177172-49-5
中文名稱(chēng)
2-氯-N-[(1R)-1-(3-甲氧基苯基)乙基]苯丙胺鹽酸鹽
英文名稱(chēng)
2-Chloro-N-[(1R)-1-(3-methoxyphenyl)ethyl]-benzenepropanaminehydrochloride
CAS
177172-49-5
分子式
C18H23Cl2NO
分子量
340.287
MOL 文件
177172-49-5.mol
更新日期
2023/12/27 09:22:15
177172-49-5 結(jié)構(gòu)式
基本信息
中文別名
2-氯-N-[(1R)-1-(3-甲氧基苯基)乙基]苯丙胺鹽酸鹽 英文別名
R-568R 568 hydrochloride
Tecalcet (Hydrochloride)
R-568 hydrochloride >=95% (HPLC)
2-Chloro-N-[(1R)-1-(3-methoxyphenyl)ethyl]-benzenepropanaminehydrochloride
(R)-3-(2-Chlorophenyl)-N-(1-(3-methoxyphenyl)ethyl)propan-1-amine hydrochloride
3-(2-chlorophenyl)-N-[(1R)-1-(3-methoxyphenyl)ethyl]propan-1-amine, hydrochloride
Benzenepropanamine, 2-chloro-N-[(1R)-1-(3-methoxyphenyl)ethyl]-, hydrochloride (1:1)
物理化學(xué)性質(zhì)
熔點(diǎn)183.3-184.4 °C
儲(chǔ)存條件Inert atmosphere,Room Temperature
溶解度DMSO : 50 mg/mL (146.93 mM; Need ultrasonic)
形態(tài)粉末
顏色White to off-white
常見(jiàn)問(wèn)題列表
生物活性
Tecalcet Hydrochloride (R 568 Hydrochloride) 是一個(gè)口服有效的擬鈣劑，變構(gòu)正調(diào)控鈣敏感受體 (CaSR)。Tecalcet Hydrochloride (R 568 Hydrochloride) 可提高激活細(xì)胞外Ca2+的敏感性。體外研究
Tecalcet (NPS 568, 0.1-100 μM) increase [Ca
2+
]i in a concentrationdependent and stereoselective manner.
Tecalcet (NPS 568, 0.1-100 nM) shiftes the concentration-response curve for extracellular Ca
2+
to the left without affecting the maximal response and, thereby, decreases
the EC
50
value for extracellular Ca21 to 0.61±0.04 mM.
體內(nèi)研究
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)
2
D
3
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. |