ACOLBIFENE;EM652
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- CAS号:
- 182167-02-8
- 英文名:
- Sch 57068
- 英文别名:
- Em-652;Em 652;CS-1409;Sch 57068;ACOLBIFENE;EM652;Acolbifene (EM 652, SCH57068);EM652; EM-652; SCH-57068; SCH 57068;EM 652; EM-652; EM652; SCH57068; SCH-57068; SCH 57068.;(S)-3-(4-hydroxyphenyl)-4-Methyl-2-[4-[2-(1-piperidinyl)ethoxy]phenyl]-2H-1-benzopyran-7-ol;(2S)-3-(4-Hydroxyphenyl)-4-methyl-2-[4-[2-(1-piperidinyl)ethoxy]phenyl]-2H-1-benzopyran-7-ol
- 中文名:
- ACOLBIFENE;EM652
- 中文别名:
- 阿考比芬;化合物 T10239
- CBNumber:
- CB32495544
- 分子式:
- C29H31NO4
- 分子量:
- 457.56
- MOL File:
- 182167-02-8.mol
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ACOLBIFENE;EM652化学性质
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沸点:
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651.5±55.0 °C(Predicted)
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密度:
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1.217±0.06 g/cm3(Predicted)
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溶解度:
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DMSO:50.0(Max Conc. mg/mL);109.28(Max Conc. mM)
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形态:
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A solid
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酸度系数(pKa):
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9.70±0.40(Predicted)
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ACOLBIFENE;EM652性质、用途与生产工艺
Acolbifene (EM-652) 是 EM800 的活性代谢物，是具有口服活性的纯抗刺激素和选择性的雌激素受体 (ER) 的拮抗剂，其在 T-47D 细胞中的 IC50 值为 0.110 nM。Acolbifene (EM-652) 具有抗癌活性。
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Estrogen receptor
0.110 nM (IC
50
, T-47D cells)
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Acolbifene (ACOL) does not affect pathways of cholesterol synthesis, supporting the involvement of the clearance-related receptors in its hypocholesterolemic action.
Acolbifene (EM-652) shows no agonistic activity on ERα and ERβ transcriptional function and blocks the estradiol (E2)-mediated activation of both ERα and ERβ.
Acolbifene (EM-652) shows the most potent inhibition of estradiol-stimulated cell proliferation in human breast cancer cancer cells (ZR-75-1, MCF-7, T-47D) and is devoid of any intrinsic estrogenic activity.
Acolbifene (ACOL) reduces food intake and strongly decreases cholesterolemia in rats fed a cholesterol-free diet.
Acolbifene (ACOL) reduces food intake (16%) and weight gain (45%, mainly fat) similarly in both dietary cohorts.
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Animal Model:
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Female Sprague-Dawley rats (n = 42) initially weighing 175-200 g.
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Dosage:
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2.5 mg/kg.
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Administration:
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Oral gavage, once daily for 21 d.
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Result:
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Prevents tumor growth in rats.
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ACOLBIFENE;EM652
上下游产品信息
上游原料
下游产品
182167-02-8, ACOLBIFENE;EM652 相关搜索:
- 化学物质-药物相关的化学物质
- 化合物 T10239
- 阿考比芬
- 182167-02-8
- 2H-1-Benzopyran-7-ol, 3-(4-hydroxyphenyl)-4-methyl-2-[4-[2-(1-piperidinyl)ethoxy]phenyl]-, (2S)-
- EM 652; EM-652; EM652; SCH57068; SCH-57068; SCH 57068.
- CS-1409
- EM652; EM-652; SCH-57068; SCH 57068
- (2S)-3-(4-Hydroxyphenyl)-4-methyl-2-[4-[2-(1-piperidinyl)ethoxy]phenyl]-2H-1-benzopyran-7-ol
- Acolbifene (EM 652, SCH57068)
- ACOLBIFENE;EM652
- (S)-3-(4-hydroxyphenyl)-4-Methyl-2-[4-[2-(1-piperidinyl)ethoxy]phenyl]-2H-1-benzopyran-7-ol
- Sch 57068
- Em-652
- Em 652
- 2H-1-Benzopyran-7-ol, 3-(4-hydroxyphenyl)-4-methyl-2-(4-(2-(1-piperidinyl)ethoxy)phenyl)-, (S)-
- ( )-(2S)-3-(4-Hydroxyphenyl)-4-methyl-2-(4-(2-(piperidin-1-yl)ethoxy)phenyl)-2H-1-benzopyran-7-ol