GYY 4137 morpholine salt
目录号 : GC11088
GYY 4137 morpholine salt是一种新型缓释硫化氢（H2S）供体，具有血管扩张、抗高血压、抗炎和抗癌活性。
Cas No.:106740-09-4
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Cell experiment [1]: | |
Cell lines | HepG2、Bel7402、LO2 cells |
Preparation method | HepG2, Bel7402 and LO2 cells were incubated three times at a density of 1×104 cells in 96-well plates with 100 μl of medium per well and incubated with GYY 4137 morpholino salt (0–400μM) for 24, 48, and 72 h. |
Reaction Conditions | 0–400μM; 24, 48, and 72 h |
Applications | GYY 4137 morpholine salt inhibited tumor cell viability time- and dose-dependently, while it showed weak inhibition on normal hepatocellular LO2 cells. |
Animal experiment [1]: | |
Animal models | Female severe combined immunodeficient (SCID) mice |
Preparation method | Female severe combined immunodeficient (SCID) mice were housed in-house and maintained in specific pathogen-free (SPF) isolators at all times. Exponentially growing HL-60 and MV4-11 cells (1×107) were washed twice in phosphate-buffered saline and injected subcutaneously into the loose skin between the shoulder blade and left foreleg of recipient mice. When tumors formed an average size of 100 mm3, animals were treated with GYY 4137 morpholine salt (100, 200, and 300 mg/kg/day, i.p.) or saline (1 ml/kg/day, i.p.) for 14 days. |
Dosage form | 100, 200, and 300 mg/kg/day; i.p. |
Applications | Treatment with GYY 4137 morpholine salt significantly reduced the tumor volume in both animal models, in a dose-dependent manner. |
References: | |
GYY 4137 morpholine salt is a novel slow-release hydrogen sulfide (H2S) donor with vasodilatory, antihypertensive, anti-inflammatory, and anticancer activities[1, 2]. This product is provided in the form of GYY 4137 morpholine salt.
In vitro, GYY 4137 morpholine salt (0–400 μM) was used to treat liver cancer cells (HepG2 and Bel7402 cells) for 24-72 hours. It inhibited cell viability in a time- and dose-dependent manner, caused cell cycle arrest, and induced apoptosis. It also inhibited IL-6-induced STAT3 phosphorylation and hypoxia-induced expression of VEGF and HIF-1α[3]. GYY 4137 morpholine salt (500 μM) treated CBS-deficient cell lines GES1 and HFE145 for 24 hours, significantly reducing the activity of the inflammatory factor NF-κB within the cells[4].
In vivo, GYY 4137 morpholine salt (100, 200, and 300 mg/kg/day; i.p.) was administered to HL-60 and MV4-11 cell xenograft mice for 14 days, resulting in a dose-dependent reduction in tumor volume. At the highest dose, tumor volume was reduced by 52.5±9.2% and 55.3±5.7% in the respective models[5]. GYY 4137 morpholine salt (50 mg/kg; i.p.) significantly improved motor deficits and reduced the loss of tyrosine hydroxylase (TH)-positive neurons in the substantia nigra and the decrease in TH expression in the striatum in a Parkinson's disease mouse model[6]. GYY 4137 morpholine salt (50 mg/kg; i.p.) administered to mice with acute arthritis 18 hours after complete Freund's adjuvant (CFA) significantly reduced knee swelling and decreased synovial myeloperoxidase (MPO) activity[7].
References:
[1] Rose P, Dymock B W, Moore P K. GYY4137, a novel water-soluble, H2S-releasing molecule[J]. Methods in enzymology, 2015, 554: 143-167.
[2] Nin D S, Idres S B, Song Z J, et al. Biological effects of morpholin-4-Ium 4 methoxyphenyl (morpholino) phosphinodithioate and other phosphorothioate-based hydrogen sulfide donors[J]. Antioxidants & redox signaling, 2020, 32(2): 145-158.
[3] Lu S, Gao Y, Huang X, et al. GYY4137, a hydrogen sulfide (H2S) donor, shows potent anti-hepatocellular carcinoma activity through blocking the STAT3 pathway[J]. International journal of oncology, 2014, 44(4): 1259-1267.
[4] Padmanabhan N, Kyon H K, Boot A, et al. Highly recurrent CBS epimutations in gastric cancer CpG island methylator phenotypes and inflammation[J]. Genome biology, December 2021.
[5] Lee Z W, Zhou J, Chen C S, et al. The slow-releasing hydrogen sulfide donor, GYY4137, exhibits novel anti-cancer effects in vitro and in vivo[J]. PloS one, 2011, 6(6): e21077.
[6] Hou X, Yuan Y, Sheng Y, et al. GYY4137, an H2S slow-releasing donor, prevents nitrative stress and α-synuclein nitration in an MPTP mouse model of Parkinson’s disease[J]. Frontiers in Pharmacology, 2017, 8: 741.
[7] Li L, Fox B, Keeble J, et al. The complex effects of the slow‐releasing hydrogen sulfide donor GYY 4137 in a model of acute joint inflammation and in human cartilage cells[J]. Journal of cellular and molecular medicine, 2013, 17(3): 365-376.
GYY 4137 morpholine salt是一种新型缓释硫化氢（H2S）供体，具有血管扩张、抗高血压、抗炎和抗癌活性[1, 2]。本产品以GYY 4137吗啉盐的形式提供。
在体外，GYY 4137 morpholine salt （0–400μM）处理肝癌细胞（HepG2和Bel7402细胞）24-72h，以时间和剂量依赖性的方式抑制了细胞活力，导致细胞周期停滞并诱导凋亡，还抑制了IL-6诱导的STAT3磷酸化以及缺氧诱导的VEGF和HIF-1α的表达[3]。GYY 4137 morpholine salt （500μM）处理GES1和 HFE145 胱硫醚 β-合酶（CBS）缺陷细胞系24h，显著降低了细胞内炎症因子NF-κB的活性[4]。
在体内，GYY 4137 morpholine salt（100, 200, and 300 mg/kg/day; i.p.）治疗HL-60和MV4-11细胞异种移植小鼠14天，剂量依赖性地减少了两种模型中的肿瘤体积，在最高剂量给药下，肿瘤体积分别减少了52.5±9.2%和55.3±5.7%[5]。GYY 4137 morpholine salt（50mg/kg；i.p.）治疗帕金森模型小鼠，显著改善了运动障碍，减轻了黑质中酪氨酸羟化酶（TH）阳性神经元的损失和纹状体中TH表达的减少[6]。GYY 4137 morpholine salt（50 mg/kg；i.p.）在完全弗氏佐剂（CFA）后18小时治疗急性关节炎小鼠，减少了膝关节肿胀，降低了滑液髓过氧化物酶（MPO）活性[7]。
| Cas No. | 106740-09-4 | SDF | |
| 化学名 | morpholin-4-ium (4-methoxyphenyl)(morpholino)phosphinodithioate | ||
| Canonical SMILES | [S-][P@](N1CCOCC1)(C(C=C2)=CC=C2OC)=S.O3CC[NH2+]CC3 | ||
| 分子式 | C11H16NO2PS2.C4H9NO | 分子量 | 376.47 |
| 溶解度 | ≥ 12.85mg/mL in DMSO | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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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 |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。