(4-甲氧基苯基)吗啉基-二硫代膦酸与吗啉的化合物
| 中文名称 | (4-甲氧基苯基)吗啉基-二硫代膦酸与吗啉的化合物 |
|---|---|
| 中文同义词 | (4-甲氧基苯基)吗啉基-二硫代膦酸与吗啉的化合物;4-甲氧基苯基硫代磷酸酯(吗啉)吗啉盐 4-METHOXYPHENYL(MORPHOLINO)PHOSPHINODITHIOATE MORPHOLINIUM SALT;4-甲氧基苯基硫代磷酸酯(吗啉)吗啉盐;化合物GYY 4137 MORPHOLINE SALT;(4-甲氧基苯基)(吗啉)二硫代单膦酸吗啉盐;GYY 4137,水溶性,缓释H 2 S供体 |
| 英文名称 | GYY 4137 Morpholine salt |
| 英文同义词 | GYY 4137 MORPHOLINE SALT;GYY 4137;(4-Methoxyphenyl)morpholino-phosphinodithioic acid compound with morpholine;P-(4-Methoxyphenyl)-P-4-morpholinylphosphinodithioic acid morpholine salt;GYY4137;GYY-4137;GYY 4137;morpholin-4-ium (4-methoxyphenyl)(morpholino)phosphinodithioate;(4-methoxyphenyl)-morpholin-4-yl-sulfanylidene-sulfido-λ5-phosphane,morpholin-4-ium;4-Methoxyphenyl(morpholino)phosphinodithioate morpholinium salt |
| CAS号 | 106740-09-4 |
| 分子式 | C15H25N2O3PS2 |
| 分子量 | 376.474361 |
| EINECS号 | |
| 相关类别 | 抑制剂;试剂盒-细胞分析试剂盒 |
| Mol文件 | 106740-09-4.mol |
| 结构式 |  |
(4-甲氧基苯基)吗啉基-二硫代膦酸与吗啉的化合物 性质
| 熔点 | 164-166℃ |
|---|---|
| 溶解度 | DMF：20mg/mL； DMSO：15mg/mL； PBS（pH 7.2）：3 mg/mL |
| 形态 | 白色固体。 |
| 颜色 | 白色 |
GYY4137 (400-800 µM) causes concentration-dependent killing of seven different human cancer cell lines (HeLa, HCT-116, Hep G2, HL-60, MCF-7, MV4-11 and U2OS) but did not affect survival of normal human lung fibroblasts (IMR90, WI-38).
GYY4137 (0.1-0.5 mM) decreases LPS-induced production of nitrite (NO2−), PGE2, TNF-α and IL-6 from human synoviocytes (HFLS) and articular chondrocytes (HAC), reduces the levels and catalytic activity of inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2) and reduced LPS-induced NF-κB activation.
Cell Viability Assay
| Cell Line: | HeLa, HCT-116, Hep G2, HL-60, MCF-7, MV4-11 and U2OS |
| Concentration: | 400 or 800 µM |
| Incubation Time: | 5 days |
| Result: | Significantly affected cancer cell survivability. |
GYY4137 (100-300 mg/kg; i.p.; daily for 14 days) significantly reduces the tumor volume in both animal models, in a dose-dependent manner.
In the complete Freund's adjuvant (CFA)-treated mouse, GYY4137 (50 mg/kg, i.p.) injected 1 hr prior to CFA increased knee joint swelling while an anti-inflammatory effect, as demonstrated by reduced synovial fluid myeloperoxidase (MPO) and N-acetyl-β-D-glucosaminidase (NAG) activity and decreased TNF-α, IL-1β, IL-6 and IL-8 concentration, was apparent when GYY4137 was injected 6 hrs after CFA.
GYY4137 significantly inhibited tumor growth in the subcutaneous HepG2 xenograft model by inhibiting STAT3 activation and its target gene expression.
GYY4137 prevents nitrative stress and α-synuclein nitration in an MPTP mouse model of parkinson’s disease.
| Animal Model: | Female, severe combined immunodeficiency (SCID) mice (bearing HL-60 or MV4-11 cells) |
| Dosage: | 100, 200 and 300 mg/kg |
| Administration: | I.p.; daily for 14 days |
| Result: | Reduced tumor volume by 52.5±9.2% and 55.3±5.7% in HL-60 and MV4–11 injected animals. |
安全信息
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2024/04/30 | HY-107632 | GYY4137 | 5 mg | 350元 | |
| 2024/04/30 | HY-107632 | (4-甲氧基苯基)吗啉基-二硫代膦酸与吗啉的化合物 GYY4137 | 106740-09-4 | 10mg | 550元 |