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.
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- CAS. Nr.: 1253691-50-7
- Formel: C27H43O12P
- Molecular Weight:590.60
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Chemical Information
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
Biologische Aktivität
Beschreibung
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.
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Cell Line:NHLFs
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Concentration:1 µM, 3 µM, 10 µM
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Incubation Time:24.5 h
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Result:At10 μM, supressed fibronectin expression by 53% and of collagen by 86%.
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Cell Line:fibroblasts
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Concentration:10 µM
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Incubation Time:24 h
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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
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6 mice (male, 6-8 weeks old, weighing 20-25 g, unilateral ureteral obstruction model)[1]
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Dosage:10 μM
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Administration:i.p.; daily; 7 days
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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%.
Chemical Information
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CAS. Nr. 1253691-50-7
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Molecular Weight 590.60
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Formel C27H43O12P
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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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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
[1]. Zhang J, et al. A cationic-independent mannose 6-phosphate receptor inhibitor (PXS64) ameliorates kidney fibrosis by inhibiting activation of transforming growth factor-β1. PLoS One. 2015;10(2):e0116888. Published 2015 Feb 6. [Content Brief]
[2]. Schilter H, et al. The mannose-6-phosphate analogue, PXS64, inhibits fibrosis via TGF-β1 pathway in human lung fibroblasts. Immunol Lett. 2015;165(2):90-101. [Content Brief]
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
PXS 64 Related Classifications
HY-181431 Related Classifications
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