2. Apoptosis Metabolic Enzyme/Protease
  3. Glutathione Peroxidase
  4. MPO-IN-10

MPO-IN-10 是一种口服有效、选择性且不可逆的髓过氧化物酶 (MPO) 抑制剂，对人 MPO 的 IC50 为 0.080 μM。MPO-IN-10 对细胞外 MPO 的选择性高于细胞内 (中性粒细胞) 的 MPO。MPO-IN-10 可用于血管疾病等炎症相关疾病的研究。

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MPO-IN-10

MPO-IN-10 Chemical Structure

CAS No. : 2922402-01-3

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MPO-IN-10 相关抗体

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

MPO-IN-10 is an orally active, selective, and irreversible inhibitor of myeloperoxidase (MPO), with an IC50 of 0.080 μM against human MPO. MPO-IN-10 exhibits higher selectivity for extracellular MPO over intracellular (neutrophil) MPO. MPO-IN-10 can be used in the study of inflammatory diseases such as vascular disorders[1].

体外研究
(In Vitro)

MPO-IN-10 (Compound IN-4) 可抑制免疫复合物刺激人原代中性粒细胞产生中性粒细胞胞外陷阱 (NETosis)，其 IC50 为 0.147 μM[1]。

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

MPO-IN-10 相关抗体:
药代动力学
(Parmacokinetics)
Species Dose Route Indicator value
Mice[1] 1 mg/kg i.v. CLplasma 69 mL/min/kg
Mice[1] 1 mg/kg i.v. Vdss 10 L/kg
Mice[1] 1 mg/kg i.v. T1/2 1.1 h
Mice[1] 1 mg/kg i.v. AUClast 641 nM·h
Mice[1] 10 mg/kg p.o. Cmax 101 nM
Mice[1] 10 mg/kg p.o. AUClast 338 nM·h
Mice[1] 10 mg/kg p.o. Tmax 1.3 h
Mice[1] 10 mg/kg p.o. Bioavailability 54 %
Rat[1] 1 mg/kg i.v. CLplasma 29 mL/min/kg
Rat[1] 1 mg/kg i.v. Vdss 8 L/kg
Rat[1] 1 mg/kg i.v. T1/2 2.5 h
Rat[1] 1 mg/kg i.v. AUClast 1574 nM·h
Rat[1] 3 mg/kg p.o. Cmax 183 nM
Rat[1] 3 mg/kg p.o. AUClast 1672 nM·h
Rat[1] 3 mg/kg p.o. Tmax 2.5 h
Rat[1] 3 mg/kg p.o. Bioavailability ~100 %
Dog[1] 0.3 mg/kg i.v. CLplasma 9 mL/min/kg
Dog[1] 0.3 mg/kg i.v. Vdss 7.3 L/kg
Dog[1] 0.3 mg/kg i.v. T1/2 8.6 h
Dog[1] 0.3 mg/kg i.v. AUClast 4000 nM·h
Dog[1] 3 mg/kg p.o. Cmax 361 nM
Dog[1] 3 mg/kg p.o. AUClast 4893 nM·h
Dog[1] 3 mg/kg p.o. Tmax 2 h
Dog[1] 3 mg/kg p.o. Bioavailability ~100 %
体内研究
(In Vivo)

MPO-IN-10 (30-150 mg/kg；灌胃；单次给药) 在小鼠腹膜炎模型中呈剂量依赖性抑制血浆 MPO 活性，其中 150 mg/kg 剂量可实现近乎完全的抑制[1]。
MPO-IN-10 (10-100 mg/kg；灌胃；单次给药) 可在西式饮食急性饲喂的小鼠模型中呈剂量依赖性抑制血浆 MPO 活性[1]。
MPO-IN-10 (约 30-250 mg/kg；饲料给药；10 天) 可西式饮食亚慢性喂养的小鼠中呈剂量依赖性抑制血浆 MPO 活性，其 IC50 约为 0.5 μM[1]。

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

Animal Model: C57BL/6j (male, 8 weeks old) treated thioglycolate broth[1]
Dosage: 30, 150 mg/kg
Administration: p.o.; single dose
Result: Reduced plasma MPO activity by 69% at 30 mg/kg AND reduced plasma MPO activity by ~100% at 150 mg/kg at 5 hours post-dose.
分子量

359.46

Formula

C23H25N3O
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

MPO-IN-10 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:

MPO-IN-102922402-01-3Glutathione Peroxidaseinflammatory conditionsratsdogsneutrophilsmiceneutrophil extracellular trap formatioInhibitorinhibitorinhibit

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