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R-7050

Cat. No. M8516
R-7050 Structure
Synonym:

TNF-α Antagonist III; R7050

Size Price Availability Quantity
5mg USD 75  USD75 In stock
10mg USD 108  USD108 In stock
25mg USD 240  USD240 In stock
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Quality Control & Documentation
Biological Activity

R-7050 is a cell-permeable TNF-α receptor antagonist that blocks TNF-α-induced binding of TNF-αRI with TNFαR-associated death domain protein and receptor interacting protein 1, blocking internalization of the TNFα-TNFαR complex. R-7050 was found to reduce neurovascular injury in a mouse model of hemorrhagic stroke.

R-7050 (TNF-α Antagonist III) (6 mg/kg) reduces Evans blue extravasation to 28.7±5.9 μg and 30.3±1.9 μg Evans blue/g brain tissue when administered at 0.5 h or 2 h post-ICH, respectively (p<0.05 and p<0.01 vs ICH, respectively; not significantly different from sham). Brain water content, a measure of brain edema, increases from 75.6±0.3% in sham-operated mice to 81.5±0.5% at 24h post-ICH (p<0.05 vs. sham).

Chemical Information
Molecular Weight 380.77
Formula C16H8ClF3N4S
CAS Number 303997-35-5
Solubility (25°C) DMSO 20 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Min Ji, et al. Microglia-derived TNF-α mediates Müller cell activation by activating the TNFR1-NF-κB pathway

[2] Shih-Yi Lin, et al. TNF-α Receptor Inhibitor Alleviates Metabolic and Inflammatory Changes in a Rat Model of Ischemic Stroke

[3] Tolulope E Ayo, et al. TNF Production in Activated RBL-2H3 Cells Requires Munc13-4

[4] Yi Wen, et al. KLF4 in Macrophages Attenuates TNF α-Mediated Kidney Injury and Fibrosis

[5] Melanie D King, et al. TNF-alpha receptor antagonist, R-7050, improves neurological outcomes following intracerebral hemorrhage in mice

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Keywords: R-7050, TNF-α Antagonist III; R7050 supplier, TNF Receptor, inhibitors, activators


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