Benpyrine racemate

Catalog No.S3515 Batch:S351501

Technical Data

Formula	C₁₆H₁₆N₆O
Molecular Weight	308.34	CAS No.	1333714-43-4
Solubility (25°C)*	In vitro	DMSO	31 mg/mL (100.53 mM)
		Water	Insoluble
		Ethanol	Insoluble
* <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.)

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Biological Activity

Description

Benpyrine racemate ((Rac)-Benpyrine) is a potent, highly specific and orally active inhibitor of TNF-α and attenuates TNF-α-induced inflammation, thereby reducing liver and lung injury.

Targets

TNF-α ^[1]

In vitro

Benpyrine directly binds to TNF-α and blocks TNF-α-trigged signaling activation.^[1]

In vivo

Benpyrine attenuates TNF-α-induced inflammation in endotoxemic murine model, thereby reducing liver and lung injury, and significantly reliefs the symptoms of collagen-induced arthritis and imiquimod-induced psoriasiform inflammation in mice.^[1]

Protocol (from reference)

Cell Assay:^{^[1]}	Cell lines RAW264.7 macrophages Concentrations 5, 10 or 20 μM Incubation Time 12 h Method RAW 264.7 cells were grown to 50−70% confluence in a glass chamber, pretreated with DMSO or benpyrine for 12 h, and then stimulated with 10 ng/mL TNF-α for 2 h. Cell treatments were terminated by washing the cells with PBS, followed by fixation with freshly prepared 4% paraformaldehyde in PBS for 20 min. The fixed cells were washed three times with PBS and then permeabilized with 0.25% Triton X-100 in PBS for 10 min. After blocking with 2 mg/mL BSA for 1 h at room temperature, we added the NF-κB/p65 antibody at a 1:1000 dilution at 4 °C overnight, washed three times with PBS, then incubated with a 1:500 dilution of the secondary antibody for 1 h at room temperature in the dark. Finally, 4′,6-diamidino-2-phenyl indole (DAPI) was used to stain the nuclei at 37 °C for 30 min in the dark.
Animal Study:^{^[1]}	Animal Models CIA mice, Imiquimod-Induced Psoriasis-like Skin Lesions mice mode Dosages 25, 50 mg/kg Administration i.g.

Cell Assay:^{^[1]}

Cell lines
RAW264.7 macrophages
Concentrations
5, 10 or 20 μM
Incubation Time
12 h
Method
RAW 264.7 cells were grown to 50−70% confluence in a glass chamber, pretreated with DMSO or benpyrine for 12 h, and then stimulated with 10 ng/mL TNF-α for 2 h. Cell treatments were terminated by washing the cells with PBS, followed by fixation with freshly prepared 4% paraformaldehyde in PBS for 20 min. The fixed cells were washed three times with PBS and then permeabilized with 0.25% Triton X-100 in PBS for 10 min. After blocking with 2 mg/mL BSA for 1 h at room temperature, we added the NF-κB/p65 antibody at a 1:1000 dilution at 4 °C overnight, washed three times with PBS, then incubated with a 1:500 dilution of the secondary antibody for 1 h at room temperature in the dark. Finally, 4′,6-diamidino-2-phenyl indole (DAPI) was used to stain the nuclei at 37 °C for 30 min in the dark.

Animal Study:^{^[1]}

Animal Models
CIA mice, Imiquimod-Induced Psoriasis-like Skin Lesions mice mode
Dosages
25, 50 mg/kg
Administration
i.g.

References

[1] Weiguang Sun, et al. J Med Chem. 2020 Aug 13;63(15):8146-8156.

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SHIPPING AND STORAGE
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