TNF-α-IN-2 - ≥98% , CAS No.2074702-04-6

CAS: 2074702-04-6 Cat. No.: T649275 Summenformel: C₂₅H₂₁ClF₂N₆O Molekulargewicht: 494.92

GRADE & PURITY ≥98%

Storage

Store at -20°C

Shipped In

Ice chest + Ice pads

Übersicht

TNF-α-IN-2 is a potent and orally active inhibitor of tumor necrosis factor alpha (TNFα) , with an IC 50 of 25 nM in the HTRF assay. TNF-α-IN-2 distorts the TNFα trimer upon binding, leading to aberrant signaling when the trimer binds to TNFR1. TNF-α-IN-2 can be used for the research of rheumatoid arthritis

In Vitro

TNF-α-IN-2 (compound 42) (30 min) inhibits the E-selectin expression induced by soluble TNFα in HUVECs, with an IC 50 of 30 nM. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

TNF-α-IN-2 (5-25 mg/kg; p.o. 1 h before TNF stimulation) inhibits TNF-induced IL-6 in mice . TNF-α-IN-2 (2-10 mg/kg; p.o. twice daily for 10 d) dose dependently reduces both the clinical score as well as the levels of inflammatory cytokines and leukocyte cell surface receptors in mice . TNF-α-IN-2 (0.5 mg/kg; i.v.) exhibits long t 1/2 (6.2 h), low CL (6.6 mL/min•kg), and V ss (3.2 L/kg) in mice . TNF-α-IN-2 (2 mg/kg; p.o.) exhibits good oral bioavailability (58%), C max (0.47 μM), and AUC tot (5.9 μM•h) in mice . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Female C57Bl/6 mice Dosage: 5, 25 mg/kg Administration: P.o. 1 h prior to TNF stimulation Result: Inhibited IL-6 moderately at 5 mg/kg while the inhibition at 25 mg/kg was similar to mouse Enbrel, which served as the positive control in the study.

Form:Solid

IC50& Target:CD40 25 nM (IC 50 )

Specifications

Spezifikationen & Reinheit

≥98%

Biochemische und physiologische Mechanismen

TNF-α-IN-2 is a potent and orally active inhibitor of tumor necrosis factor alpha (TNFα) , with an IC 50 of 25 nM in the HTRF assay. TNF-α-IN-2 distorts the TNFα trimer upon binding, leading to aberrant signaling when the trimer binds to TNFR1. TNF-α-IN-2

Storage

Store at -20°C

Verschickt in

Ice chest + Ice pads

Dieses Produkt erfordert Kühlkettenversand. Grundversand und andere Economy-Optionen sind nicht verfügbar.

Reinheit

≥98%

Namen und Kennungen

• Molekulargewicht: 494.92

Chemische und physikalische Eigenschaften

• Löslichkeit: DMSO : 100 mg/mL (202.05 mM; Need ultrasonic)