GYY 4137 morpholine salt|106740-09-4|-陌孚医药/Medlife

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GYY 4137 morpholine salt

目录号: PC15237 纯度: ≥98%

CAS No. :106740-09-4

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中文名称	GYY 4137 morpholine salt
中文别名	(4-甲氧基苯基)吗啉基-二硫代膦酸与吗啉的化合物
英文名称	GYY 4137 morpholine salt
英文别名	GYY 4137;GYY 4137 MORPHOLINE SALT;(4-Methoxyphenyl)morpholino-phosphinodithioic acid compound with morpholine;GYY4137;Morpholine (4-methoxyphenyl)(morpholino)phosphinodithioate;GYY4137 morpholine salt;C11H16NO2PS2.C4H9NO;BCP23715;P-(4-Methoxyphenyl)-P-4-morpholinylphosphinodithioic acid morpholine salt;(4-methoxyphenyl)-morpholin-4-yl-sulfanyl-sulfanylidene-lambda5-phosphane;morpholine;UDZ9ARY4YG;Phosphinodithioic acid, (p-methoxyphenyl)morpholino-, compd. with morpholine;(4-met
Cas No.	106740-09-4
分子式	C₁₅H₂₅N₂O₃PS₂
分子量	376.47
包装储存	-20°C, stored under nitrogen *In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

生物活性

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

性状

Solid

体外研究(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.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

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(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 Freunds 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.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

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.

运输条件

Room temperature or refrigerated transportation.

储存方式

-20°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

参考文献

[1]. Li L, et al. Characterization of a novel, water-soluble hydrogen sulfide-releasing molecule (GYY4137): new insights into the biology of hydrogen sulfide. Circulation. 2008;117(18):2351-2360. [Information]

[2]. Lee ZW, et al. The slow-releasing hydrogen sulfide donor, GYY4137, exhibits novel anti-cancer effects 体外研究 and in vivo. PLoS One. 2011;6(6):e21077. [Information]

[3]. Li L, et al. The complex effects of the slow-releasing hydrogen sulfide donor GYY4137 in a model of acute joint inflammation and in human cartilage cells. J Cell Mol Med. 2013;17(3):365-376. [Information]

[4]. Lu S, Gao Y, et al. GYY4137, a hydrogen sulfide (H?S) donor, shows potent anti-hepatocellular carcinoma activity through blocking the STAT3 pathway. Int J Oncol. 2014;44(4):1259-1267. [Information]

[5]. Hou X, et al. GYY4137, an H2S Slow-Releasing Donor, Prevents Nitrative Stress and α-Synuclein Nitration in an MPTP Mouse Model of Parkinsons Disease. Front Pharmacol. 2017;8:741. Published 2017 Oct 30. [Information]

溶解度数据

体外研究:

DMSO : 100 mg/mL (265.63 mM; Need ultrasonic)

H₂O : 19.23 mg/mL (51.08 mM; Need ultrasonic)

配制储备溶液

浓度溶剂体积质量	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

产品不同，其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液；配成溶液后，建议分装保存，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, 6 months; -20°C, 1 month (stored under nitrogen)。-80°C 储存时，建议在 6 个月内使用，-20°C 储存时，建议在 1 个月内使用。

体内研究:

建议根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都建议先按照 体外研究 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

建议依照次序添加每种溶剂： PBS
Solubility: 50 mg/mL (132.81 mM); Clear solution; Need ultrasonic
2.

建议依照次序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.5 mg/mL (6.64 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (6.64 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH?O 中，得到澄清透明的生理盐水溶液
3.

建议依照次序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.5 mg/mL (6.64 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (6.64 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
4.

建议依照次序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.5 mg/mL (6.64 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (6.64 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

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产品使用指南

Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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