2. Metabolic Enzyme/Protease Apoptosis
  3. Phosphodiesterase (PDE) TNF Receptor
  4. LY2775240

LY2775240 is an orally active phosphodiesterase 4 (PDE4) inhibitor with potent inhibitory activity against PDE4A (IC50 = 0.09 nM), PDE4B (IC50 = 0.09 nM) and PDE4D (IC50 = 0.14 nM), and exhibits an IC50 of 2.4 nM against PDE4C. LY2775240 is a highly selective agent that reduces TNFα production upon immune activation. LY2775240 decreases TNFα production in rodent and rhesus monkey models. LY2775240 can be used in the research of psoriasis.

For research use only. We do not sell to patients.

LY2775240

LY2775240 Chemical Structure

CAS No. : 1628160-15-5

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LY2775240 Related Antibodies

Top Publications Citing Use of Products

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PDE1 PDE2 PDE3 PDE4 PDE5 PDE6 PDE7 PDE9 PDE10 PDE11 PDE12 PDE8 Autotaxin

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TNFRSF1A/CD120a TNFRSF3/CD18 TNFRSF4 TNFRSF5/CD40 TNFRSF6/Fas/CD95 TNFRSF7/CD27 TNFRSF8/CD30 TNFRSF9/4-1BB/CD137 TNFRSF10B/DR5/CD262 TNFRSF12A/TWEAK TNFRSF16/NGF Receptor/CD271 TNFRSF18/GITR/CD357

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Description

LY2775240 is an orally active phosphodiesterase 4 (PDE4) inhibitor with potent inhibitory activity against PDE4A (IC50 = 0.09 nM), PDE4B (IC50 = 0.09 nM) and PDE4D (IC50 = 0.14 nM), and exhibits an IC50 of 2.4 nM against PDE4C. LY2775240 is a highly selective agent that reduces TNFα production upon immune activation. LY2775240 decreases TNFα production in rodent and rhesus monkey models. LY2775240 can be used in the research of psoriasis[1].

IC50 & Target[1]

PDE4A

0.09 nM (IC50)

PDE4B

0.09<br/> nM (IC50)

PDE4D

0.14 nM (IC50)

PDE4C

2.4 nM (IC50)

In Vitro

LY2775240 potently inhibits LPS (HY-D1056)-stimulated TNFα secretion in human whole blood with an IC50 of 18 nM[1].

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

LY2775240 Related Antibodies
In Vivo

LY2775240 (3-10 mg/kg; p.o.; single dose) significantly reduces LPS-induced TNFα production in mice[1].

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

Animal Model: C57Bl/6 (female, 8–10 weeks old, LPS-induced)[1]
Dosage: 3 mg/kg; 10 mg/kg
Administration: p.o.; single dose
Result: Reduced plasma TNFα to 53% of vehicle control at 3 mg/kg; reduced plasma TNFα to 35% of vehicle control at 10 mg/kg.
Clinical Trial
Molecular Weight

485.58

Formula

C26H35N3O6
CAS No.
SMILES

[C@H](C)(O)[C@@]1(C)[C@@H](CN(C([C@H](CO)O)=O)C1)C2=CC(OC3CN(C3)C4=CC=C(C)C=N4)=C(OC)C=C2
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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LY2775240 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:

LY27752401628160-15-5LY 2775240LY-2775240Phosphodiesterase (PDE)TNF ReceptorTumor Necrosis Factor ReceptorTNFRPDE4CPDE4BpsoriasisPDE4Drodent modelsTNFαPDE4Arhesus monkey modelsphosphodiesterase 4PDE4Inhibitorinhibitorinhibit

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