GYY4137|cas:106740-09-4|西域试剂

GYY4137,98.0%

产品编号：Bellancom-107632| CAS NO：106740-09-4| 分子式：C₁₅H₂₅N₂O₃PS₂| 分子量：376.47

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货号	包装	价格	库存与货期	购买量	操作
Bellancom-107632		￥1160.00	杭州北京（现货）

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GYY4137

产品介绍

GY4137 是一种缓释 H2S 供体，具有血管扩张和抗高血压活性。GY4137 还具有抗炎和抗癌活性。

生物活性

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

体外研究

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.

西域 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 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^[4].
GYY4137 prevents nitrative stress and α-synuclein nitration in an MPTP mouse model of parkinson’s disease^[5].

西域 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.

体内研究

西域 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.

体内研究

西域 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.

性状

Solid

溶解性数据

In Vitro:

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

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

配制储备液

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

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, 6 months; -20°C, 1 month (stored under nitrogen)。-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。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 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.

请依序添加每种溶剂： PBS
Solubility: 50 mg/mL (132.81 mM); Clear solution; Need ultrasonic
2.

请依序添加每种溶剂： 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 ddH₂O 中，得到澄清透明的生理盐水溶液
3.

请依序添加每种溶剂： 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.

请依序添加每种溶剂： 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。