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Biochem/physiol Actions
A-33 (A33) is a potent and selective catalytic site-targeting PDE4B inhibitor (IC50 = 15 nM/PDE4B vs. 1.7 μM/PDE4D) that effectively prevents PDE4B-medicated cellular cAMP hydrolysis (150%/320% increased cAMP level with 100 nM/1 μM A-33 pre-treament in murine hippocampal HT-22 cells following 10 nM isoproterenol stimulation) in vitro and inhibits LPS-induced TNF-α production in mice in vivo (ID50 = 14 mg/kg p.o.). When administered via intraperitoneal injection, A-33 improves cognitive function in a rat model of traumatic brain injury (0.3 mg/kg i.p.) and exhibits antidepressant property in mice (0.3-1 mg/kg i.p.) in vivo.
Orally acive, potent and selective catalytic site-targeting PDE4B inhibitor with anti-inflammatory, antidepressant, and cognition-improving efficacy in vivo.
| assay | ≥98% (HPLC) |
| form | powder |
| color | white to beige |
| solubility | DMSO: 2 mg/mL, clear |
| web metadata keyword.default | 2-(4-{[2-(5-Chlorothiophen-2-yl)-5-ethyl-6-methylpyrimidin-4-yl]amino}phenyl)acetic acid,A-33 1 mg/mL solution for laboratory use,A-33 PDE4B inhibitor 915082-52-9,A-33 PDE4B inhibitor IC50 value,A-33 chemical structure and properties,A-33 cognitive function improvement study,A-33 compound for TNF-α production inhibition,A-33 for in vitro studies,A-33 intraperitoneal injection study,A-33 lab-grade PDE4B inhibitor,A-33 pharmacological profile and applications,A-33 research chemical for neuroscience applications,A-33 selective PDE4B inhibitor for research,PDE4B inhibitor A-33,Sigma-Aldrich A-33 |
| storage temp. | 2-8°C |
| SMILES string | O=C(O)CC1=CC=C(NC2=NC(C3=CC=C(Cl)S3)=NC(C)=C2CC)C=C1 |
| InChI key | FDVSPBLZPJMXFV-UHFFFAOYSA-N |
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