Tecalcet hydrochloride

Research use only, not for human use.

Tecalcet (R-568;NPS R-568;KRN-568;NPS-568) is a calcimimetic acting agent and potent, selective positive allosteric modulator (agonist) of CaSR.

Tecalcet (R-568;NPS R-568;KRN-568;NPS-568) is a calcimimetic acting agent and potent, selective positive allosteric modulator (agonist) of CaSR; potentiates the effects of extracellular Ca2+ on [Ca2+]i and PTH secretion without effect in the absence of extracellular Ca2+, does not affect responses elicited by the homologous mGluRs; prevents parathyroid hyperplasia in rats with severe secondary hyperparathyroidism.Hyperparathyroidism Phase 2 Discontinued.

Tecalcet (NPS 568, 0.1-100 μM) increase [Ca2+]i in a concentrationdependent and stereoselective manner.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, decreases the EC50 value for extracellular Ca21 to 0.61±0.04 mM.

Tecalcet (1.5 and 15 mg/kg, orally, twice daily for 4 days) inhibits PT cell proliferation in rats with renal insufficiency. Animal Model:10-wk-old Male Sprague-Dawley rats weighing 310-350 g.Dosage:1.5 and 15 mg/kg.Administration:Orally twice daily for 4 days.Result:Did not significantly change serum 1,25 (OH)2D3 levels. In contrast, serum PTH levels were reduced by in a dose-dependent manner.Clearly reduced the number of BrdU-positive PT cells by 20% at a low dose (1.5 mg/kg body wt), and by 50% at a high dose (15 mg/kg body wt), indicating an antiproliferative effect on PT cells.Reduced PT cell volume in a dose-dependent manner.

R-568 | NPS R-568 | KRN-568 | NPS-568

GPCR/G Protein

CaSR

CaSR

Endocrinology

Hyperparathyroidism

177172-49-5

340.288

C18H23Cl2NO

>98% (HPLC)

In Vitro:?DMSO : 50 mg/mL (146.93 mM)

CC(C1=CC(=CC=C1)OC)NCCCC2=CC=CC=C2Cl.Cl

2-chloro-N-[(1R)-1-(3-methoxyphenyl)ethyl]-benzenepropanamine, monohydrochloride

(-20℃)

With Ice Pack

≥ 2 years