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Synonyms:
PDE4B/D-IN-5
| Pack Size | Price | USA Stock | Global Stock | Quantity |
|---|---|---|---|---|
| 10 mg | Inquiry | 10-14 weeks | 10-14 weeks | |
| 50 mg | Inquiry | 10-14 weeks | 10-14 weeks |
| Description | PDE4B/D-IN-5 (Compound P32) is a peripherally restrictive, orally active inhibitor of PDE4B and PDE4D with minimal blood-brain barrier penetration, exhibiting IC50 values of 3.4 nM and 2.2 nM, respectively. It suppresses TNF-α production and significantly reduces the Bax/Bcl2 ratio, mitigates oxidative stress by decreasing MPO activity and NO levels. PDE4B/D-IN-5 possesses anti-inflammatory, antioxidant, and anti-apoptotic (Anti-apoptotic) properties and is applicable for acute lung injury research. |
| Targets & IC50 | PDE4B1:3.4 nM |
| In vitro | PDE4B/D-IN-5 effectively inhibits recombinant PDE4B1 in vitro with an IC50 of 3.4 nM in fluorescence polarization enzyme assays. The compound demonstrates high metabolic stability in rat liver microsomes, with 94.8% remaining after 60 minutes, a half-life of 5.5 hours, and a clearance rate as low as 0.0021 mL min−1 mg−1. Additionally, PDE4B/D-IN-5 (1-4 μM; 1 h) dose-dependently inhibits LPS-induced TNF-α production in RAW264.7 murine macrophages. |
| In vivo | PDE4B/D-IN-5, when administered orally at doses of 1-6 mg/kg, does not induce vomiting in beagle dogs. Administered via intraperitoneal injection at doses of 6-12 mg/kg, once daily for five consecutive days, PDE4B/D-IN-5 exhibits dose-dependent anti-inflammatory, antioxidative, and anti-apoptotic effects that alleviate acute lung injury induced by lipopolysaccharide (LPS) in male C57BL/6 mice through the cAMP-Epac pathway. |
| Molecular Weight | 425.43 |
| Formula | C22H21F2N5O2 |
| Cas No. | 3064814-26-9 |
| Smiles | O=C(O)CC1=CC=C(C=C1)NC2=CC=C3C(=C2)C(=NN3CC(F)F)C4=CC=NN4CC |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. |
Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 µL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 µL Tween 80 and mix well until fully clarified.
3) Add 450 µL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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