2. Metabolic Enzyme/Protease
  3. MetAP
  4. PPI-2458

PPI-2458 是一种口服有效的、选择性和不可逆的蛋氨酸氨基肽酶-2 (MetAP-2) 抑制剂。PPI-2458 可用于关节炎和淋巴瘤研究。

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PPI-2458 Chemical Structure

PPI-2458 Chemical Structure

CAS No. : 431077-35-9

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥8172
In-stock
1 mg ￥3500
In-stock
5 mg 现货 询价
10 mg 现货 询价
25 mg 现货 询价
50 mg   询价  
100 mg   询价  

* Please select Quantity before adding items.

Customer Review

PPI-2458 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

PPI-2458 is a potent, orally active, selective and irreversible inhibitor of methionine aminopeptidase-2 (MetAP-2). PPI-2458 can be used for arthritis and lymphoma research[1][2].

体外研究
(In Vitro)

PPI-2458 可有效抑制 HUVEC 增殖，GI50 为0.2 nM，在1 nM 时最大抑制率大于 95%[1]。
PPI-2458 (0-100 nM, 6天)抑制 SU-DHL-16 细胞的增殖和MetAP-2[2]。

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

PPI-2458 相关抗体:

Cell Proliferation Assay[2]

Cell Line: SU-DHL-16 cells
Concentration: 0, 0.01, 0.1, 1, 10, and 100 nM
Incubation Time: 6 days
Result: Inhibited SU-DHL-16 proliferation in a dose-dependent fashion with maximum inhibition of 60% achieved at the highest concentration (100 nmol/L) and GI50 at 1.9 nmol/L.
体内研究
(In Vivo)

PPI-2458 (0-50 mg/kg，口服，隔日一次)逆转 PG-PS (25 mg/kg, i.p) 诱导的关节炎模型中的关节肿胀和炎症[1]。
PPI-2458 (0-3 mg/kg，鼻胃插管，隔日一次)可导致实验初代食蟹猴生发中心生发中心淋巴细胞减少[2]。
PPI-2458 (0-100 mg/kg，口服，隔日一次)以剂量依赖的方式显著抑制肿瘤生长在SR肿瘤异种移植的严重联合免疫缺陷小鼠中[2]。

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

Animal Model: Female Lewis rats (101–121 g, PG-PS (25 mg/kg, i.p.)-induced arthritis model)[1]
Dosage: 0.25, 1, 5, and 50 mg/kg
Administration: Orally (po), started at day 15 after the chronic destructive phase of the disease was established and terminated on day 31
Result: Significantly and dose-dependently attenuated the chronic inflammatory response. Markedly attenuated paw swelling in a dose-dependent manner with maximal protection at an orally administered dose of 50 mg/kg at day 31.
Animal Model: Forty-two experimentally naive cynomolgus monkeys[2]
Dosage: 0.1 mg/kg (three males and three females), 0.3 mg/kg (three males and three females), 1.0 mg/kg (five males and five females), and 3.0 mg/kg (five males and five females)
Administration: Nasogastric intubation every other day (QOD) for 13 days (total of seven treatments)
Result: Exhibited a marked decrease in germinal center lymphocytes.
Animal Model: 60 female Fox Chase severe combined immunodeficient mice (SR lymphoma cells were injected s.c. above the right hind leg)[2]
Dosage: 10, 30, or 100 mg/kg
Administration: oral gavage, QOD
Result: Significantly suppressed tumor growth in a dose-dependent manner. PPI-2458 administered at 100 mg/kg produced the greatest degree of tumor growth inhibition, which was 57% (P < 0.001) at the end of the study.
Clinical Trial
分子量

424.53

Formula

C22H36N2O6
CAS 号
性状

固体

颜色

White to off-white

运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
细胞实验： 

DMSO 中的溶解度 : ≥ 100 mg/mL (235.55 mM; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

* "≥" means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.3555 mL 11.7777 mL 23.5555 mL
5 mM 0.4711 mL 2.3555 mL 4.7111 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。-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

只
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
参考文献

PPI-2458 相关分类

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。-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 2.3555 mL 11.7777 mL 23.5555 mL 58.8887 mL
5 mM 0.4711 mL 2.3555 mL 4.7111 mL 11.7777 mL
10 mM 0.2356 mL 1.1778 mL 2.3555 mL 5.8889 mL
15 mM 0.1570 mL 0.7852 mL 1.5704 mL 3.9259 mL
20 mM 0.1178 mL 0.5889 mL 1.1778 mL 2.9444 mL
25 mM 0.0942 mL 0.4711 mL 0.9422 mL 2.3555 mL
30 mM 0.0785 mL 0.3926 mL 0.7852 mL 1.9630 mL
40 mM 0.0589 mL 0.2944 mL 0.5889 mL 1.4722 mL
50 mM 0.0471 mL 0.2356 mL 0.4711 mL 1.1778 mL
60 mM 0.0393 mL 0.1963 mL 0.3926 mL 0.9815 mL
80 mM 0.0294 mL 0.1472 mL 0.2944 mL 0.7361 mL
100 mM 0.0236 mL 0.1178 mL 0.2356 mL 0.5889 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.

Keywords:

PPI-2458431077-35-9PPI2458PPI 2458MetAPMethionine AminopeptidaseHUVECarthritisinflammatoryorally activeNHL tumorSU-DHL-16SR lymphoma cellsInhibitorinhibitorinhibit

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