| Bioactivity | LP-922056 is an orally active, highly potent Notum Pectinacetylesterase inhibitor with EC50s of 21 nM, 55 nM in human and mouse cellular assay, respectively. LP-922056 significantly increases midshaft femur cortical bone thickness in mice and rats[1][2]. | ||||||||||||
| Target | EC50: 21 nM (human Notum Pectinacetylesterase) and 55 nM (mouse Notum Pectinacetylesterase) | ||||||||||||
| Invitro | NOTUM can inactivate WNTs by functioning as a WNT lipase[2]. | ||||||||||||
| In Vivo | LP-922056 (compound 44; 3-30 mg/kg; oral gavage; daily; for 25 days) causes an increase in cortical bone thickness at all doses[1]. LP-922056 (10 mg/kg; orally) achieves high Cmax (129 μM) and AUC (1533 μM•h)[1]. LP-922056 (10 mg/kg; daily diet; for 4 weeks) increases cortical bone thickness and strength in midshaft femur, bone mass in the femoral neck and vertebral body cortical shell in Twelve-week-old male mice[2]. Animal Model: | ||||||||||||
| Name | LP-922056 | ||||||||||||
| CAS | 1365060-22-5 | ||||||||||||
| Formula | C11H9ClN2O2S2 | ||||||||||||
| Molar Mass | 300.78 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. James E Tarver Jr, et al. Stimulation of cortical bone formation with thienopyrimidine based inhibitors of Notum Pectinacetylesterase. Bioorg Med Chem Lett. 2016 Mar 15;26(6):1525-1528. [2]. Robert Brommage, et al. NOTUM inhibition increases endocortical bone formation and bone strength. Bone Res. 2019 Jan 8;7:2. |
LP-922056
CAS: 1365060-22-5 F: C11H9ClN2O2S2 W: 300.78
LP-922056 is an orally active, highly potent Notum Pectinacetylesterase inhibitor with EC50s of 21 nM, 55 nM in human an
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