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

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.

For research use only. We do not sell to patients.

PXS 64

PXS 64 Chemical Structure

CAS No. : 1253691-50-7

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Description

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].

In Vitro

PXS 64 (10 µM; 48 h) inhibits latent TGF-β1 activation, suppresses pro-fibrotic and pro-inflammatory marker expression, and selectively reduces TGF-β1-induced pSmad2 expression without affecting pAKT or pERK. PXS64 alone has no effect on\nfibronectin, collagen IV and MCP-1mRNA and protein expression[1].
PXS64 (1-10 µM; 24.5 h) demonstrates a significant inhibition of fibrotic markers ( fibronectin and collagen) in rhTGF-β1 stimulated NHLFs[2].
PXS64 (10 µM; 24 h) presents an improved phenotype in terms of their morphological appearance, as well as a decrease in fibrotic markers (collagen, CTGF, TGF-β3, tenascin C, αSMA and THBS1) in fibroblasts[2].
PXS64 exhibits a very potent anti-fibrotic activity (as measured by the inhibition of αSMA, fibronectin and collagen) in HF19 cells[2].

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

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.
In Vivo

PXS 64 (10 μM; i.p.; daily; 7 days) ameliorates kidney fibrosis in male C57BL/6 mice (UUO model)[1].

MedChemExpress (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%.
Molecular Weight

590.60

Formula

C27H43O12P

CAS No.
SMILES

CC(C)(C)C(OCOP(CC[C@H]([C@H]([C@@H]([C@@H]1O)O)O)O[C@@H]1OC2=C(C=C(C=C2)C)C)(OCOC(C(C)(C)C)=O)=O)=O

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Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
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    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.

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Product Name:
PXS 64
Cat. No.:
HY-181431
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