GYY 4137 morpholine salt

SKU: orb1219138

Description

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

Key Properties

• CAS Number: 106740-09-4
• MW: 376.47
• Purity: >98% (HPLC)
• Formula: C₁₁H₁₆NO₂PS₂·C₄H₉NO
• SMILES: SP(N1CCOCC1)(C2=CC=C(OC)C=C2)=S.N3CCOCC3
• Target: Others
• Solubility: DMSO:12.85mg/mL

Bioactivity

• In Vivo:
  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.
• In Vitro:
  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.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

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Others