For research use only. Not for therapeutic Use.
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].
NOTUM can inactivate WNTs by functioning as a WNT lipase[2].
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].
| Catalog Number | I031026 |
| CAS Number | 1365060-22-5 |
| Synonyms | 2-(6-chloro-7-cyclopropylthieno[3,2-d]pyrimidin-4-yl)sulfanylacetic acid |
| Molecular Formula | C11H9ClN2O2S2 |
| Purity | ≥95% |
| InChI | InChI=1S/C11H9ClN2O2S2/c12-10-7(5-1-2-5)8-9(18-10)11(14-4-13-8)17-3-6(15)16/h4-5H,1-3H2,(H,15,16) |
| InChIKey | LJYRIWUQISYYHA-UHFFFAOYSA-N |
| SMILES | C1CC1C2=C(SC3=C2N=CN=C3SCC(=O)O)Cl |
| 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. |
