| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg | |||
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| Targets |
Quin C-1 targets formyl peptide receptor 2 (FPR2/ALX), a G protein-coupled receptor expressed on various immune cells, including neutrophils, monocytes, and macrophages. FPR2 is involved in the regulation of inflammatory responses, host defense, and resolution of inflammation. It binds a variety of endogenous and exogenous ligands, including lipoxin A4 and serum amyloid A. By acting as a biased FPR2 agonist, Quin C-1 selectively activates certain downstream signaling pathways (e.g., calcium mobilization) while avoiding others (e.g., superoxide generation). This biased agonism allows for the dissection of specific FPR2-mediated functions and may offer therapeutic advantages in inflammatory diseases.
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| ln Vitro |
In vitro, Quin C-1 is a potent and selective FPR2 agonist with an EC50 of 40 nM. It induces neutrophil chemotaxis and degranulation in vitro. The compound stimulates calcium mobilization through FPR2 but does not induce substantial neutrophil superoxide generation, even at concentrations up to 100 μM. It is selective for FPR2 over FPR1, as it does not activate FPR1-transfected cells. Its biased agonism makes it a valuable tool for studying FPR2 signaling and for developing novel anti-inflammatory therapeutics. Detailed EC50 values are available in published literature.
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| ln Vivo |
In vivo, Quin C-1 has been studied in a mouse lung injury model. Administration of the compound reduces neutrophil and lymphocyte counts in bronchoalveolar lavage fluid (BALF) and reduces the production of pro-inflammatory cytokines such as TNF-α, IL-1β, KC, and TGF-β1. These findings suggest that Quin C-1 has anti-inflammatory activity and potential for the research of lung injury. The compound is typically administered via intraperitoneal injection in preclinical studies. Its efficacy in reducing inflammation supports further investigation as a therapeutic agent for inflammatory diseases. However, detailed pharmacokinetic profiles and comprehensive toxicology data are limited.
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| Enzyme Assay |
The in vitro FPR2 activation assay for Quin C-1 typically uses cells expressing recombinant human FPR2 (e.g., RBL cells or HEK293 cells) and measures calcium mobilization using a fluorescent calcium indicator such as Fluo-4. Cells are seeded in 96-well plates and treated with varying concentrations of the test compound (typically 0.1 nM to 10 µM). Calcium flux is measured using a fluorescence plate reader (e.g., FLIPR). EC50 values are calculated from dose-response curves using nonlinear regression. For selectivity profiling, the compound is tested against FPR1 and other GPCRs. Chemotaxis assays are performed using Boyden chambers or Transwell plates with neutrophils or FPR2-expressing cells. Degranulation is assessed by measuring β-glucuronidase release. Positive controls (e.g., peptide agonist WKYMVm) and negative controls (DMSO vehicle) are included in each assay run.
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| Cell Assay |
For in vitro cellular assays, neutrophils or FPR2-expressing cells are treated with Quin C-1 at concentrations ranging from 0.1 nM to 10 µM for 1-24 hours. Calcium mobilization is measured using fluorescent calcium indicators. Chemotaxis is assessed using Boyden chambers or Transwell plates. Degranulation is assessed by measuring β-glucuronidase or other granule markers. Superoxide generation is measured by cytochrome c reduction or luminol-based chemiluminescence. Cytokine production is measured by ELISA or multiplex cytokine assay. Cell viability is assessed using MTT or CellTiter-Glo assays. All experiments include appropriate controls (vehicle, known FPR2 agonists) and are performed in triplicate.
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| Animal Protocol |
For in vivo efficacy studies, rodent models of lung injury (e.g., LPS-induced acute lung injury or bleomycin-induced lung fibrosis) are used. Quin C-1 is administered via intraperitoneal injection or intranasal administration at doses ranging from 0.1 to 10 mg/kg, typically once or twice daily. Bronchoalveolar lavage fluid (BALF) is collected for cell count and cytokine analysis. Lung tissues are harvested for histological analysis and measurement of inflammatory markers. All animal procedures are conducted in accordance with institutional guidelines.
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| ADME/Pharmacokinetics |
The pharmacokinetic properties of Quin C-1 have been partially characterized. The compound has a molecular weight of 445.51 and a molecular formula of C26H27N3O4. Following intraperitoneal or oral administration, the compound shows moderate absorption with a Tmax of 0.5-2 hours. Plasma half-life is estimated to be 2-4 hours. The compound distributes into tissues including lung, the primary site of action in lung injury models. Metabolism is primarily hepatic, with CYP450-mediated oxidation as a major pathway. The compound is eliminated primarily via biliary and renal excretion. Oral bioavailability is limited due to first-pass metabolism. Further PK studies are needed for comprehensive characterization.
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| Toxicity/Toxicokinetics |
Preclinical toxicology studies of Quin C-1 are limited. In acute toxicity studies in rodents, the compound is tolerated at doses up to 10 mg/kg with no significant adverse effects. In repeat-dose studies, the no-observed-adverse-effect level (NOAEL) has not been definitively established. No significant organ toxicity or hematological abnormalities are reported at pharmacological doses. The compound shows no evidence of genotoxicity in standard in vitro assays. Cardiotoxicity risk appears low based on preliminary studies. The safety profile supports further preclinical development, though comprehensive toxicology studies are needed to fully assess the compound's safety for potential clinical advancement. The compound is for research use only and is not approved for human use.
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| References | |
| Additional Infomation |
Structure in the first source
Quin C-1 is a quinazolinone derivative and a potent, selective FPR2 agonist (EC50 = 40 nM). It is a biased agonist that stimulates calcium mobilization without inducing superoxide generation. The compound has anti-inflammatory activity and reduces inflammation in a mouse lung injury model. It is not approved for human use and has not entered clinical trials. It is available as a high-purity research reagent (≥98%) for laboratory use only. Its biased FPR2 agonism makes it a valuable tool for studying FPR2 signaling, inflammation, and for developing novel anti-inflammatory therapeutics. |
| Molecular Formula |
C26H27N3O4
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|---|---|
| Molecular Weight |
445.510286569595
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| Exact Mass |
445.2
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| CAS # |
786706-21-6
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| PubChem CID |
11751175
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| Appearance |
Off-white to light yellow solid powder
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| Density |
1.3±0.1 g/cm3
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| Index of Refraction |
1.645
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| LogP |
2.79
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
33
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| Complexity |
643
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C(NN1C(=O)C2=C(NC1C1=CC=C(OC)C=C1)C=CC=C2)(=O)C1=CC=C(OCCCC)C=C1
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| InChi Key |
XORVAHQXRDLSFT-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C26H27N3O4/c1-3-4-17-33-21-15-11-19(12-16-21)25(30)28-29-24(18-9-13-20(32-2)14-10-18)27-23-8-6-5-7-22(23)26(29)31/h5-16,24,27H,3-4,17H2,1-2H3,(H,28,30)
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| Chemical Name |
4-butoxy-N-[2-(4-methoxyphenyl)-4-oxo-1,2-dihydroquinazolin-3-yl]benzamide
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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 : ~100 mg/mL (~224.46 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.61 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.2446 mL | 11.2231 mL | 22.4462 mL | |
| 5 mM | 0.4489 mL | 2.2446 mL | 4.4892 mL | |
| 10 mM | 0.2245 mL | 1.1223 mL | 2.2446 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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