GYY 4137 morpholine salt

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

GYY4137是一种新型水溶性缓释H2S供体，具有血管扩张和抗高血压活性。

GYY4137 is a novel water-soluble and slow releasing H2S donor with vasodilator and antihypertensive activity.?GYY4137 also exhibits anti-inflammatory and anticancer activity.

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 daysResult:Reduced tumor volume by 52.5±9.2% and 55.3±5.7% in HL-60 and MV4–11 injected animals.

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Others

Other Targets

Others

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106740-09-4

376.47

C11H16NO2PS2·C4H9NO

>98% (HPLC)

DMSO:12.85mg/mL

SP(N1CCOCC1)(C2=CC=C(OC)C=C2)=S.N3CCOCC3

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(-20℃)

With Ice Pack

≥ 2 years