LP-922056

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

LP-922056 是一种 Notum 果胶乙酰酯酶抑制剂，对人和小鼠的 EC50 值分别为 21 nM、55 nM。

LP-922056 is an inhibitor of Notum Pectinacetylesterase with EC50 values of 21 nM, 55 nM for human and mouse, respectively.(In Vitro):LP-922056 can be used as a complementary chemical tool for exploring the role of Notum in Wnt signaling.(In Vivo):In mice, LP-922056 (3, 10, 30 mg/kg; gavage) significantly increases midshaft femur cortical bone thickness. LP-922056 (10 mg/kg) achieved high Cmax of 129 μM and AUC of 1533 μM?h while volume of distribution is 0.13 L/kg and low clearance is 0.49 mL/min?kg. LP-922056 (10?mg/kg; oral) increases cortical bone thickness and strength in the midshaft femur, bone mass in the femoral neck, and vertebral body cortical shell.

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Animal Model:F1 male hybrid (129xC57) mice at 8.7 weeks of ageDosage:3, 10, 30 mg/kg Administration:Oral gavage; daily; for 25 days Result:Caused an increase in cortical bone thickness at all doses.Animal Model:Mouse Dosage:10 mg/kg (Pharmacokinetic Analysis) Administration:Orally Result:Achieved high Cmax (129 μM) and AUC (1533 μM?h) while has low clearance (0.49 mL/min?kg) and volume of distribution (0.13 L/kg).

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Wnt/Notch/Hedgehog

Wnt/beta/catenin

sAHP

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1365060-22-5

300.78

C11H9ClN2O2S2

>98% (HPLC)

In Vitro:?DMSO : 125 mg/mL (415.59 mM)

O=C(O)CSC1=NC=NC2=C1SC(Cl)=C2C3CC3

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(-20℃)

With Ice Pack

≥ 2 years