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Submit ReviewPF 04671536 hydrochloride is a potent and selective PDE8B/8A inhibitor (IC50 values are 1.3 and 1.9 nM, respectively). Exhibits selectivity for PDE8A/B over other PDEs (IC50 values are >10 μM) and a range of other targets. Increases glucose-dependent insulin secretion from human pacreatic islet cells. Orally bioavailable.
Sold for research purposes under agreement from Pfizer Inc
PF 04671536 hydrochloride is also offered as part of the Tocriscreen 2.0 Max. 了解 Tocris 化合物库的更多信息。
分子量 | 382.87 |
公式 | C14H18N8OS.HCl |
储存 | Desiccate at RT |
纯度 | ≥98% (HPLC) |
CAS Number | 1305116-67-9 |
PubChem ID | 131954582 |
InChI Key | KNBIGIZPAKPDTF-HNCPQSOCSA-N |
Smiles | CC1=NC(N)=C2N=NN(C2=N1)C[C@H]3CN(CCO3)CC4=NC=CS4.Cl |
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 | |||
water | 7.66 | 20 温和加热 | |
DMSO | 38.29 | 100 |
以下数据基于产品分子量 382.87。 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 | 2.61 mL | 13.06 mL | 26.12 mL |
5 mM | 0.52 mL | 2.61 mL | 5.22 mL |
10 mM | 0.26 mL | 1.31 mL | 2.61 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。
DeNinno et al (2012) Discovery of triazolopyrimidine-based PDE8B inhibitors: exceptionally ligand-efficient and lipophilic ligand-efficient compounds for the treatment of diabetes. Bioorg.Med.Chem.Lett. 22 5721 PMID: 22858141
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