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Submit ReviewA 33 is a potent and selective PDE4B inhibitor (IC50 = 15 nM); exhibits >100-fold selectivity for PDE4B over 4D. Regulates cAMP in inflammatory cells. Inhibits LPS-induced TNF-α production and neutrophil accumulation in mouse lungs. Reduces microglial and neutrophil activation, and improves behavioral deficits in a traumatic brain injury model in vivo. Also exhibits antidepressant-like effects. Orally bioavailable.
分子量 | 387.88 |
公式 | C19H18ClN3O2S |
储存 | Store at -20°C |
纯度 | ≥98% (HPLC) |
CAS Number | 915082-52-9 |
PubChem ID | 15951010 |
InChI Key | FDVSPBLZPJMXFV-UHFFFAOYSA-N |
Smiles | CCC1=C(N=C(C2=CC=C(S2)Cl)N=C1NC3=CC=C(C=C3)CC(O)=O)C |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 38.79 | 100 |
以下数据基于产品分子量 387.88。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 2.58 mL | 12.89 mL | 25.78 mL |
5 mM | 0.52 mL | 2.58 mL | 5.16 mL |
10 mM | 0.26 mL | 1.29 mL | 2.58 mL |
50 mM | 0.05 mL | 0.26 mL | 0.52 mL |
参考文献是支持产品生物活性的出版物。
Naganuma et al (2009) Discovery of selective PDE4B inhibitors. Bioorg.Med.Chem.Lett. 19 3174 PMID: 19447034
Zhang et al (2017) Comparison of the pharmacological profiles of selective PDE4B and PDE4D inhibitors in the central nervous system. Sci.Rep. 7 40115 PMID: 28054669
Wilson et al (2017) Therapeutic benefits of phosphodiesterase 4B inhibition after traumatic brain injury. PLoS One 12 e0178013 PMID: 28542295
If you know of a relevant reference for A 33, please let us know.
关键词: A 33, A 33 supplier, A33, potent, selective, PDE4B, phosphodiesterase, inhibitors, inhibits, orally, bioavailable, anti-inflammatory, antidepressant, TBI, traumatic, brain, injury, Phosphodiesterases, 6313, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 A 33 的部分引用包括:
Eyal et al (2022) PDE4B Is a Homeostatic Regulator of Cyclic AMP in Dendritic Cells. Front Pharmacol 13 833832 PMID: 35387344
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