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Benpyrine racemate

Cat. No. M10643
Benpyrine racemate Structure
Synonym:

(Rac)-Benpyrine

Size Price Availability Quantity
5mg USD 175  USD175 In stock
10mg USD 280  USD280 In stock
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Biological Activity

Benpyrine racemate ((Rac)-Benpyrine) is a racemate of Benpyrine, Benpyrine racemate ((Rac)-Benpyrine) is a potent and orally active TNF-α inhibitor and has the potential for TNF-α mediated inflammatory and autoimmune disease research. (Rac)-Benpyrine (5-10 μM; 24 hours) treatment inhibits the expression level of TNF-α downstream pathway protein NF-κB in the nucleus in RAW264.7 macrophages. In vivo, (Rac)-Benpyrine (25-50 mg/kg/day; oral gavage; 3 weeks) treatment obviously reduces the inflammatory cytokines IFN-γ, IL-1β and IL-6 in the blood serum, and the anti-inflammatory factor IL-10 is obviously increased, the foot swelling degree of the arthritis part is also obviously slowed down.

Chemical Information
Molecular Weight 308.34
Formula C16H16N6O
CAS Number 1333714-43-4
Solubility (25°C) DMSO 9 mg/mL
Storage 2-8°C, protect from light, sealed
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] Weiguang Sun, et al. J Med Chem . Discovery of an Orally Active Small-Molecule Tumor Necrosis Factor-α Inhibitor

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Keywords: Benpyrine racemate, (Rac)-Benpyrine supplier, TNF Receptor, inhibitors, activators


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