2. Metabolic Enzyme/Protease Neuronal Signaling
  3. Adenosine Kinase
  4. GP515

GP515 是一种强效且具有选择性的腺苷激酶 (adenosine kinase) 抑制剂，其对人体的 IC50 值为 4 nM。GP515 具有组织保护作用，可在出血性休克后产生持久的肝脏微循环改善作用，并能以剂量和时间依赖的方式诱导常氧大鼠心肌成肌细胞中 VEGF mRNA 和蛋白的表达，在轻度缺氧条件下 VEGF 表达呈叠加性增加，而在重度缺氧条件下则无此作用。GP515 可抑制 DSS 诱导的结肠炎中 IFNγ 的合成和 CD69 的表达。GP515 还表现出剂量依赖性的 TNF-α 生成抑制作用，其 IC50 值为 80 μM，且该抑制作用可被 cAMP 拮抗剂 (Rp)-cAMPS 逆转。GP515 与腺苷或罗利普兰联用可导致 TNF-α 合成的叠加性抑制。 GP515 可用于出血性休克和炎症性肠病的研究。

MCE 的所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

GP515

GP515 Chemical Structure

CAS No. : 144928-48-3

1.  客户无需承担相应的运输费用。

2.  同一机构（单位）同一产品试用装仅限申领一次，同一机构（单位）一年内

     可免费申领三个不同产品的试用装。

3.  试用装只面向终端客户。

规格 是否有货
50 mg   询价  
100 mg   询价  
250 mg   询价  

* Please select Quantity before adding items.

Customer Review

GP515 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

GP515 is a potent and selective adenosine kinase inhibitor with a human IC50 of 4 nM. GP515 exerts tissue protective effects, produces long-lasting hepatic microcirculation effects after hemorrhagic shock, and induces dose- and time-related VEGF mRNA and protein expression in normoxic rat myocardial myoblasts, with additive VEGF increases during mild hypoxia and no effect during severe hypoxia. GP515 suppresses IFNγ synthesis and CD69 expression in DSS-induced colitis. GP515 also shows a dose-dependent suppression of TNF-α production with an IC50 of 80 μM and can be reversed in the presence of the cAMP antagonist (Rp)-cAMPS. Combinations of GP515 with either adenosine or rolipram led to an additive inhibition of TNF-α synthesis. GP515 can be used for the research of hemorrhagic shock[1][2][3][4].

体外研究
(In Vitro)

GP515 可强效且特异性地抑制分离得到的人心肌腺苷激酶，其 IC50 为 4 nM[2]。
GP515 (2-20 μM；18 小时) 在常氧孵育 18 小时后，可使培养的大鼠心肌成肌细胞中 VEGF mRNA 的表达分别上调 1.67 倍和 1.82 倍[2]。
GP515 (0.2-200 μM；18 小时) 在常氧孵育 18 小时后，可诱导培养的大鼠心肌成肌细胞中 VEGF 蛋白表达呈剂量依赖性升高，在最高浓度下升高幅度可达 54%[2]。
GP515 (1 μM；12-24 小时) 在常氧孵育 12 小时后可显著上调培养大鼠心肌成肌细胞中的 VEGF 蛋白表达，且该效应可持续至 24 小时[2]。
GP515 (2 μM；18 小时) 与腺苷脱氨酶共同孵育可完全阻断常氧孵育 18 小时后培养大鼠心肌成肌细胞中 VEGF 蛋白的诱导作用[2]。
GP515 (20 μM；24 小时) 可将人脐静脉内皮细胞的增殖能力提升 98%，并在孵育 24 h 后使[3H]胸苷掺入量增加 82%，但对大鼠心肌成肌细胞的增殖无影响[2]。
GP515 (20 μM；18 小时) 可在常氧条件下使培养的大鼠心肌成肌细胞中 VEGF 蛋白表达量提升 37%；在轻度缺氧 (10% O2) 孵育 18 h 后，该表达量可进一步提升 27%，但在重度缺氧 (1% O2) 条件下无作用[2]。

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

GP515 相关抗体:

ELISA Assay[2]

Cell Line: cultured rat myocardial myoblasts (RMMs)
Concentration: 0.2 μM; 2 μM; 20 μM; 200 μM
Incubation Time: 18 h
Result: Increased VEGF protein levels to 1.99 ng/mg total cell protein (8% increase) at 0.2 μM.
Increased VEGF protein levels to 2.50 ng/mg total cell protein (36% increase) at 2 μM.
Increased VEGF protein levels to 2.56 ng/mg total cell protein (39% increase) at 20 μM.
Increased VEGF protein levels to 2.84 ng/mg total cell protein (54% increase) at 200 μM; control VEGF protein levels were 1.84 ng/mg total cell protein, with all increases statistically significant.

ELISA Assay[2]

Cell Line: cultured rat myocardial myoblasts (RMMs)
Concentration: 1 μM
Incubation Time: 2 h; 6 h; 12 h; 24 h
Result: Did not significantly increase VEGF protein levels after 2 or 6 h of incubation.
Caused a significant 20% increase after 12 h.
Continued to increase levels such that by 24 h, levels were quantitatively similar to those induced by equimolar adenosine.

ELISA Assay[2]

Cell Line: cultured rat myocardial myoblasts (RMMs)
Concentration: 2 μM (co-incubated with 10 U/mL adenosine deaminase)
Incubation Time: 18 h
Result: Co-incubation with adenosine deaminase completely blocked the GP515-induced increase in VEGF protein, reducing levels to 0.75 ng/mg total cell protein, a 60% decrease compared to control levels of 1.84 ng/mg total cell protein.

Cell Proliferation Assay[2]

Cell Line: human umbilical vein endothelial cells (HUVECs), rat myocardial myoblasts (RMMs)
Concentration: 20 μM
Incubation Time: 24 h
Result: Increased HUVEC cell number by 98% (from control 8.5 × 105 cells/well).
Increased [3H]thymidine incorporation by 82% (from control 11.91 × 103 cpm/well), with both changes statistically significant.
Had no effect on RMM proliferation.

ELISA Assay[2]

Cell Line: cultured rat myocardial myoblasts (RMMs)
Concentration: 20 μM
Incubation Time: 18 h (under normoxia, mild hypoxia, severe hypoxia)
Result: Increased VEGF protein levels by 37% (to 2.79 ng/mg total cell protein) compared to normoxic control levels of 2.04 ng/mg total cell protein under normoxia.
Increased VEGF protein levels by an additional 27% (to 4.17 ng/mg total cell protein) compared to mild hypoxia control levels of 3.29 ng/mg total cell protein under mild hypoxia.
Had no effect on VEGF protein levels (5.84 ng/mg total cell protein vs.
severe hypoxia control levels of 6.06 ng/mg total cell protein) under severe hypoxia.
体内研究
(In Vivo)

GP515 (0.25 mg/kg；静脉注射；持续输注 1 小时；失血性低血压发作 90 分钟后开始给药) 在雌性 Sprague-Dawley 大鼠 (200-250 g) 失血性休克后全身给药，可显著改善休克后 2 天的肝脏微循环参数 (肝窦血流量、直径和灌注指数)，且这些参数在第 5 天恢复正常[1]。

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

Animal Model: Sprague-Dawley (female, 200-250 g, pressure-controlled hemorrhagic hypotension induced by blood withdrawal to maintain mean arterial pressure at 40 mmHg for 90 minutes, followed by resuscitation with 60% shed blood and lactate Ringer’s solution)[1]
Dosage: 0.25 mg/kg
Administration: i.v.; continuous infusion over 1 hour; starting 90 minutes after onset of hemorrhagic hypotension
Result: Increased sinusoidal blood flow to 40833 µm3/s, mean sinusoidal diameter to 12.08 µm, and perfusion index to 91.5% at 2 days post-shock, with all values significantly higher than placebo.
Normalized sinusoidal diameters, blood flow, and perfusion index by 5 days post-shock, with no significant difference from placebo-treated rats.
分子量

345.15

Formula

C10H13BrN6O3
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

GP515 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

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

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
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.

Keywords:

GP515144928-48-3GP 515GP-515Adenosine KinaseADKVEGFrat myocardial myoblastshemorrhagic shockhuman umbilical vein endothelial cellhepatic microcirculationadenosine kinaseadenosine deaminaseadenosine transportersadenosine receptorsAMP deaminaseInhibitorinhibitorinhibit

您最近查看的产品:

Your information is safe with us. * Required Fields.

   产品名称：

  

* 需求量：

* 客户姓名：

 

* Email：

* 电话：

 

* 公司或机构名称：

   留言给我们：

Bulk Inquiry

Inquiry Information

产品名称：
GP515
目录号：
HY-182503
需求量：

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

   产品名称：

  

* Lot #：

* 客户姓名：

 

* Email：

   电话：

 

* 部门：

* 公司或机构名称：

 

   留言给我们：

Request for HNMR Report

We have received your request and will respond to you as soon as possible.

嗨！很高兴为您提供帮助！

尊敬的 MCE 客户您好，
请您选择所在区域，我们将转接对应客服为您服务！

热门区域

A

B

C

F

G

H

J

L

N

Q

S

T

X

Y

Z

热 A B C F G H J L N Q S T X Y Z