(4-甲氧基苯基)吗啉基-二硫代膦酸与吗啉的化合物

生物活性体外研究体内研究 (4-甲氧基苯基)吗啉基-二硫代膦酸与吗啉的化合物试剂级价格

CAS号:106740-09-4
英文名:GYY 4137 Morpholine salt
中文名:(4-甲氧基苯基)吗啉基-二硫代膦酸与吗啉的化合物
CBNumber:CB02538277
分子式:C15H25N2O3PS2
分子量:376.474361
MOL File:106740-09-4.mol

(4-甲氧基苯基)吗啉基-二硫代膦酸与吗啉的化合物化学性质

熔点 :164-166℃
溶解度 :DMF: 20 mg/ml; DMSO: 15 mg/ml; PBS (pH 7.2): 3 mg/ml
形态 :White solid.
颜色 :White

(4-甲氧基苯基)吗啉基-二硫代膦酸与吗啉的化合物性质、用途与生产工艺

生物活性 GY4137 是一种缓释 H2S 供体，具有血管扩张和抗高血压活性。GY4137 还具有抗炎和抗癌活性。

体外研究

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.

体内研究

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.