NPS-2143

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

一种有效的、选择性的、口服活性的 CaSR 拮抗剂，IC50 为 43 nM。

A potent, selective and orally active CaSR antagonist with IC50 of 43 nM; does not inhibit cytoplasmic Ca2+ responses to glutamate in HEK 293 cells engineered to express mGluRs and GABAB receptors; stimulates parathyroid hormone (PTH ) secretion from bovine parathyroid cells in vitro (EC50=39 nM) and increases plasma PTH levels in vivo; also inhibits lipopolysaccharide-induced pulmonary inflammation.Osteoporosis Discontinued.

NPS-2143 (SB-262470A) stimulates parathyroid hormone (PTH) secretion from bovine parathyroid cells with EC50 of 41 nM. Moreover, NPS 214 also blocks the inhibitory effects of calcimimetic NPS R-467 on PTH secretion from bovine parathyroid cells and the inhibitory effects of extracellular Ca2+ on isoproterenol-stimulated increases in cyclic AMP formation.In HEK 293 cells transiently expressing hCaSRs, NPS-2143 significantly suppresses the kokumi taste by effectively inhibiting the activity of both GSH and γ-Glu-Val-Gly.A recent study shows that NPS-2143 treatment suppresses low molecular weight fractions of azuki hydrolysate-induced cholecystokinin (CCK) secretion in CaSR-transfected HEK 293 cells.

NPS-2143 (SB-262470A) results in a rapid 4- to 5-fold increase in plasma PTH levels in rats.?In normotensive rats, NPS-2143 administration (1 mg/kg, i.v.) markedly increases mean arterial blood pressure (MAP) in the presence of parathyroid glands.

NPS 2143 | SB-262470 | NPS2143 | SB 262470

GPCR/G Protein

CaSR

Ca(2+)receptor

Metabolic Disease

Osteoporosis

284035-33-2

408.9205

C24H25ClN2O2

>98% (HPLC)

10 mM in DMSO

CC(C)(CC1=CC2=CC=CC=C2C=C1)NC[C@H](COC3=C(C(=CC=C3)Cl)C#N)O

Benzonitrile, 2-chloro-6-[(2R)-3-[[1,1-dimethyl-2-(2-naphthalenyl)ethyl]amino]-2-hydroxypropoxy]-

(-20℃)

With Ice Pack

≥ 2 years