NPS 2143 (hydrochloride)

Calcium-sensing receptor (CaSR) is a G protein-coupled receptor that is involved in calcium homeostasis. Activation of CaSR on parathyroid cells decreases the secretion of parathyroid hormone (PTH), which in turn reduces blood calcium concentration. NPS 2143 is a potent and selective antagonist of CaSR (IC50 = 43 nM) that stimulates PTH secretion from parathyroid cells in vitro (EC50 = 39 nM). It is effective in vivo, causing a sustained increase in plasma PTH in rats when given intravenously. Daily oral administration of NPS 2143 to osteopenic ovariectomized rats results in a dramatic increase in bone turnover, as well as increased circulating PTH levels.Formal Name: 2-chloro-6-[(2R)-3-[[1,1-dimethyl-2-(2-naphthalenyl)ethyl]amino]-2-hydroxypropoxy]-benzonitrile, monohydrochloride. CAS Number: 324523-20-8. Synonyms: SB-262470A. Molecular Formula: C24H25ClN2O2 . HCl. Formula Weight: 445.4. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 30 mg/ml, DMSO: 30 mg/ml, DMSO:PBS(pH 7.2) (1:3): 0.25 mg/ml, Ethanol: 2 mg/ml. lambdamax: 225 nm. SMILES: CC(NC[C@@H](O)COC1=C(C#N)C(Cl)=CC=C1)(C)CC2=CC3=CC=CC=C3C=C2.Cl. InChi Code: InChI=1S/C24H25ClN2O2.ClH/c1-24(2,13-17-10-11-18-6-3-4-7-19(18)12-17)27-15-20(28)16-29-23-9-5-8-22(25)21(23)14-26,/h3-12,20,27-28H,13,15-16H2,1-2H3,1H/t20-,/m1./s1. InChi Key: ZEBNDUQLNGYBNL-VEIFNGETSA-N.