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78351-75-4

中文名称 1-(3-氯苯胺基)-4-苯基酞嗪
英文名称 MY-5445
CAS 78351-75-4
分子式 C20H14ClN3
分子量 331.8
MOL 文件 78351-75-4.mol
更新日期 2023/03/20 15:41:21
78351-75-4 结构式 78351-75-4 结构式

基本信息

中文别名
化合物MY-5445
1-(3-氯苯胺基)-4-苯基酞嗪
N-(3-氯苯基)-4-苯基酞嗪-1-胺
英文别名
MY-5445
MY 5445
MY5445
1-(3-CHLOROANILINO)-4-PHENYLPHTHALAZINE
1-(3-Chloroanilino)-4-phenylphthalazine >
1-(3-CHLOROPHENYLAMINO)-4-PHENYLPHTHALAZINE
N-(3-chlorophenyl)-4-phenylphthalazin-1-amine
N-(3-Chlorophenyl)-4-phenyl-1-phthalazinamine

物理化学性质

储存条件Store at RT
溶解度DMF: 2 mg/ml; DMSO: 2 mg/ml; DMSO:PBS(pH 7.2) (1:2): 0.3 mg/ml
形态黄色固体
颜色白色至浅黄色

安全数据

危险性符号(GHS)
GHS07
警示词警告
危险性描述H319-H315-H335
危险品标志Xi
危险类别码36/37/38
安全说明26-36
海关编码2933.99.8290

常见问题列表

生物活性
MY-5445 是一种特异性的 cGMP 磷酸二酯酶 PDE5 抑制剂,其 Ki 值为 1.3 μM。MY-5445 能抑制人血小板凝集。MY-5445 是一种 ABCG2 转运蛋白调节剂,具有抗增殖活性。
靶点

PDE5

1.3 μM (Ki)

PDE5

6.7 μM (IC 50 )

PDE4

37 μM (IC 50 )

体外研究

MY-5445 inhibits human platelet aggregation by increasing cyclic GMP content and that it provides a useful probe for elucidating the role of cyclic GMP in platelet aggregation .
MY-5445 selectively reverses ABCG2-mediated multidrug resistance in ABCG2-overexpressing cells.
MY-5445 reverses ABCG2-mediated multidrug resistance (MDR) by potentiating the cytotoxicity of an ABCG2 substrate drug in ABCG2-overexpressing multidrug-resistant cancer cells, possibly by modulating the function and/or the protein expression of ABCG2.
MY-5445 (3 μM; 48 hours) substantially increases the topotecan-induced apoptosis in S1-M1-80 cell.

Apoptosis Analysis

Cell Line: Human S1 colon cancer cells, S1-M1-80 cancer cells
Concentration: 3 μM
Incubation Time: 48 hours
Result: Enhanced drug-induced apoptosis in ABCG2-overexpressing cancer cells.
体内研究

MY-5445 (0.5-3 mg/kg; i.p.; twice a day; for 15 days) produces a significant relief of mechanical hypersensitivity.

Animal Model: C57BL/6J male mice
Dosage: 0.5 mg/kg, 3 mg/kg
Administration: Intraperitoneal injection, twice a day, for 15 days
Result: Alleviated the cuff-induced allodynia.
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