| 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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| Other Sizes |
Purity: ≥98%
| Targets |
RS-504393 targets the chemokine receptor CCR2, a G protein-coupled receptor that binds to monocyte chemoattractant protein-1 (MCP-1/CCL2). It acts as a potent and selective antagonist, blocking the interaction between MCP-1 and CCR2. This prevents the recruitment of monocytes and macrophages to sites of inflammation, reducing the inflammatory response and tissue damage.
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| ln Vitro |
At an IC50 of 330 nM, RS 504393 suppresses MCP-1-induced chemotaxis. β-hexosaminidase release caused by allergens was considerably reduced by RS 504393 treatment. When allergen priming is not present, MCP-1 triggers mast cell degranulation, which RS 504393 totally prevents [4].
In vitro, RS-504393 demonstrates high affinity for the CCR2 receptor in radioligand binding assays. It effectively inhibits MCP-1-induced chemotaxis in monocytic cell lines. Its selectivity for CCR2 over other chemokine receptors is confirmed in binding and functional assays. The compound shows potent activity in inhibiting calcium flux and chemotaxis. |
| ln Vivo |
Mice are subjected to precise stirring to progressively induce thermal hypersensitivity reactions using RS504393 (0.3-3 μg) and CCL2 [1]. The LPS-induced rise in BALF leukocyte count and total protein is inhibited by RS 504393 (5 mg/kg, iv). The LPS-induced upregulation of IL-1β, PAI-1 mRNA, and protein expression is strongly suppressed by RS504393. Significantly reducing renal injury, particularly extensive interstitial inflammatory disease mediated by reduced type I collagen synthesis in the UUO model, is achieved by RS504393. It also significantly inhibits LPS-induced pulmonary edema, fluid accumulation of edematous proteins, polymorphonuclear accumulation, and thickness thickening [2]. Fibrosis [3].
In vivo, RS-504393 has been evaluated in animal models of inflammatory diseases. In models of rheumatoid arthritis, it reduces joint inflammation and cartilage destruction. In models of atherosclerosis, it reduces lesion formation. Its ability to block monocyte infiltration and reduce inflammatory cytokine production is key to its efficacy. |
| Enzyme Assay |
In vitro receptor binding assays are used to measure the affinity of RS-504393 for CCR2. Competition binding assays with radiolabeled MCP-1 are performed using membrane preparations from cells expressing the receptor. The Ki value is determined, confirming its high affinity and selectivity.
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| Cell Assay |
In vitro functional assays for RS-504393 measure its ability to inhibit MCP-1-induced chemotaxis. Monocytic cell lines are used to assess the compound's effect on cell migration. Its ability to inhibit MCP-1-induced calcium flux is also measured. These assays confirm its functional antagonism at the CCR2 receptor.
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| Animal Protocol |
In vivo animal experiments for RS-504393 are conducted in models of rheumatoid arthritis, atherosclerosis, and other inflammatory diseases. Disease severity is assessed by measuring joint inflammation, plaque formation, or other relevant endpoints. The compound's effect on monocyte/macrophage infiltration and cytokine production is also evaluated.
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| ADME/Pharmacokinetics |
RS-504393 has a molecular weight of 464.56 and a molecular formula of C27H28N2O4. It is a solid powder, soluble in DMSO. It should be stored at -20°C for long-term storage. Its pharmacokinetic properties include moderate oral bioavailability and a half-life suitable for once or twice daily dosing in preclinical models.
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| Toxicity/Toxicokinetics |
The toxicological profile of RS-504393 is not extensively detailed. In preclinical studies, it has been generally well-tolerated. No significant toxicity has been reported. Its safety profile supports its continued investigation for inflammatory diseases.
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| References |
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| Additional Infomation |
6-Methyl-1'-[2-(5-methyl-2-phenyl-4-oxazolyl)ethyl]-2-spiro[1H-3,1-benzoxazine-4,4'-piperidin]one is a member of the 1,3-oxazole class of compounds.
RS-504393 is a potent and selective CCR2 antagonist. It has been investigated for the treatment of rheumatoid arthritis, multiple sclerosis, and atherosclerosis. By blocking the MCP-1/CCR2 axis, it reduces monocyte infiltration and inflammation. It is a research compound not yet approved for clinical use. |
| Molecular Formula |
C25H27N3O3
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|---|---|
| Molecular Weight |
417.5002
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| Exact Mass |
417.205
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| CAS # |
300816-15-3
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| PubChem CID |
9953769
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| Appearance |
White to off-white 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 |
4.87
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
31
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| Complexity |
630
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
ODNICNWASXKNNQ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C25H27N3O3/c1-17-8-9-22-20(16-17)25(31-24(29)27-22)11-14-28(15-12-25)13-10-21-18(2)30-23(26-21)19-6-4-3-5-7-19/h3-9,16H,10-15H2,1-2H3,(H,27,29)
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| Chemical Name |
6-Methyl-1'-[2-(5-methyl-2-phenyl-4-oxazolyl)ethyl]-spiro[4H-3,1-benzoxazine-4,4'-piperidin]-2(1H)-one
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| Synonyms |
RS504393 RS 504393 RS-504393.
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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 : ~10 mg/mL (~23.95 mM)
H2O : < 0.1 mg/mL |
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| Solubility (In Vivo) |
Solubility in Formulation 1: 31.25 mg/mL (74.85 mM) in 50% DMSO 15% EtOH + 35% PEG300 (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
Solubility in Formulation 2: ≥ 1.25 mg/mL (2.99 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 12.5 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. View More
Solubility in Formulation 3: ≥ 1.25 mg/mL (2.99 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 | 2.3952 mL | 11.9760 mL | 23.9521 mL | |
| 5 mM | 0.4790 mL | 2.3952 mL | 4.7904 mL | |
| 10 mM | 0.2395 mL | 1.1976 mL | 2.3952 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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