LP-922056 is an orally active, potent and selective NOTUM pectinacetylesterase inhibitor that activates Wnt signaling. LP-922056 stimulates endocortical bone formation in rodents and in humanized NOTUM mouse line.
orally active, potent and selective NOTUM pectinacetylesterase inhibitor that activates Wnt signaling and stimulates bone formation
Storage Class
11 - Combustible Solids
wgk_germany
WGK 3
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A group of small molecule thienopyrimidine inhibitors of Notum Pectinacetylesterase are described. We explored both 2-((5,6-thieno[2,3-d]pyrimidin-4-yl)thio)acetic acids and 2-((6,7-thieno[3,2-d]pyrimidin-4-yl)thio)acetic acids. In both series, highly potent, orally active Notum Pectinacetylesterase inhibitors were identified.
The disability, mortality and costs caused by non-vertebral osteoporotic fractures are enormous. Existing osteoporosis therapies are highly effective at reducing vertebral but not non-vertebral fractures. Cortical bone is a major determinant of non-vertebral bone strength. To identify novel osteoporosis drug
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