1. Anti-infection Metabolic Enzyme/Protease
  2. Bacterial HIF/HIF Prolyl-Hydroxylase Antibiotic
  3. Gramicidin A

Gramicidin A 是 Gramicidin 的一种肽成分,是一种抗生素(antibiotic)的混合物,最初从 B. brevis 中分离得到。 Gramicidin A 是一种高度疏水的通道形成离子载体,在人工膜中形成一价阳离子可渗透的通道。Gramicidin A 诱导缺氧诱导因子 1α (HIF-1α) 的降解。

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Custom Peptide Synthesis

Gramicidin A Chemical Structure

Gramicidin A Chemical Structure

CAS No. : 11029-61-1

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5 mg ¥2700
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Other Forms of Gramicidin A:

MCE 顾客使用本产品发表的 1 篇科研文献

查看 HIF/HIF Prolyl-Hydroxylase 亚型特异性产品:

查看 Antibiotic 亚型特异性产品:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Gramicidin A is a peptide component of gramicidin, an antibiotic mixture originally isolated from B. brevis. Gramicidin A is a highly hydrophobic channel-forming ionophore that forms channels in model membranes that are permeable to monovalent cations. Gramicidin A induces degradation of hypoxia inducible factor 1 α (HIF-1α)[1][2].

IC50 & Target

HIF-1α[2]

体外研究
(In Vitro)

Gramicidin A displays potent broad-spectrum antibiotic activity against Gram-positive strains, even multidrug-resistant strains[1].
Gramicidin A has the disadvantage of high hemolytic activity[1].
Gramicidin A (0.1 nM-10 μM, 72 h) reduces the viability of RCC cell lines and affects cell viability comparable to Monensin (HY-N4302)[2].
Gramicidin A cellular sensitivity is significantly altered by neither VHL nor HIF-1α expression[2].
Gramicidin A (1 and 10 μM, 48 or 72 h) induces nonapoptotic cell death in RCC cells[2].
Gramicidin A (0-10 μM, 24 h) depletes cellular energy and induces metabolic dysfunction in RCC cells[2].
Gramicidin A (0-1 μM, 24-72 h) reduces HIF-1α and HIF-2α protein expression, reduces HIF transcriptional activity and target gene expression (24 h)[3]

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

Cell Viability Assay[2]

Cell Line: A498, 786-O, Caki-1, SN12C, ACHN, UMRC6, UMRC6+VHL, HEK293T+pcDNA3, HEK293T+HA-HIF-1α, HEK293T+HA-HIF-1α-mut
Concentration: 0.1 nM-10 μM
Incubation Time: 72 h
Result: Reduced the viability with IC50s of 0.420, 0.430, 0.228, 0.104, 0.783, 0.253, 0.425, 0.057, 0.058 and 0.067 μM against A498, 786-O, Caki-1, SN12C, ACHN, UMRC6, UMRC6+VHL, HEK293T+pcDNA3, HEK293T+HA-HIF-1α, HEK293T+HA-HIF-1α-mut cells, respectively.

Western Blot Analysis[2][3]

Cell Line: 786-O, SN12C, Caki-1, ACHN
Concentration: 1 and 10 μM or 0.1, 0.5 and 1.0 μM
Incubation Time: 24, 48 or 72 h
Result: PARP cleavage was not detected. Increased the phosphorylation of AMPKα and its substrate ACC at both 24 and 48 hours. Reduced HIF-1α and HIF-2α protein expression. Hypoxic expression of CA-IX, GLUT-1, and GAPDH were all decreased in a dose-dependent manner.

RT-PCR[3]

Cell Line: SN12C, Caki-1, ACHN
Concentration: 0.1, 0.5 and 1.0 μM
Incubation Time: 24 h
Result: Significantly altered transcript expression for only HIF-2α in SN12C cells.
体内研究
(In Vivo)

Gramicidin A (0.11 mg/kg; intratumoral injection; twice weekly for 14 days) inhibits the growth of RCC tumor xenografts[2].
Gramicidin A (0.22 mg/kg; intratumoral injection; thrice weekly for 26 days) inhibits the growth and angiogenesis of VHL-expressing RCC tumor xenografts[3].

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

Animal Model: Female hairless Nu/J mice, 6- to 8-week old, injected subcutaneously with a suspension of SN12C cells (1.0 × 106) in a 50% growth factor–reduced Matrigel solution[2]
Dosage: 0.11 mg/kg body weight
Administration: Intratumoral injection, twice weekly for 14 days
Result: The average tumor mass was reduced by approximately 40% without significant toxicity.
Animal Model: Female hairless 6- to 8-week-old Nu/J mice, injected subcutaneously with a suspension of Caki-1-td-Tomato cells (1.5 × 106) in a 50% growth factor-reduced Matrigel solution[3].
Dosage: 0.22 mg/kg
Administration: Intratumoral injection, thrice weekly for 26 days
Result: Inhibited tumor growth. HIF-2α and GAPDH protein expression was substantially reduced.
分子量

1882.29

Formula

C99H140N20O17

CAS 号
性状

固体

颜色

White to off-white

Sequence

{For}-Val-Gly-Ala-{D-Leu}-Ala-{D-Val}-Val-{D-Val}-Trp-{D-Leu}-Trp-{D-Leu}-Trp-{D-Leu}-Trp-{NHCH2CH2OH}

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Sealed storage, away from moisture

Powder -80°C 2 years
-20°C 1 year

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据
细胞实验: 

DMSO 中的溶解度 : 100 mg/mL (53.13 mM; 超声加热助溶; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 0.5313 mL 2.6563 mL 5.3127 mL
5 mM 0.1063 mL 0.5313 mL 1.0625 mL
查看完整储备液配制表

* 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 (sealed storage, away from moisture)。-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。

  • 摩尔计算器

  • 稀释计算器

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

质量
=
浓度
×
体积
×
分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料

纯度: 98.1%

参考文献

完整储备液配制表

* 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 (sealed storage, away from moisture)。-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。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 0.5313 mL 2.6563 mL 5.3127 mL 13.2817 mL
5 mM 0.1063 mL 0.5313 mL 1.0625 mL 2.6563 mL
10 mM 0.0531 mL 0.2656 mL 0.5313 mL 1.3282 mL
15 mM 0.0354 mL 0.1771 mL 0.3542 mL 0.8854 mL
20 mM 0.0266 mL 0.1328 mL 0.2656 mL 0.6641 mL
25 mM 0.0213 mL 0.1063 mL 0.2125 mL 0.5313 mL
30 mM 0.0177 mL 0.0885 mL 0.1771 mL 0.4427 mL
40 mM 0.0133 mL 0.0664 mL 0.1328 mL 0.3320 mL
50 mM 0.0106 mL 0.0531 mL 0.1063 mL 0.2656 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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产品名称:
Gramicidin A
目录号:
HY-P2324
需求量: