TP-10

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

TP-10 是 PDE10A 对抗其他 PDE 的选择性抑制剂，IC50 为 0.8 nM。

TP-10 is a selective inhibitor of PDE10A against other PDEs with IC50 of 0.8 nM.(In Vivo):TP-10 is active in the mouse behavioral model for positive symptoms. TP-10 demonstrates good in vitro and in vivo activity with extremely high intrinsic clearance (CLint) of t>1000 mL/min/kg in mouse liver microsomes (MLM) in assay.

TP-10 (10 μg /mL; 24 h) affects total reactive oxygen species in human brain-derived cells (U-87 MG). Cell Viability Assay Cell Line:U-87 MG cells Concentration:10 μg/ml Incubation Time:24 hours Result:Decreased the total number of ROS-positive cells and showed no toxic effects to U-87 MG cells.

TP-10 (0.1-10 mg/kg; i.h. once) shows an effect on cyclic nucleotides. Animal Model:Male CD ratsDosage:0.1, 0.32, 1.0, 3.2 and 10 mg/kg Administration:Subcutaneous injection; 0.1-10 mg/kg once Result:Dose- and time-dependently increased the levels of both cGMP and cAMP in striatal of mice. Increased pCREB-LI level first and returned to basal levels after injected for 3 hours at a dose of 3.2 mg/kg.

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Angiogenesis

PDE

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898563-00-3

460.46

C26H19F3N4O

>98% (HPLC)

In Vitro:?DMSO : 100 mg/mL (217.18 mM)

FC(F)(F)Cn1cc(c(n1)-c1ccc(OCc2ccc3ccccc3n2)cc1)-c1ccncc1

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(-20℃)

With Ice Pack

≥ 2 years