199864-86-3
基本信息
4-(4-氟-1-萘基)-6-(1-甲基乙基)-2-嘧啶胺盐酸盐
RS 127445 hydrochloride NEW
4-(4-Fluoro-1-naphthyl)-6-isopropylpyriMidin-2-aMine
2-Amino-4-(4-fluoronaphth-1-yl)-6-isopropylpyrimidine hydrochloride
2-AMino-4-(4-fluoronaphth-1-yl)-6-isopropylpyriMidine Monohydrochloride
4-(4-Fluoro-1-naphthalenyl)-6-(1-methylethyl)-2-pyrimidinamine monohydrochloride
2-PyriMidinaMine, 4-(4-fluoro-1-naphthalenyl)-6-(1-Methylethyl)-, Monohydrochloride
物理化学性质
| 熔点 | 158 °C |
| 储存条件 | 2-8°C |
| 溶解度 | 二甲基亚砜：≥20mg/mL |
| 形态 | 粉末 |
| 颜色 | 白色至棕褐色 |
安全数据
| 危险性符号(GHS) |  GHS06 |
| 警示词 | 危险 |
| 危险性描述 | H301-H315-H319-H335 |
| 防范说明 | P301+P310+P330-P302+P352-P305+P351+P338 |
| 危险品标志 | T |
| 危险类别码 | 25-36 |
| 安全说明 | 26-45 |
| 危险品运输编号 | UN 2811 6.1 / PGIII |
| WGK Germany | 3 |
| 海关编码 | 2933.59.5300 |
4-(4-氟-1-萘基)-6-(1-甲基乙基)-2-嘧啶胺盐酸盐价格(试剂级)
| 报价日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
| 2024/11/08 | R0221 | RS-127445盐酸盐 RS-127445 Hydrochloride | 199864-86-3 | 10mg | 350元 |
| 2024/11/08 | R0221 | RS-127445盐酸盐 RS-127445 Hydrochloride | 199864-86-3 | 50mg | 1650元 |
常见问题列表
|
sPLA2 5.5 (pKi) |
5-HT 3 Receptor <6 (pKi) |
5-HT 5 Receptor <6 (pKi) |
5-HT 6 Receptor <6 (pKi) |
5-HT 2A Receptor 6.3 (pKi) |
5-HT 2C Receptor 6.4 (pKi) |
5-HT 2B Receptor 9.5 (pKi) |
RS-127445 is found to has nanomolar affinity for the 5-HT 2B receptor (pK i =9.5±0.1) and 1,000 fold selectivity for this receptor as compared to numerous other receptor and ion channel binding sites. RS-127445 potently displaces [ 3 H]-5-HT from human recombinant 5-HT 2B receptors expressed in CHO-K1 cells. The affinity (pK i value) of RS-127445 for the 5-HT 2B receptor is 9.5±0.1 (n=9). RS-127445 is selective for the 5-HT 2B receptor, having approximately 1000 fold lower affinity for the human recombinant 5-HT 2A , 5-HT 2C , 5-HT 5 , 5-HT 6 and 5-HT 7 receptors, a 5-HT 1A receptor in rat brain membranes, a 5-HT 1B/D receptor in bovine caudate, and a monoamine uptake site in rabbit platelets. RS-127445 potently blocks the 5-HT (10 nM) evoked increases in intracellular calcium concentrations in the HEK-293 cells expressing the 5-HT 2B receptor (pIC 50 of 10.4±0.1). In cells expressing human recombinant 5-HT 2B receptors, RS-127445 potently antagonizes 5-HT-evoked formation of inositol phosphates (pK B =9.5±0.1) and 5-HT-evoked increases in intracellular calcium (pIC 10 =10.4±0.1). RS-127445 also blocks 5-HT-evoked contraction of rat isolated stomach fundus (pA 2B =9.5±1.1) and (±)α-methyl-5-HT-mediated relaxation of the rat jugular vein (pA 2 =9.9±0.3).
In rats, the fraction of RS-127445 that is bioavailable via the oral or intraperitoneal routes is 14 and 60% respectively. Intraperitoneal administration of RS-127445 (5 mg/kg) produced plasma concentrations predicted to fully saturate accessible 5-HT 2B receptors for at least 4 h.RS-127445 (5 mg/kg) is administered to rats by oral, intraperitoneal and intravenous routes. Peak plasma concentrations are rapidly achieved with the highest concentrations being found at the first time-point measured following intravenous and intraperitonael administration (0.08 h) and by 0.25 h following dosing by the oral route of administration. RS-127445 is cleared from plasma with an estimated terminal elimination half-life of approximately 1.7 h. The bioavailability of RS-127445, when administered by the oral and intraperitoneal routes is approximately 14 and 62% of that obtained by intravenous administration. Approximately 60% of an intraperitoneal dose and 14% of the oral dose of RS-127445 (5 mg/kg) is bioavailable. RS-127445 (1-30 mg/kg), dose-dependently reduces faecal output, reaching significance at 10 and 30 mg/kg (n=6-11). In blood and brain, >98% of RS-127445 is protein-bound.