Bioactivity | Tecalcet Hydrochloride (R 568 Hydrochloride), an orally active calcimimetic compound, allosterically and positively modulates the calcium-sensing receptor (CaSR). Tecalcet Hydrochloride (R 568 Hydrochloride) increases the sensitivity to activation by extracellular Ca2+[1][2][3]. |
Invitro | Tecalcet (NPS 568, 0.1-100 μM) increase [Ca2+]i in a concentrationdependent and stereoselective manner[3].Tecalcet (NPS 568, 0.1-100 nM) shiftes the concentration-response curve for extracellular Ca2+ to the left without affecting the maximal response and, thereby, decreasesthe EC50 value for extracellular Ca21 to 0.61±0.04 mM[3]. |
In Vivo | Tecalcet (1.5 and 15 mg/kg, orally, twice daily for 4 days) inhibits PT cell proliferation in rats with renal insufficiency[1]. Animal Model: |
Name | Tecalcet Hydrochloride |
CAS | 177172-49-5 |
Formula | C18H23Cl2NO |
Molar Mass | 340.29 |
Appearance | Solid |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
Reference | [1]. Wada, M., et al. The calcimimetic compound NPS R-568 suppresses parathyroid cell proliferation in rats with renal insufficiency. Control of parathyroid cell growth via a calcium receptor. Journal of Clinical Investigation 100(12), 2977-2983 (1997). [2]. Nemeth, E.F., et al. The parathyroid calcium receptor: a novel therapeutic target for treating hyperparathyroidism. Pediatr.Nephrol. 10(3), 275-279 (1996). [3]. Nemeth, E.F., et al. Calcimimetics with potent and selective activity on the parathyroid calcium receptor. Proceedings of the National Academy of Sciences of the United States of America 95(7), 4040-4045 (1998). |