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R243 (R-243) is a novel and potent inhibitor of CCR8 signaling with antinociceptive and anti-inflammatory activity. It inhibits CCR8 signaling and chemotaxis, inhibits CCL1-induced Ca2+ flux and CCL1-driven peritoneal macrophages aggregation. It also reduced secretion of cytokines such as TNF-α, IL-6, and most strikingly IL-10 from WT PMφ (peritoneal macrophages), but not BMMφ (bone marrow-derived macrophages).
| ln Vitro |
CCL1-induced Ca2+ flow and CCL1-driven peritoneal macrophage accumulation are antagonistic to CCR8 in R243 [1]. R243 reduces the amount of TNF-α, IL-6, and IL-10 that wild-type peritoneal macrophages (WT PMφ) secrete [1]. After lipopolysaccharide (LPS) treatment, R243-treated WT PMφ demonstrated reduction of NF-κB signaling and c-jun N-terminal kinase activity compared to WT PMφ [1].
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| ln Vivo |
R243 (0.1-1 mg/kg; intraperitoneal injection; once; male Swiss mice) therapy decreased CCL1-induced analgesia in a dose-dependent manner [2].
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| Animal Protocol |
Animal/Disease Models: Male Swiss mice (7-9 weeks old) were injected with CCL1[2]
Doses: 0.1 mg/kg, 0.3mg/kg, 1 mg/kg Route of Administration: intraperitoneal (ip) injection; Experimental Results:CCL1 (10 μg/kg ; 1 h; sc)-induced analgesia was dose-dependently inhibited. |
| References |
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| Molecular Formula |
C21H27NO4
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|---|---|
| Molecular Weight |
357.443386316299
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| Exact Mass |
357.194
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| Elemental Analysis |
C, 70.56; H, 7.61; N, 3.92; O, 17.90
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| CAS # |
688352-84-3
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| PubChem CID |
2962888
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| Appearance |
White to off-white solid powder
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| LogP |
3.9
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
26
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| Complexity |
499
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
JJMLDSFDOODCIR-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C21H27NO4/c1(2-26-21-8-14-3-15(9-21)5-16(4-14)10-21)22-11-17-6-19-20(25-13-24-19)7-18(17)23-12-22/h6-7,14-16H,1-5,8-13H2
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| Chemical Name |
7,8-Dihydro-7-[2-(tricyclo[3.3.1.1(3,7)]dec-1-yloxy)ethyl]-6H-1,3-dioxolo[4,5-g][1,3]benzoxazine
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| Synonyms |
R-243 R243 R 243
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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 : ~125 mg/mL (~349.71 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.82 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 20.8 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. Solubility in Formulation 2: ≥ 2.08 mg/mL (5.82 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 20.8 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 | 2.7977 mL | 13.9884 mL | 27.9767 mL | |
| 5 mM | 0.5595 mL | 2.7977 mL | 5.5953 mL | |
| 10 mM | 0.2798 mL | 1.3988 mL | 2.7977 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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT05670483 | Recruiting | Device: Use Of APRV mode of Ventilation
Device: Use of conventional Synchronized Intermittent Mandatory Ventilation (SIMV) volume control mode |
Morbid Obesity Pulmonary Atelectasis Pulmonary Complication |
Ain Shams University | 2022-12-03 | Not Applicable |
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