2. Cell Cycle/DNA Damage Vitamin D Related/Nuclear Receptor Metabolic Enzyme/Protease NF-κB Immunology/Inflammation
  3. PPAR Reactive Oxygen Species (ROS) Keap1-Nrf2
  4. PIISVYWK

PIISVYWK 是一种具有口服活性的PPARγ抑制剂、血红素加氧酶-1激活剂和Nrf2激活剂。PIISVYWK 通过 HO-1/Nrf2 通路介导活性，可改善氧化应激、减轻炎症并介导抗肥胖活性。PIISVYWK 可用于肥胖相关研究。

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PIISVYWK

PIISVYWK Chemical Structure

CAS No. : 2016043-80-2

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PIISVYWK 相关抗体

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PPARα PPARβ/δ PPARγ PPAR PPARδ

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PIISVYWK is an orally active PPARγ Inhibitor, heme oxygenase-1 Activator, and Nrf2 Activator. PIISVYWK mediates activity via the HO-1/Nrf2 pathway, ameliorates oxidative stress, reduces inflammation, and mediates anti-obesity activity. PIISVYWK can be used for the research of obesity[1].

体外研究
(In Vitro)

PIISVYWK (10-100 μM；作用 48 h) 对 BMMSCs 无细胞毒性[1]。
PIISVYWK (10-100 μM；作用 7 天) 通过抑制成脂转录因子与脂肪生成酶、增强脂解作用，抑制BMMSCs的脂肪细胞分化；在 100 μM 浓度下，其对脂质蓄积的抑制率最高可达 40.97%[1]。
PIISVYWK (10-100 μM；Nrf2 处理 2 天，HO-1 处理 3 天) 可激活 BMMSCs 中的 HO-1/Nrf2 信号通路，在 100 μM 浓度下上调 HO-1 的细胞质表达水平与 Nrf2 的细胞核表达水平[1]。
PIISVYWK (10-100 μM；作用 7 天) 可通过减少 ROS 生成、提高抗氧化酶活性，降低骨髓间充质干细胞 (BMMSCs) 成脂分化过程中的氧化应激，且在 100 μM 浓度下效果显著[1]。
PIISVYWK (10-100 μM；作用 7 天) 通过抑制促炎细胞因子的产生并调控MAPK通路，减轻BMMSCs的炎症反应，在 100 μM 浓度下作用效果显著[1]。
PIISVYWK (100 μM；处理 7 天，预先用 5 μM ZnPP 处理 1 小时) 可通过 HO-1 介导在骨髓间充质干细胞 (BMMSCs) 中发挥抗成脂作用，因为预先用 ZnPP 处理可逆转其对脂肪细胞分化、转录因子表达和脂解的抑制作用[1]。
PIISVYWK (100 μM；处理 7 天，预处理时用 5 μM ZnPP 孵育 1 小时) 在骨髓间充质干细胞 (BMMSCs) 中发挥氧化应激抑制及抗炎作用，该作用由 HO-1 介导，因为 ZnPP 预处理可逆转上述效应[1]。

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

PIISVYWK 相关抗体:

Cell Differentiation Assay[1]

Cell Line: bone marrow-derived mesenchymal stem cells (BMMSCs)
Concentration: 10-100 μM
Incubation Time: 7 days
Result: Inhibited lipid accumulation in BMMSCs in a dose-dependent manner, with up to 40.97% inhibition at 100 μM; suppressed the expression of adipogenic transcription factors PPARγ, SREBP-1, and C/EBPα, alongside adipocyte protein 2 (aP2); increased free glycerol levels in the culture medium; inhibited lipogenic enzymes FAS and LPL; upregulated lipolysis-related p-HSL.

Western Blot Analysis[1]

Cell Line: bone marrow-derived mesenchymal stem cells (BMMSCs)
Concentration: 10-100 μM
Incubation Time: 2 days (Nrf2); 3 days (HO-1)
Result: Elevated HO-1 expression in the cytoplasm of BMMSCs, with significance at 100 μM (P < 0.05); increased Nrf2 expression in the cell nucleus at high concentrations (P < 0.05); induced Nrf2 nuclear translocation as observed via immunostaining.

ELISA Assay[1]

Cell Line: bone marrow-derived mesenchymal stem cells (BMMSCs)
Concentration: 10-100 μM
Incubation Time: 7 days
Result: Significantly reduced the production of pro-inflammatory cytokines (IL-6, IL-1β, TNF-α) in BMMSCs compared to the control group, with significant effects at higher concentrations (P < 0.01 for 100 μM; P < 0.05 for lower concentrations); modulated the MAPK pathway, with changes in p-ERK, p-P38, and p-JNK expression.
体内研究
(In Vivo)

PIISVYWK (1-10 mg/kg；灌胃；每日给药；连续 15 周) 可显著减少高脂饮食 (HFD) 诱导肥胖小鼠的体重增加、脂肪堆积与促炎细胞因子水平，同时在 10 mg/kg 剂量下激活抗肥胖及抗氧化通路，1 mg/kg 剂量下仅产生中等程度的效果[1]。

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

Animal Model: C57BL/6 (male, 3 weeks old at acclimation start, 6 weeks old at study initiation, HFD-induced obesity model)[1]
Dosage: 1 mg/kg; 10 mg/kg
Administration: p.o.; daily; 15 weeks
Result: Reduced weight gain to 17.29 g, decreased fat percentage to 45.26%, reduced adipose tissue weight, suppressed adipogenic transcription factors (PPARγ, SREBP-1, C/EBPα) and lipogenic enzymes (LPL, FAS, aP2) in subcutaneous adipose tissue, increased p-HSL and p-AMPK expression in subcutaneous adipose tissue, reduced fasting blood glucose to 146.00 mg/dL, reduced total cholesterol (4.98 mmol/L), LDL (1.00 mmol/L), and triglycerides (1.43 mmol/L), increased HDL (1.49 mmol/L) and free glycerol levels, reduced serum pro-inflammatory cytokines (IL-6: 34.33 pg/mL, IL-1β: 17.00 pg/mL, TNFα: 22.67 pg/mL), increased antioxidant enzyme activities (CAT: 35.4 U/mL, SOD: 165.2 U/mL, GPx: 82.7 U/mL), and activated HO-1 and Nrf2 in subcutaneous adipose tissue at 10 mg/kg; moderately reduced weight gain, fasting blood glucose, LDL, pro-inflammatory cytokines, and increased antioxidant enzyme activities at 1 mg/kg.
分子量

1005.21

Formula

C51H76N10O11
CAS 号
Sequence

Pro-Ile-Ile-Ser-Val-Tyr-Trp-Lys
Sequence Shortening

PIISVYWK
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

PIISVYWK 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:

PIISVYWK2016043-80-2PPARReactive Oxygen Species (ROS)Keap1-Nrf2Peroxisome proliferator-activated receptorsnuclear factor erythroid 2-related factor 2CCAAT/enhancer-binding protein alphaheme oxygenase-1bone marrow-derived mesenchymal stem cellAMP-activated protein kinaseperoxisome proliferator-activated receptor gammamitogen-activated protein kinase pathwayhormone-sensitive lipasesterol regulatory element-binding protein 1high-fat diet-induced obese miceInhibitorinhibitorinhibit

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