1. MAPK/ERK Pathway Apoptosis Immunology/Inflammation
  2. p38 MAPK TNF Receptor Interleukin Related
  3. CBS-3408

CBS-3408 is an orally active p38α MAPK inhibitor. CBS-3408 inhibits the release of TNFα and IL-1β. CBS-3408 reduces the disease severity of arthritis in mice. CBS-3408 inhibits TNFα release in a rat endotoxemia model. CBS-3408 can be used in studies related to endotoxemia and arthritis.

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CBS-3408

CBS-3408 Chemical Structure

CAS No. : 452056-93-8

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Description

CBS-3408 is an orally active p38α MAPK inhibitor. CBS-3408 inhibits the release of TNFα and IL-1β. CBS-3408 reduces the disease severity of arthritis in mice. CBS-3408 inhibits TNFα release in a rat endotoxemia model. CBS-3408 can be used in studies related to endotoxemia and arthritis[1].

In Vitro

CBS-3408 (Compound 3) inhibits LPS (HY-D1056)-induced IL-1β and TNFα release in human whole blood[1].
CBS-3408 (10 μM) inhibits JNK3 and p38β kinases by over 70%[1].
CBS-3408 (10 μM) inhibits CYP2C9 (46%) and CYP2D6 (45%), shows weak inhibitory activity against CYP1A2 (18%), and exhibits no relevant activity against CYP2C19 or CYP3A4[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Parmacokinetics
Species Dose Route Tmax Cmax AUC0-t T1/2
Rat[1] 30 mg/kg p.o. 1.0 h 738 ng/mL 4928 ng·h/mL 3.0 h
In Vivo

CBS-3408 (10 mg/kg; p.o.; single administration) achieves 97% inhibition of TNFα release in LPS-induced endotoxemia models of male Wistar rats[1].
CBS-3408 (50 mg/kg; p.o.; twice daily) significantly reduces the disease severity of collagen (HY-NP003)-induced arthritis in male DBA/1 mice[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Wistar (male)[1]
Dosage: 10 mg/kg
Administration: p.o.; single dose
Result: Achieved 97% inhibition of plasma TNFα concentrations compared to control animals.
Animal Model: DBA/1 (male)[1]
Dosage: 50 mg/kg
Administration: p.o.; twice daily
Result: Substantially reduced arthritic disease severity, with a notably lower arthritic score compared to vehicle control animals over the course of the study.
Showed no treatment-related toxicity aside from body weight loss identical to controls.
Molecular Weight

356.42

Formula

C18H17FN4OS

CAS No.
SMILES

O=C(C)NC1=NC=CC(C2=C(C3=CC=C(C=C3)F)N=C(N2C)SC)=C1

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Purity & Documentation
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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CBS-3408
Cat. No.:
HY-182579
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