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324523-20-8

中文名稱 2-氯-6-[(2R)-3-[[1,1-二甲基-2-(2-萘基)乙基]氨基]-2-羥基丙氧基]苯腈鹽酸鹽
英文名稱 2-Chloro-6-[(2R)-3-[[1,1-dimethyl-2-(2-naphthalenyl)ethyl]amino]-2-hydroxypropoxy]benzonitrile hydrochloride
CAS 324523-20-8
分子式 C24H26Cl2N2O2
分子量 445.38
MOL 文件 324523-20-8.mol
324523-20-8 結構式 324523-20-8 結構式

基本信息

中文別名
NPS2143鹽酸鹽
2-氯-6-[(2R)-3-[[1,1-二甲基-2-(2-萘基)乙基]氨基]-2-羥基丙氧基]苯腈鹽酸鹽
英文別名
NPS-2143 HCL
NPS-2143 (Mono HCl)
NPS2143
NPS 2143 HCL
SB-262470-A hydrochloride
NPS2143 hydrochloride, >=98%
2-Chloro-6-[(2R)-3-[[1,1-dimethyl-2-(2-naphthalenyl)ethyl]amino]-2-hydroxypropoxy]benzonitrile hydrochloride
2-Chloro-6-[(2R)-3-[[1,1-dimethyl-2-(2-naphthalenyl)ethyl]amino]-2-hydroxypropoxy]-benzonitrile hydrochloride (1:1)

物理化學性質

儲存條件2-8°C
溶解度二甲基亞砜:>10mg/mL
形態(tài)粉末
顏色白色至米色
旋光性 (optical activity)[α]20/D +20 to +24°, c = 1.0 in methanol

安全數(shù)據(jù)

危險性符號(GHS)GHS hazard pictogramsGHS hazard pictograms
GHS07,GHS09
警示詞警告
危險性描述H302+H312+H332-H410
危險品標志Xn,N
危險類別碼20/21/22-50/53
安全說明36/37-60-61
危險品運輸編號UN 3077 9 / PGIII
WGK Germany3

常見問題列表

生物活性
NPS-2143 hydrochloride (SB-262470A hydrochloride),口服活性溶鈣劑,是選擇性的鈣敏感受體 (CaSR) 拮抗劑。NPS-2143 hydrochloride (SB-262470A hydrochloride) 通過激活表達人 Ca2+ 受體的 HEK 293 細胞中的 Ca2+ 受體而引起的胞漿 Ca2+ 濃度增加 (IC50=43 nM)。
體外研究

NPS-2143 hydrochloride (SB-262470A hydrochloride) stimulates parathyroid hormone (PTH) secretion from bovine parathyroid cells with EC 50 of 41 nM. Moreover, NPS-2143 hydrochloride 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.

體內研究

When infused intravenously in normal rats, NPS-2143 hydrochloride (SB-262470A hydrochloride) causes a rapid and large increase in plasma levels of PTH. Ca 2+ receptor antagonists are termed calcilytics and NPS-2143 is the first substance (either atomic or molecular) shown to possess such activity.
When administered together with an antiresorptive agent (estradiol), NPS 2143 causes an increase in trabecular bone volume and bone mineral density in osteopenic rats.

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