2. Stem Cell/Wnt TGF-beta/Smad
  3. TGF-beta/Smad
  4. PXS 64

PXS 64 是一种甘露糖-6-磷酸 (M6P) 类似物，为 PXS 25 (HY-181430) 的亲脂性前药。PXS 64 通过抑制潜伏型 TGF-β1 的活化，发挥有效的抗纤维化作用。PXS 64 通过 TGF-β1 通路抑制人肺成纤维细胞中的纤维化。PXS 64 可降低肾细胞中 TGFβ 介导的胶原 IV、纤连蛋白、MCP-1 和磷酸化 smad2 的表达。PXS 64 可减少皮肤瘢痕成纤维细胞中的胶原沉积。PXS 64 可用于慢性肾病、特发性肺纤维化及瘢痕形成的研究。

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PXS 64

PXS 64 Chemical Structure

CAS No. : 1253691-50-7

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PXS 64 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

PXS 64, a mannose-6-phosphate (M6P) analogue. a lipophilic prodrug of PXS 25 (HY-181430). PXS 64 is an effective anti-fibrotic agent by inhibiting the activation of latent TGF-β1. PXS64, inhibits fibrosis via TGF-β1 pathway in human lung fibroblasts. PXS 64 reduces TGFβ-mediated collagen IV, fibronectin, MCP-1, and phospho-smad2 expression in kidney cells. PXS 64 reduces collagen deposition in dermal scar fibroblasts. PXS 64 can be used for the research of chronic kidney disease, idiopathic pulmonary fibrosis, scarring[1][2][3].

体外研究
(In Vitro)

PXS 64 (10 µM；48 h) 可抑制潜伏态 TGF-β1的活化，抑制促纤维化和促炎性标志物的表达，并选择性降低 TGF-β1诱导的 pSmad2 表达，而不影响 pAKT 或 pERK。PXS 64 单独使用对纤连蛋白、IV 型胶原和 MCP-1 的 mRNA 及蛋白表达无影响[1]。
PXS64 (1–10 μM；24.5 h) 在 rhTGF-β1 刺激的 NHLFs 中表现出对纤维化标志物 (纤维连接蛋白和胶原) 的显著抑制作用[2]。
PXS64 (10 µM；24 h) 处理后，成纤维细胞的形态学表现改善，同时纤维化标志物 (胶原蛋白、CTGF、TGF-β3、tenascin C、αSMA 和 THBS1) 水平下降[2]。
PXS64 在 HF19 细胞中表现出非常强的抗纤维化活性 (通过抑制 αSMA、纤连蛋白和胶原蛋白来衡量)[2]。

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

PXS 64 相关抗体:

Western Blot Analysis[2]

Cell Line: NHLFs
Concentration: 1 µM, 3 µM, 10 µM
Incubation Time: 24.5 h
Result: At10 μM, supressed fibronectin expression by 53% and of collagen by 86%.

Cell Viability AssayWestern Blot AnalysisCell Proliferation AssayApoptosis AnalysisCell Cytotoxicity AssayCell Cycle AnalysisRT-PCRCell Autophagy AssayImmunofluorescenceCell Differentiation AssayCell Invasion AssayCell Migration Assay Real Time qPCRELISA Assay[2]

Cell Line: fibroblasts
Concentration: 10 µM
Incubation Time: 24 h
Result: Down-regulated a number of fibrotic associated genes, such as collagen, connective tissue growth factor (CTGF), TGF-β3, tenascin C, αSMA and thrombospondin 1 (THBS1).
Changed from a senescent, growth-arrested state (as expected to be seen in fibroblasts) to a regular fusiform, healthy phenotype.
体内研究
(In Vivo)

PXS 64 (10 μM；腹腔注射；每日一次；连续 7 天) 可改善雄性 C57BL/6 小鼠 (UUO 模型) 的肾纤维化[1]。

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

Animal Model: C57BL/6 mice (male, 6-8 weeks old, weighing 20-25 g, unilateral ureteral obstruction model)[1]
Dosage: 10 μM
Administration: i.p.; daily; 7 days
Result: Reduced the tubulointerstitial fibrosis index from 3.2 to 2.5, decreased fibronectin mRNA from 12-fold to 1.8-fold and collagen IV mRNA from 9.6-fold to 2.1-fold expression, lowered fibronectin protein from 314.6% to 71.9% and collagen content from 0.69 μg/mg to 0.4 μg/mg, reduced MCP-1 mRNA expression, decreased CD45-positive cell accumulation from 6.7%/area to 1.1%/area and F4/80-positive cell infiltration from 11.3%/area to 7.9%/area, suppressed active TGF-β1 levels from 599.4 pg/mL to 55 pg/mL, and reduced phosphorylated Smad2 protein expression by 80%.
分子量

590.60

Formula

C27H43O12P
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

PXS 64 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:

PXS 641253691-50-7PXS64PXS-64TGF-beta/SmadTransforming growth factor betalung fibroblastsphospho-smad2CI-M6PRfibronectinkidney fibrosis micecationic-independent mannose 6-phosphate receptorcollagen IVTGF-β1MCP-1kidney cellsInhibitorinhibitorinhibit

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