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78351-75-4

中文名稱 1-(3-氯苯胺基)-4-苯基酞嗪
英文名稱 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 2024/10/24 13:31:47
78351-75-4 結(jié)構(gòu)式 78351-75-4 結(jié)構(gòu)式

基本信息

中文別名
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
英文別名
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

物理化學性質(zhì)

儲存條件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
形態(tài)黃色固體
顏色白色至淺黃色

安全數(shù)據(jù)

危險性符號(GHS)GHS hazard pictograms
GHS07
警示詞警告
危險性描述H319-H315-H335
危險品標志Xi
危險類別碼36/37/38
安全說明26-36
海關(guān)編碼2933.99.8290

常見問題列表

生物活性
MY-5445 是一種特異性的 cGMP 磷酸二酯酶 PDE5 抑制劑,其 Ki 值為 1.3 μM。MY-5445 能抑制人血小板凝集。MY-5445 是一種 ABCG2 轉(zhuǎn)運蛋白調(diào)節(jié)劑,具有抗增殖活性。
靶點

PDE5

1.3 μM (Ki)

PDE5

6.7 μM (IC 50 )

PDE4

37 μM (IC 50 )

體外研究

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.
體內(nèi)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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