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.
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- CAS No.: 1628160-15-5
- 화학식: C26H35N3O6
- 분자량:485.58
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
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
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1628160-15-5
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분자량 485.58
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화학식 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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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)