| Size | Price | Stock | Qty |
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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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Purity: ≥98%
RS-102895 HCl (RS 102895), the hydrochloride salt of RS102895, is a novel and potent chemokine receptor CCR2 antagonist anticancer activity. It exhibits no effect on CCR1 but inhibits CCR2 with an IC50 of 360 nM. At IC50 values of 32 nM and 1.7 μM, respectively, RS-102895 HCl inhibits MCP-1-stimulated calcium influx and chemotaxis. Moreover, it blocks 5-HT1A, α1A, and α1D receptors.
| Targets |
CCR2 ( IC50 = 360 nM ); CCR1 ( IC50 = 17800 nM ); Human α1a receptor ( IC50 = 130 nM ); Human α1d receptor ( IC50 = 320 nM ); 5HT-1a receptor ( IC50 = 470 nM )
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| ln Vitro |
RS-102895's effect on leukocyte chemotaxis toward CCL2 is validated by an in vitro chemotaxis assay. Based on the data, it appears that elevated CCL2 in SS kidneys plays a significant role in the initial leukocyte recruitment. Blocking this recruitment with RS-102895 then reduces hypertension and renal damage.[2]
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| ln Vivo |
The biological function of the CCL2/CCR2 pathway is tested by daily administration of CCR2 antagonist RS-102895. Assessments are made of blood pressure, renal damage, and renal leukocyte infiltration. The findings show that following a 21-day high-salt diet, RS-102895 treatment reduces hypertension and renal damage. It is found that by day three of the high-salt diet, renal leukocyte infiltration is blunted. [2]
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| Cell Assay |
After being collected, peritoneal cells are centrifuged, filtered through a 40-μm strainer, and then resuspended in medium without serum. After using a hemocytometer to count the cells, the concentration was adjusted to 107 cells/mL. The cells are left untreated or incubated for 30 minutes with DMSO vehicle, urine from animals treated with CCR2 antagonists in vivo, or RS-102895 at different concentrations.
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| References |
| Molecular Formula |
C21H22CLF3N2O2
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|---|---|
| Molecular Weight |
426.8598
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| Exact Mass |
426.13
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| Elemental Analysis |
C, 59.09; H, 5.20; Cl, 8.30; F, 13.35; N, 6.56; O, 7.50
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| CAS # |
1173022-16-6
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| Related CAS # |
RS102895; 300815-41-2
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| Appearance |
Solid powder
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| SMILES |
C1CN(CCC12C3=CC=CC=C3NC(=O)O2)CCC4=CC=C(C=C4)C(F)(F)F.Cl
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| InChi Key |
KRRISOFSWVKYBF-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C21H21F3N2O2.ClH/c22-21(23,24)16-7-5-15(6-8-16)9-12-26-13-10-20(11-14-26)17-3-1-2-4-18(17)25-19(27)28-20;/h1-8H,9-14H2,(H,25,27);1H
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| Chemical Name |
1'-[2-[4-(trifluoromethyl)phenyl]ethyl]spiro[1H-3,1-benzoxazine-4,4'-piperidine]-2-one;hydrochloride
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| Synonyms |
RS-102895HCl; RS-102895; RS 102895; RS-102895 HCl; RS102895
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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 Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| 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: 41.7~85 mg/mL (97.6~199.1 mM)
Ethanol: 85 mg/mL |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.87 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 20.8 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: ≥ 2.08 mg/mL (4.87 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. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (4.87 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 5%DMSO+ Corn oil: 4.5mg/ml (10.54mM) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3427 mL | 11.7134 mL | 23.4269 mL | |
| 5 mM | 0.4685 mL | 2.3427 mL | 4.6854 mL | |
| 10 mM | 0.2343 mL | 1.1713 mL | 2.3427 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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