| Bioactivity | PDE4B-IN-2 is an orally active and selective PDE4B inhibitor with an IC50 of 15 nM. PDE4B-IN-2 inhibits PDE4D (IC50=1.7 µM). PDE4B-IN-2 exhibits potent anti-inflammatory effects[1]. | ||||||||||||
| Invitro | PDE4B-IN-2 (compound 33) does not inhibit CYP1A2, CYP3A4, CYP2C9, and CYP2D (IC50>10 µM)[1].PDE4B-IN-2 inhibits LPS-induced TNF-aproduction in vitro from mouseperipheral blood mononuclear cell (PBMC; IC50=0.5 M)[1]. | ||||||||||||
| In Vivo | PDE4B-IN-2 (compound 33; 2 mg/kg; po) has a Cmax of 8.7 μg/mL and an AUC of 52.3 μg•h/mL in mice[1]. | ||||||||||||
| Name | PDE4B-IN-2 | ||||||||||||
| CAS | 915082-52-9 | ||||||||||||
| Formula | C19H18ClN3O2S | ||||||||||||
| Molar Mass | 387.88 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. Kenji Naganuma, et al. Discovery of selective PDE4B inhibitors. Bioorg Med Chem Lett. 2009 Jun 15;19(12):3174-6. |