| Size | Price | Stock | Qty |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg | |||
| Other Sizes |
| Targets |
GYY 4137 is a hydrogen sulfide (H2S) donor. H2S is an endogenous gasotransmitter involved in various physiological processes, including vasodilation, inflammation, and cytoprotection. GYY 4137 releases H2S slowly by hydrolysis in aqueous solutions.
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| ln Vitro |
GYY4137 (400-800 μM) kills seven distinct human cancer cell lines (HeLa, HCT-116, Hep G2, HL-60, MCF-7, MV4-11, and U2OS) in a concentration-dependent manner, while it has no effect on the survival of human lung fibroblasts that are normal cells (IMR90, WI-38) [2]. In human synoviocytes (HFLS) and articular chondrocytes (HAC), GYY4137 (0.1-0.5 mM) decreases LPS-induced production of nitrite (NO2), PGE2, TNF-α, and IL-6. It also decreases inducible nitric acid salt levels and catalytic activity of oxidative oxide synthase (iNOS) and cyclooxygenase-2 (COX-2) as well as LPS-induced NF-κB activation [3].
GYY 4137 releases H2S slowly in aqueous solutions. It exhibits vasodilator activity in vitro and in vivo. It protects against myocardial ischemia and reperfusion injury by attenuating oxidative stress and apoptosis. It also exhibits potent anticancer activity. |
| ln Vivo |
In two animal models, GYY4137 (100–300 mg/kg; intraperitoneal injection; once daily for 14 days) significantly and dose-dependently decreased the volume of tumors [2]. ?GYY4137 (50 mg/kg, i.p.) was injected one hour prior to complete Freund's adjuvant (CFA) treatment in mice. This resulted in an increase in knee joint swelling as well as anti-inflammatory effects, as demonstrated by the decrease in (MPO) and N. Acetyl-β-D-glucosaminidase (NAG) activity was considerably decreased and TNF-α, IL-1β, IL-6, and IL-8 concentrations were decreased when GYY4137 was administered six hours after CFA [3]. ?In the subcutaneous HepG2 xenograft model, GYY4137 effectively suppresses tumor development by blocking both STAT3 activation and the expression of its target gene [4]. ?GYY4137 inhibits α-synuclein nitration and nitrative stress in the MPTP animal model of Parkinson's disease [5].
GYY 4137 exhibits vasodilator and antihypertensive activity in vivo. It protects against myocardial ischemia and reperfusion injury in rats. These effects are attributed to the release of H2S, which has cardioprotective properties. |
| Enzyme Assay |
The in vitro assay for GYY 4137 involves measuring the release of H2S in aqueous solutions. This can be done using a sulfide-selective electrode or a colorimetric assay. The rate of H2S release is determined.
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| Cell Assay |
Cell Viability Assay[2]
Cell Types: HeLa, HCT-116, Hep G2, HL-60, MCF-7, MV4-11 and U2OS Tested Concentrations: 400 or 800 µM Incubation Duration: 5 days Experimental Results: Dramatically affected cancer cells survivability. Specific in vitro cell-based assay protocols for GYY 4137 are not detailed. Its cytoprotective effects can be assessed in cell culture models of oxidative stress or ischemia-reperfusion. Cells are treated with GYY 4137, and cell viability, apoptosis, and oxidative stress markers are measured. |
| Animal Protocol |
Animal/Disease Models: Female, severe combined immunodeficiency (SCID) mice (carrying HL-60 or MV4-11 cells) [2]
Doses: 100, 200 and 300 mg/kg Route of Administration: intraperitoneal (ip) injection; one time/day for 14 Day Experimental Results: The tumor volume of animals injected with HL-60 and MV4-11 was diminished by 52.5±9.2% and 55.3±5.7%. GYY 4137 has been evaluated in a rat model of myocardial ischemia and reperfusion injury. Rats are subjected to ischemia-reperfusion, and GYY 4137 is administered. The extent of myocardial damage, oxidative stress, and apoptosis is assessed. |
| ADME/Pharmacokinetics |
Pharmacokinetic data for GYY 4137 are not reported in the available literature. As a slow-releasing H2S donor, its pharmacokinetics would be determined by the rate of H2S release and the clearance of the compound and its metabolites.
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| Toxicity/Toxicokinetics |
Specific toxicological data for GYY 4137 are not available. As a research compound, its safety profile has not been comprehensively characterized. Toxicity studies would be required to determine its safety margin.
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| References |
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| Additional Infomation |
Morpholine (4-methoxyphenyl) (morpholinyl) dithiophosphonate is an organic molecular entity.
GYY 4137 is a research tool for studying the biological effects of H2S. It is used to investigate the role of H2S in vasodilation, inflammation, and cardioprotection. It is not an approved therapeutic agent. |
| Molecular Formula |
C15H25N2O3PS2
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|---|---|
| Molecular Weight |
376.47
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| Exact Mass |
376.104
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| CAS # |
106740-09-4
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| PubChem CID |
46937261
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| Appearance |
White to off-white solid powder
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| Melting Point |
164-166 ºC
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| LogP |
2.246
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
23
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| Complexity |
324
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
YZMHNNLDUWRZFW-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C11H16NO2PS2.C4H9NO/c1-13-10-2-4-11(5-3-10)15(16,17)12-6-8-14-9-7-12;1-3-6-4-2-5-1/h2-5H,6-9H2,1H3,(H,16,17);5H,1-4H2
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| Chemical Name |
(4-methoxyphenyl)-morpholin-4-yl-sulfanyl-sulfanylidene-λ5-phosphane;morpholine
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| Synonyms |
GYY 4137 morpholine salt GYY-4137GYY4137ZYJ1122 ZYJ-1122
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~265.63 mM)
H2O : ~19.23 mg/mL (~51.08 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.64 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (6.64 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (6.64 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 50 mg/mL (132.81 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.6563 mL | 13.2813 mL | 26.5625 mL | |
| 5 mM | 0.5313 mL | 2.6563 mL | 5.3125 mL | |
| 10 mM | 0.2656 mL | 1.3281 mL | 2.6563 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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