| Hazard Information | Back Directory | [Description]
CH5447240 is a potent Human Parathyroid Hormone Receptor 1 (hPTHR1) Agonist for Treatment of Hypoparathyroidism. CH5447240 exhibited a potent in vitro hPTHR1 agonist effect with EC20 of 3.0 nM and EC50 of 12 nM and showed excellent physicochemical properties, such as high solubility in fasted state simulated intestinal fluid and good metabolic stability in human liver microsomes. mportantly, CH5447240 showed 55% oral bioavailability, and a significantly elevated serum calcium level in hypocalcemic model rats. | [Uses]
CH5447240 is an agonist for parathyroid hormone receptor 1 (PTHR1), that inhibits human PTHR1 with an EC50 of 12 μM. CH5447240 exhibits good metabolic stability in human liver microsomes. CH5447240 increases serum calcium levels in rats. CH5447240 can be used in research about hypoparathyroidism[1]. | [IC 50]
PTH1R: 12 μM (EC50) | [References]
[1] Nishimura Y, et al., Development of a Novel Human Parathyroid Hormone Receptor 1 (hPTHR1) Agonist (CH5447240), a Potent and Orally Available Small Molecule for Treatment of Hypoparathyroidism. J Med Chem. 2018 Jul 26;61(14):5949-5962. DOI:10.1021/acs.jmedchem.8b00182 |
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Biorbyt Ltd.
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http://www.biorbyt.com |
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