R-7050

Catalog No.S6643 Batch:S664303

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Technical Data

Formula

C16H8ClF3N4S
Molecular Weight 380.77 CAS No. 303997-35-5
Solubility (25°C)* In vitro DMSO (warmed with 50ºC water bath) 13 mg/mL (34.14 mM)
Water Insoluble
Ethanol Insoluble
In vivo (Add solvents to the product individually and in order)
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O

Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.

 0.350mg/ml (0.92mM) Taking the 1 mL working solution as an example, add 50 μL of clarified DMSO stock solution of 7 mg/ml to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify it; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
Clear solution
5% DMSO 95% corn oil

Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.

 0.650mg/ml (1.71mM) Taking the 1 mL working solution as an example, add 50 μL of 13 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description R-7050 is a cell permeable TNF-α receptor antagonist and is 2.3-fold more selective for TNF-α-mediated signaling than for that driven by IL-1β.
Targets
TNF-α [2] IL-1β [2]
0.63 μM(EC50) 1.45 μM(EC50)
In vitro

This compound has a clear selectivity toward TNFα and to a slightly weaker extent toward the LPA receptor which belongs to a GPCR class over IL-1β, tyrosine kinase, or Fas receptor systems.
In vivo

R-7050 attenuates neurovascular injury after intracerebral hemorrhage (ICH) in mice, Up to 2h post-injury administration of this compound significantly reduced blood-brain barrier opening and attenuated edema development at 24h post-ICH. Neurological outcomes were also improved over the first three days after injury. In contrast, it did not reduce hematoma volume.

Protocol (from reference)

Animal Study:

[1]
  • Animal Models

    A mouse collagenase model of ICH (based on male CD-1 mice)

  • Dosages

    6–18 mg/kg

  • Administration

    IP

References

  • https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3744337/
  • https://pubmed.ncbi.nlm.nih.gov/17961823/

Selleck's R-7050 Has Been Cited by 13 Publications

TNF-α-downregulated SIRT1 regulates mitochondrial-autophagy and apoptosis in renal vascular endothelial cells involved in trichloroethylene-induced immune kidney injury [ Int Immunopharmacol, 2024, 143(Pt 2):113521] PubMed: 39476564
TNFR1 signaling converging on FGF14 controls neuronal hyperactivity and sickness behavior in experimental cerebral malaria [ Journal of Neuroinflammation, 2023, 306] PubMed: 38115011.0
Macrophage polarization induces endothelium-to-myofibroblast transition in chronic allograft dysfunction [ Ren Fail, 2023, 45(1):2220418] PubMed: 37288756
Macrophage polarization induces endothelium-to-myofibroblast transition in chronic allograft dysfunction [ Renal Failure, 2023, 2220418] PubMed: 37288756.0
Zika virus causes placental pyroptosis and associated adverse fetal outcomes by activating GSDME [ eLife, 2022, e73792] PubMed: 35972780.0
Zika virus causes placental pyroptosis and associated adverse fetal outcomes by activating GSDME [ Elife, 2022, 11e73792] PubMed: 35972780
DAMPs Released from Proinflammatory Macrophages Induce Inflammation in Cardiomyocytes via Activation of TLR4 and TNFR [ Int J Mol Sci, 2022, 23(24)15522] PubMed: 36555168
Soluble tumor necrosis factor-alpha-induced hyperexcitability contributes to retinal ganglion cell apoptosis by enhancing Nav1.6 in experimental glaucoma [ Journal of Neuroinflammation, 2021, 182] PubMed: 34419081.0
The effect of macrophage polarization on the expression of the oxytocin signalling system in enteric neurons [ J Neuroinflammation, 2021, 18(1):261] PubMed: 34749758
The effect of macrophages polarization on the expression of oxytocin signaling system in enteric neurons [ Research Square, 2021, 10.21203/rs.3.rs-611538/v1] PubMed: None

RETURN POLICY
Selleck Chemical’s Unconditional Return Policy ensures a smooth online shopping experience for our customers. If you are in any way unsatisfied with your purchase, you may return any item(s) within 7 days of receiving it. In the event of product quality issues, either protocol related or product related problems, you may return any item(s) within 365 days from the original purchase date. Please follow the instructions below when returning products.

SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.