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25mg |
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50mg |
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Purity: ≥98%
R-7050 (R7050) is a novel, potent and selective tumor necrosis factor/ TNF-α receptor antagonist acting by blocking receptor-adaptor molecule complex formation and subsequent receptor internalization, but not TNF-α ligand-receptor binding. Showing a high degree of selectivity for TNF.
Targets |
TNF-α (EC50 = 0.63 μM); IL-1β (EC50 = 1.45 μM)
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ln Vitro |
R-7050 has a distinct preference for TNFα and to a slightly lesser extent, for the LPA receptor, which is a type of GPCR, as opposed to IL-1β, tyrosine kinase, or Fas receptor systems[2].
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ln Vivo |
R-7050 reduces the neurovascular damage caused by intracerebral hemorrhage (ICH) in mice. R-7050 administration up to two hours after the injury markedly decreased blood-brain barrier opening and slowed the onset of edema 24 hours after the injury. Over the first three days following the injury, neurological results also improved. R-7050, on the other hand, had no effect on hematoma volume reduction[1].
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Animal Protocol |
Mice: A mouse collagenase model of ICH is utilized. In a nutshell, 8–10 week old male CD-1 mice are positioned in a stereotactic frame, and a burr hole with a diameter of 0.5 mm is drilled over the parietal cortex, 2.2 mm lateral to the bregma. The left striatum is injected directly from the surface of the skull 3 mm down using a 26-gauge Hamilton syringe filled with 0.04 U of bacterial type IV collagenase in 0.5 L saline. To avoid solution reflux and excessive diffusion, the syringe is depressed at 450 nL/min and left in place for a few minutes after the procedure. Sham animals undergo the same surgical procedure, except that saline is stereotactically injected rather than collagenase. After the syringe is removed, bone wax is used to close the burr hole, the incision is surgically stapled, and mice are kept warm until recovery of the righting reflex. R-7050 (6-18 mg/kg) is administered via intraperitoneal route at the time of injury or up to 2 h post-ICH.
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References |
Molecular Formula |
C16H8CLF3N4S
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Molecular Weight |
380.774730682373
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Exact Mass |
380.011
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Elemental Analysis |
C, 50.47; H, 2.12; Cl, 9.31; F, 14.97; N, 14.71; S, 8.42
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CAS # |
303997-35-5
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Related CAS # |
303997-35-5
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Appearance |
Solid powder
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SMILES |
C1=CC=C(C=C1)SC2=NC3=C(C=C(C=C3)Cl)N4C2=NN=C4C(F)(F)F
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InChi Key |
SUUMKHOVGVYGOP-UHFFFAOYSA-N
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InChi Code |
InChI=1S/C16H8ClF3N4S/c17-9-6-7-11-12(8-9)24-13(22-23-15(24)16(18,19)20)14(21-11)25-10-4-2-1-3-5-10/h1-8H
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Chemical Name |
8-chloro-4-phenylsulfanyl-1-(trifluoromethyl)-[1,2,4]triazolo[4,3-a]quinoxaline
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Synonyms |
TNF-α Antagonist III; R-7050; R7050; R 7050
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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: 9~25 mg/mL (23.6~65.7 mM)
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Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (6.57 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
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 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: ≥ 2.5 mg/mL (6.57 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 | 2.6263 mL | 13.1313 mL | 26.2626 mL | |
5 mM | 0.5253 mL | 2.6263 mL | 5.2525 mL | |
10 mM | 0.2626 mL | 1.3131 mL | 2.6263 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.