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GYY4137 

目录号: HY-107632 纯度: >95.0%
产品使用指南

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。

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GYY4137 Chemical Structure

GYY4137 Chemical Structure

CAS No. : 106740-09-4

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Description

GYY4137 is a slow releasing H2S donor with vasodilator and antihypertensive activity. GYY4137 also exhibits anti-inflammatory and anticancer activity[1][2][3].

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)[2].
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[3].

Cell Viability Assay[2]

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.
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[2].
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[3].
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].

Animal Model: Female, severe combined immunodeficiency (SCID) mice (bearing HL-60 or MV4-11 cells) [2]
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.
Molecular Weight

376.47

Formula

C₁₅H₂₅N₂O₃PS₂

CAS No.

106740-09-4

SMILES

SP(N1CCOCC1)(C2=CC=C(OC)C=C2)=S.N3CCOCC3

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

-20°C, stored under nitrogen

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

Solvent & Solubility
In Vitro: 

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

Preparing
Stock Solutions
Concentration Solvent Mass 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: 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
  • 2.

    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
  • 3.

    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。

*以上所有助溶剂都可在 MCE 网站选购。
References

Purity: >95.0%

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The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

Keywords:

GYY4137GYY 4137GYY-4137OthersH2Sdonorvasodilatorantihypertensiveanti-inflammatoryCFAanti-hepatocellularcarcinomaparkinson’sdiseaseInhibitorinhibitorinhibit

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产品名称:
GYY4137
目录号:
HY-107632
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