1-(3-氯苯胺基)-4-苯基酞嗪

生物活性靶点体外研究体内研究 1-(3-氯苯胺基)-4-苯基酞嗪试剂级价格

1-(3-氯苯胺基)-4-苯基酞嗪

CAS号:78351-75-4
英文名:MY-5445
中文名:1-(3-氯苯胺基)-4-苯基酞嗪
CBNumber:CB9739543
分子式:C20H14ClN3
分子量:331.8
MOL File:78351-75-4.mol

1-(3-氯苯胺基)-4-苯基酞嗪化学性质

沸点 :539.7±50.0 °C(Predicted)
密度 :1.310±0.06 g/cm3(Predicted)
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
酸度系数(pKa) :4.91±0.30(Predicted)
形态 :Yellow solid.
颜色 :White to Light yellow

安全信息

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

1-(3-氯苯胺基)-4-苯基酞嗪性质、用途与生产工艺

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.