网站主页 >> CAS数据库列表 >> (2E)-N-(2,3-二氢-1,4-苯并二噁英-6-基)-3-[4-(1,1-二甲基乙基)苯基]-2-丙酰胺
(2E)-N-(2,3-二氢-1,4-苯并二噁英-6-基)-3-[4-(1,1-二甲基乙基)苯基]-2-丙酰胺
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- CAS号:
- 545395-94-6
- 英文名:
- AMG 9810
- 英文别名:
- 9810;CS-2548;AMG 9810;AMG 9810;AMG-9810;AMG 9810 >=98% (HPLC), powder;(2E)-N-(2,3-Dihydro-1,4-benzodi;3-[4-(TERT-BUTYL)PHENYL]-N-(2,3-DIHYDRO-1,4-BENZODIOXIN-6-YL)ACRYLAMIDE;3-(4-tert-Butyl-phenyl)-N-(2,3-dihydro-benzo[1,4]dioxin-6-yl)-acrylamide;(2E)-3-(4-tert-butylphenyl)-N-(2,3-dihydro-1,4-benzodioxin-6-yl)prop-2-enamide;(2E)-N-(2,3-Dihydro-1,4-benzodioxin-6-yl)-3-[4-(1,1-dimethylethyl)phenyl]-2-propanamide
- 中文名:
- (2E)-N-(2,3-二氢-1,4-苯并二噁英-6-基)-3-[4-(1,1-二甲基乙基)苯基]-2-丙酰胺
- 中文别名:
- 化合物AMG9810;AMG 9810,竞争性香草酸TRPV1受体拮抗剂;(E)-3-(4-(叔丁基)苯基)-N-(2,3-二羟基苯并[B][1,4]二氧杂环己烷基-6-基)丙烯酰胺;(2E)-N-(2,3-二氢-1,4-苯并二噁英-6-基)-3-[4-(1,1-二甲基乙基)苯基]-2-丙酰胺
- CBNumber:
- CB0306302
- 分子式:
- C21H23NO3
- 分子量:
- 337.41
- MOL File:
- 545395-94-6.mol
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(2E)-N-(2,3-二氢-1,4-苯并二噁英-6-基)-3-[4-(1,1-二甲基乙基)苯基]-2-丙酰胺化学性质
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沸点:
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512.5±50.0 °C(Predicted)
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密度:
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1.175±0.06 g/cm3(Predicted)
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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: >5mg/mL
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酸度系数(pKa):
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12.22±0.20(Predicted)
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形态:
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powder
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颜色:
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white to beige
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(2E)-N-(2,3-二氢-1,4-苯并二噁英-6-基)-3-[4-(1,1-二甲基乙基)苯基]-2-丙酰胺性质、用途与生产工艺
AMG-9810 是一种有效的、竞争性和选择性的 vanilloid receptor 1 (TRPV1) 的拮抗剂,可抑制辣椒素capsaicin的活化,对人TRPV1和大鼠TRPV1的IC50值分别为24.5 nM和85.6 nM。AMG-9810 可阻止所有已知模式的TRPV1激活,包括protons-,heat-和endogenous ligands,例如anandamide,N-arachidonyl dopamine和oleoyldopamine。AMG-9810 可显著降低 TLR2 和 TLR4 的mRNA表达。AMG-9810 还可通过 EGFR/Akt/mTOR 信号通路来促进小鼠皮肤肿瘤发生的缓解。
Target | Value |
TLR2
()
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TLR4
()
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hTRPV1
(Cell-free assay)
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24.5 nM
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rTRPV1
(Cell-free assay)
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85.6 nM
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AMG9810 is a competitive antagonist of capsaicin activation (IC
50
value for human TRPV1, 24.5±15.7 nM; rat TRPV1, 85.6±39.4 nM) and blocks all known modes of TRPV1 activation, including protons (IC
50
value for rat TRPV1, 294±192 nM; human TRPV1, 92.7±72.8 nM), heat (IC
50
value for rat TRPV1, 21±17 nM; human TRPV1, 15.8±10.8 nM), and endogenous ligands, such as anandamide, N-arachidonyl dopamine, and oleoyldopamine. AMG9810 blocks capsaicin-evoked depolarization and calcitonin gene-related peptide release in cultures of rat dorsal root ganglion primary neurons. AMG9810 inhibits capsaicin-, proton-, heat-, and endogenous ligand-induced uptake of
45
Ca
2+
into TRPV1-expressing cells.
AMG9810 is effective at preventing capsaicin-induced eye wiping in a dose-dependent manner, and it reverses thermal and mechanical hyperalgesia in a model of inflammatory pain induced by intraplantar injection of complete Freund's adjuvant. At effective doses, AMG9810 does not show any significant effects on motor function. AMG9810 is the first cinnamide TRPV1 antagonist reported to block capsaicin-induced eye wiping behavior and reverse hyperalgesia in an animal model of inflammatory pain. AMG9810, promotes mouse skin tumor development. The topical application of AMG9810 results in a significant increase in the expression level of the epidermal growth factor receptor (EGFR) and its downstream Akt/mammalian target of rapamycin (mTOR)-signaling pathway.
(2E)-N-(2,3-二氢-1,4-苯并二噁英-6-基)-3-[4-(1,1-二甲基乙基)苯基]-2-丙酰胺
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 |
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2024/01/25 | HY-101736 | AMG9810 | | 1 mg | 200元 |
2024/01/25 | HY-101736 | (2E)-N-(2,3-二氢-1,4-苯并二噁英-6-基)-3-[4-(1,1-二甲基乙基)苯基]-2-丙酰胺 AMG9810 | 545395-94-6 | 5mg | 500元 |
(2E)-N-(2,3-二氢-1,4-苯并二噁英-6-基)-3-[4-(1,1-二甲基乙基)苯基]-2-丙酰胺
生产厂家
545395-94-6, (2E)-N-(2,3-二氢-1,4-苯并二噁英-6-基)-3-[4-(1,1-二甲基乙基)苯基]-2-丙酰胺 相关搜索:
- Vanilloid/TRPV channel
- 合成有机化合物配体
- AMG 9810,竞争性香草酸TRPV1受体拮抗剂
- (E)-3-(4-(叔丁基)苯基)-N-(2,3-二羟基苯并[B][1,4]二氧杂环己烷基-6-基)丙烯酰胺
- 化合物AMG9810
- (2E)-N-(2,3-二氢-1,4-苯并二噁英-6-基)-3-[4-(1,1-二甲基乙基)苯基]-2-丙酰胺
- 545395-94-6
- (2E)-N-(2,3-Dihydro-1,4-benzodi
- Transient receptor potential channels,inhibit,Inhibitor,AMG-9810,AMG9810,AMG 9810,TRP Channel
- (2E)-3-(4-tert-butylphenyl)-N-(2,3-dihydro-1,4-benzodioxin-6-yl)prop-2-enamide
- AMG 9810 >=98% (HPLC), powder
- 9810
- 3-(4-tert-Butyl-phenyl)-N-(2,3-dihydro-benzo[1,4]dioxin-6-yl)-acrylamide
- AMG 9810;AMG-9810
- CS-2548
- 2-PropenaMide, N-(2,3-dihydro-1,4-benzodioxin-6-yl)-3-[4-(1,1-diMethylethyl)phenyl]-, (2E)-
- (2E)-N-(2,3-Dihydro-1,4-benzodioxin-6-yl)-3-[4-(1,1-dimethylethyl)phenyl]-2-propanamide
- (2E)-N-(2,3-DIHYDRO-1,4-BENZODIOXIN-6-YL)-3-[4-(1,1-DIMETHYLETHYL)PHENYL]-2-PROPENAMIDE
- AMG 9810
- 3-[4-(TERT-BUTYL)PHENYL]-N-(2,3-DIHYDRO-1,4-BENZODIOXIN-6-YL)ACRYLAMIDE