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.
- CAS No.: 1628160-15-5
- Formula: C26H35N3O6
- Molecular Weight:485.58
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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PDE4A 0.09 nM (IC50) |
PDE4B 0.09 |
PDE4D 0.14 nM (IC50) |
PDE4C 2.4 nM (IC50) |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57Bl/6 (female, 8–10 weeks old, LPS-induced)[1]
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Dosage:3 mg/kg; 10 mg/kg
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Administration:p.o.; single dose
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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.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1628160-15-5
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Molecular Weight 485.58
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Formula C26H35N3O6
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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
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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