexity |
561
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| Defined Atom Stereocenter Count |
0
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| SMILES |
N1=C(NC2N=C3C=CC=CC3=C(C3C=CC=CC=3)N=2)NC(C)=CC1(C)C
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| InChi Key |
DXICUHJLOMNKOU-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C21H21N5/c1-14-13-21(2,3)26-20(22-14)25-19-23-17-12-8-7-11-16(17)18(24-19)15-9-5-4-6-10-15/h4-13H,1-3H3,(H2,22,23,24,25,26)
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| Chemical Name |
(4-Phenyl-quinazolin-2-yl)-(4,6,6-trimethyl-1,6-dihydro-pyrimidin-2-yl)-amine
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| Synonyms |
0990-CL 0990 CL 0990CL
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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 : ~250 mg/mL (~727.97 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.28 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 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: ≥ 2.5 mg/mL (7.28 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 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: ≥ 2.5 mg/mL (7.28 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 | 2.9118 mL | 14.5590 mL | 29.1180 mL | |
| 5 mM | 0.5824 mL | 2.9118 mL | 5.8236 mL | |
| 10 mM | 0.2912 mL | 1.4559 mL | 2.9118 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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