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| 25mg |
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Purity: ≥98%
RS-504393 is a potent and highly selective CCR2 chemokine receptor antagonist with IC50s of 98 nM and > 100 µM for inhibition of human recombinant CCR2b and CCR1 receptors respectively. It inhibits MCP-1 chemotaxis (IC50 = 330 nM) and ischemia-reperfusion injury in kidneys.
| 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].
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| 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].
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| References |
[1]. Baamonde, Ana., et al. Involvement of glutamate NMDA and AMPA receptors, glial cells and IL-1β in the spinal hyperalgesia evoked by the chemokine CCL2 in mice. Neuroscience Letters (2011), 502(3), 178-181.
[2]. Yang, Dong., et al. Roles of CC chemokine receptors (CCRs) on lipopolysaccharide-induced acute lung injury. Respiratory Physiology & Neurobiology (2010), 170(3), 253-259. [3]. Kitagawa, Kiyoki., et al. Blockade of CCR2 ameliorates progressive fibrosis in kidney. American Journal of Pathology (2004), 165(1), 237-246. [4]. Tominaga T, et al. Blocking mast cell-mediated type I hypersensitivity in experimental allergic conjunctivitis by monocyte chemoattractant protein-1/CCR2. Invest Ophthalmol Vis Sci. 2009 Nov;50(11):5181-8. [5]. Mirzadegan T, et al. Identification of the binding site for a novel class of CCR2b chemokine receptor antagonists: binding to a common chemokine receptor motif within the helical bundle. J Biol Chem. 2000 Aug 18;275(33):25562-71 |
| Molecular Formula |
C25H27N3O3
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|---|---|
| Molecular Weight |
417.5002
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| CAS # |
300816-15-3
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| SMILES |
CC1=CC2=C(C=C1)NC(=O)OC23CCN(CC3)CCC4=C(OC(=N4)C5=CC=CC=C5)C
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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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| 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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