PDE4-IN-12
PDE4-IN-12 is a potent pan-PDE4 inhibitor, with IC50s of 3.5 and 15 nM for PDE4 and PDE7, respectively (SI=2.71 and 4.27, respectively). PDE4-IN-12 shows well tolerated, can be used in study of inflammatory bowel diseases (IBDs).
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- CAS No.: 2901084-32-8
- Formule: C34H35NO6
- Masse moléculaire:553.64
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
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PDE4D2 3.51 nM (IC50) |
PDE4B2 9.51 nM (IC50) |
PDE7A 15 nM (IC50) |
PDE5A1 1.24 μM (IC50) |
PDE10A 1.02 μM (IC50) |
PDE8A1 194 nM (IC50) |
PDE4-IN-12 (compound 22d) (10, 20 µM; 24 h) reduces the release of NO in LPS induced inflammation cell model (indicates anti-inflammatory effect)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Raw264.6 cells
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Concentration:10, 20 µM
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Incubation Time:24 h
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Result:Reduced the NO release by dose-dependent manner in the LPS induced inflammatory cell model.
PDE4-IN-12 (10 mg/kg; p.o.; single) shows well tolerated in dogs[1].
PDE4-IN-1 (2.5 mg/kg; i.v.; single) shows great plasma exposure, with T1/2 and AUC0-24 h values of 4.18 h and 6522 hng/mL[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male C57BL/6 mice (5 to 6-week old; 15-17 g; DSS-induced mouse model)[1].
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Dosage:5 mg/kg
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Administration:Intraperitoneal injection; twice daily for 8 days.
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Result:Ameliorated the acute colitis by decreasing disease activity index, increasing the colon length, and also ameliorating the pathological damages.
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Animal Model:Beagle dogs[1].
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Dosage:10 mg/kg (solved in 0.5% CMC-Na solution).
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Administration:Oral administration; single.
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Result:Exhibited good safety, which caused no emesis on beagle dogs at 10 mg/kg.
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Animal Model:Male C57BL/6 mice (5 to 6-week old; 15-17 g)[1].
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Dosage:2.5 mg/kg
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Administration:Intravenous injection; single.
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Result:
1.19 Pharmacokinetic Parameters of PDE4-IN-12 in Male C57BL/6 mice[1].
T1/2 (h) AUC0-24 h (h⋅ng/mL) MRT0-24 h (h) CL (mL/min/kg) Vss (mL/kg) IV (2.5 mg/kg) 4.18 6522 1.76 6.40 673
Chemical Information
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CAS No. 2901084-32-8
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Masse moléculaire 553.64
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Formule C34H35NO6
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SMILES
COC1=C(C=C2OC3=C(C(OCC4=CC=NC=C4)=C5C=CC(C)(OC5=C3)C)C(C2=C1C/C=C(C)\C)=O)OCC6CC6
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
PDE4-IN-12 Related Classifications
HY-151174 Related Classifications
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