4-(4-氟-1-萘基)-6-(1-甲基乙基)-2-嘧啶胺盐酸盐
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- CAS号:
- 199864-86-3
- 英文名:
- 2-PyriMidinaMine, 4-(4-fluoro-1-naphthalenyl)-6-(1-Methylethyl)-, Monohydrochloride
- 英文别名:
- MT 500 Hydrochloride;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
- 中文名:
- 4-(4-氟-1-萘基)-6-(1-甲基乙基)-2-嘧啶胺盐酸盐
- 中文别名:
- 4-(4-氟萘-1-基)-6-异丙基嘧啶-2-胺盐酸盐;4-(4-氟-1-萘基)-6-(1-甲基乙基)-2-嘧啶胺盐酸盐
- CBNumber:
- CB42609717
- 分子式:
- C17H17ClFN3
- 分子量:
- 317.7883832
- MOL File:
- 199864-86-3.mol
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4-(4-氟-1-萘基)-6-(1-甲基乙基)-2-嘧啶胺盐酸盐化学性质
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熔点:
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158 °C
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储存条件:
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2-8°C
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溶解度:
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DMSO: ≥20mg/mL
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形态:
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powder
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颜色:
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white to tan
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4-(4-氟-1-萘基)-6-(1-甲基乙基)-2-嘧啶胺盐酸盐性质、用途与生产工艺
RS-127445 hydrochloride 是一种有效的,具有口服活性的,高亲和力选择性 5-HT2B 受体拮抗剂,pKi 为 9.5,比作用于其他受体和离子通道的选择性高 1000 倍。
sPLA2
5.5 (pKi)
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5-HT
3
Receptor
<6 (pKi)
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5-HT
5
Receptor
<6 (pKi)
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5-HT
6
Receptor
<6 (pKi)
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5-HT
2A
Receptor
6.3 (pKi)
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5-HT
2C
Receptor
6.4 (pKi)
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5-HT
2B
Receptor
9.5 (pKi)
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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.
4-(4-氟-1-萘基)-6-(1-甲基乙基)-2-嘧啶胺盐酸盐
上下游产品信息
上游原料
下游产品
更新日期 | 产品编号 | 产品名称 | CAS编号 | 包装 | 价格 |
---|
2024/08/19 | R0221 | RS-127445盐酸盐 RS-127445 Hydrochloride | 199864-86-3 | 10mg | 350元 |
2024/08/19 | R0221 | RS-127445盐酸盐 RS-127445 Hydrochloride | 199864-86-3 | 50mg | 1650元 |
4-(4-氟-1-萘基)-6-(1-甲基乙基)-2-嘧啶胺盐酸盐
生产厂家
199864-86-3, 4-(4-氟-1-萘基)-6-(1-甲基乙基)-2-嘧啶胺盐酸盐 相关搜索:
- 17H16FN3HCl
- 4-(4-氟萘-1-基)-6-异丙基嘧啶-2-胺盐酸盐
- 4-(4-氟-1-萘基)-6-(1-甲基乙基)-2-嘧啶胺盐酸盐
- 199864-86-3
- RS 127445 hydrochloride NEW
- 4-(4-Fluoro-1-naphthalenyl)-6-(1-methylethyl)-2-pyrimidinamine monohydrochloride
- 4-(4-Fluoro-1-naphthyl)-6-isopropylpyriMidin-2-aMine
- MT 500 Hydrochloride
- 2-AMino-4-(4-fluoronaphth-1-yl)-6-isopropylpyriMidine Monohydrochloride
- 2-PyriMidinaMine, 4-(4-fluoro-1-naphthalenyl)-6-(1-Methylethyl)-, Monohydrochloride
- 2-Amino-4-(4-fluoronaphth-1-yl)-6-isopropylpyrimidine hydrochloride