| Identification | Back Directory | [Name]
A 33 | [CAS]
915082-52-9 | [Synonyms]
A-33
PDE4B-IN-2
Benzeneacetic acid, 4-[[2-(5-chloro-2-thienyl)-5-ethyl-6-methyl-4-pyrimidinyl]amino]- | [Molecular Formula]
C19H18ClN3O2S | [MDL Number]
MFCD31699853 | [MOL File]
915082-52-9.mol | [Molecular Weight]
387.88 |
| Hazard Information | Back Directory | [Uses]
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]. | [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. | [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].
| [IC 50]
PDE4B: 15 nM (IC50); PDE4D: 1.7 μM (IC50) | [storage]
Store at -20°C | [References]
[1] Kenji Naganuma, et al. Discovery of selective PDE4B inhibitors. Bioorg Med Chem Lett. 2009 Jun 15;19(12):3174-6. DOI:10.1016/j.bmcl.2009.04.121 |
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| Company Name: |
BOC Sciences
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16314854226 |
| Website: |
www.bocsci.com |
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