2. Metabolic Enzyme/Protease
  3. Phosphodiesterase (PDE)
  4. 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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PDE4-IN-12 Chemical Structure

PDE4-IN-12 Chemical Structure

CAS No. : 2901084-32-8

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PDE4-IN-12 Related Antibodies

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Description

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)[1].

IC50 & Target

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)

In Vitro

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.

PDE4-IN-12 Related Antibodies

Cell Viability Assay[1]

Cell Line: Raw264.6 cells
Concentration: 10, 20 µM
Incubation Time: 24 h
Result: Reduced the NO release by dose-dependent manner in the LPS induced inflammatory cell model.
In Vivo

PDE4-IN-12 (5 mg/kg; i.p.; twice daily for 8 days) ameliorates mouse acute colitis induced by DSS (dextran sulfate sodium)[1].
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 hng/mL[1].

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

Animal Model: Male C57BL/6 mice (5 to 6-week old; 15-17 g; DSS-induced mouse model)[1].
Dosage: 5 mg/kg
Administration: Intraperitoneal injection; twice daily for 8 days.
Result: Ameliorated the acute colitis by decreasing disease activity index, increasing the colon length, and also ameliorating the pathological damages.
Animal Model: Beagle dogs[1].
Dosage: 10 mg/kg (solved in 0.5% CMC-Na solution).
Administration: Oral administration; single.
Result: Exhibited good safety, which caused no emesis on beagle dogs at 10 mg/kg.
Animal Model: Male C57BL/6 mice (5 to 6-week old; 15-17 g)[1].
Dosage: 2.5 mg/kg
Administration: Intravenous injection; single.
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
Molecular Weight

553.64

Formula

C34H35NO6
CAS No.
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
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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PDE4-IN-12 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:

PDE4-IN-122901084-32-8Phosphodiesterase (PDE)IBDsinflammatory bowelCrohn’s diseaseulcerative colitisRaw264.6Inhibitorinhibitorinhibit

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