2. Metabolic Enzyme/Protease
  3. Phosphodiesterase (PDE)
  4. UK-500001

UK-500001 is an orally active inhibitor for phosphodiesterase 4 (PDE4), which inhibits PDE4D3 (IC50 is 0.28 nM), PDE4B2 (IC50 is 22.8 nM), PDE4A4 (IC50 is 26.1 nM) and PDE4C2 (IC50 is 271 nM). UK-500001 exhibits anti-inflammatory efficacy and inhibits TNF-α and IFN-γ release in human and rodent macrophagic cell lines in nanomolar levels. UK-500001 ameliorates chronic obstructive pulmonary disease (COPD) and asthma.

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UK-500001 Chemical Structure

UK-500001 Chemical Structure

CAS No. : 582332-31-8

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UK-500001 Related Antibodies

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Description

UK-500001 is an orally active inhibitor for phosphodiesterase 4 (PDE4), which inhibits PDE4D3 (IC50 is 0.28 nM), PDE4B2 (IC50 is 22.8 nM), PDE4A4 (IC50 is 26.1 nM) and PDE4C2 (IC50 is 271 nM). UK-500001 exhibits anti-inflammatory efficacy and inhibits TNF-α and IFN-γ release in human and rodent macrophagic cell lines in nanomolar levels. UK-500001 ameliorates chronic obstructive pulmonary disease (COPD) and asthma[1].

IC50 & Target

PDE4D3

0.28 nM (IC50)

PDE4B2

22.8 nM (IC50)

PDE4A4

26.1 nM (IC50)

PDE4C2

217 nM (IC50)

Molecular Weight

499.48

Formula

C26H24F3N3O4
CAS No.
SMILES

O=C(C1=C(C=CC(C)=C1)O)N[C@H](CC2)CC[C@H]2NC(C(C=C(F)C=N3)=C3OC4=CC(F)=C(F)C=C4)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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UK-500001 Related Classifications

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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.

Keywords:

UK-500001582332-31-8UK500001UK 500001Phosphodiesterase (PDE)THP-1NR8383RAW264.7PBMCchronic obstructive pulmonary diseaseasthmaCOPDorally activeInhibitorinhibitorinhibit

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