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.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- CAS No.: 1253691-50-7
- Formule: C27H43O12P
- Masse moléculaire:590.60
-
Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Activité biologique
-
Chemical Information
- Pureté et documentation
- Références
-
Help & FAQs
Activité biologique
Description
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.
-
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 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
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%.
Chemical Information
-
CAS No. 1253691-50-7
-
Masse moléculaire 590.60
-
Formule C27H43O12P
-
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
-
Livraison
Room temperature in continental US; may vary elsewhere.
-
Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
[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
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
PXS 64 Related Classifications
HY-181431 Related Classifications
Powered by Bioz