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Pyrintegrin 

Cat. No.: HY-13306
Handling Instructions

Pyrintegrin is an β1-integrin agonist and a 2,4-disubstituted pyrimidine that promotes embryonic stem cells survival. Pyrintegrin enhances cell-extracellular matrix (ECM) adhesion-mediated integrin signaling. Pyrintegrin can be used as a podocyte-protective agent and has robustly adipogenic.

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

Pyrintegrin Chemical Structure

Pyrintegrin Chemical Structure

CAS No. : 1228445-38-2

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Description

Pyrintegrin is an β1-integrin agonist and a 2,4-disubstituted pyrimidine that promotes embryonic stem cells survival. Pyrintegrin enhances cell-extracellular matrix (ECM) adhesion-mediated integrin signaling. Pyrintegrin can be used as a podocyte-protective agent and has robustly adipogenic[1][2][3].

IC50 & Target

β1-integrin[2]

In Vitro

Pyrintegrin (0-10 µM; 1 hour; hASCs) treatment inhibits BMP4-mediated phosphorylation of BMP responsive SMAD1/5 in a dose-dependent manner (IC50 of 1.14 μM)[1].
In vitro, Pyrintegrin stimulats human adipose stem/progenitor cells (hASCs) to differentiate into lipid-laden adipocytes by upregulating peroxisome proliferator-activated receptor (PPARγ) and CCAAT/enhancer-binding protein-α (C/EBPα), with differentiated cells increasingly secreting adiponectin, leptin, glycerol and total triglycerides. Pyrintegrin attenuates Runx2 and Osx via BMP-mediated SMAD1/5 phosphorylation[1].
Treatment with Pyrintegrin prevents damage-induced decreases in F-actin stress fibers, focal adhesions, and active β1-integrin levels in cultured cells[2].

Western Blot Analysis

Cell Line: Human adipose stem/progenitor cells (hASCs)[2]
Concentration: 0 µM, 0.2 µM, 0.5 µM, 1 µM, 2 µM, 5 µM, 10 µM
Incubation Time: 1 hour
Result: Inhibited BMP4-mediated phosphorylation of BMP responsive SMAD1/5 in a dose-dependent manner.
In Vivo

Pyrintegrin (10 mg/kg; intraperitoneal injection; once; C57BL/6J mice) treatment protects mice from LPS-induced podocyte foot process effacement and proteinuria. Analysis of the murine glomeruli shows that LPS administration reduces the levels of active β1 integrin in the podocytes, which is prevented by cotreatment with Pyrintegrin[2].
In rats, Pyrintegrin reduces peak proteinuria caused by puromycin aminonucleoside-induced nephropathy[2].
Pyrintegrin induces postnatal adipose tissue formation in vivo of transplanted adipose stem/progenitor cells (ASCs) and recruited endogenous cells. In vivo, Pyrintegrin-treated human adipose stem/progenitor cells (ASCs) in 3D-bioprinted scaffolds, when transplanted in the dorsum of athymic mice, yielded ectopically formed adipose tissue that expressed human PPARγ. Remarkably, Pyrintegrin-adsorbed collagen gel implanted in the inguinal fat pad promoted adipogenesis formed by host endogenous cells, suggesting its ability to induce in situ adipogenesis without the need for cell transplantation[1].

Animal Model: Female wild type C57BL/6J mice (10-week-old) injected with LPS[2]
Dosage: 10 mg/kg
Administration: Intraperitoneal injection; once
Result: Provided a significant protection for these animals from LPS-induced proteinuria and foot processe (FP) effacement.
Molecular Weight

451.54

Formula

C₂₃H₂₅N₅O₃S

CAS No.

1228445-38-2

SMILES

O=S(C1=CC=C(NC2=NC=CC(N3CCCC4=C3C=CC(O)=C4)=N2)C=C1)(NCC5CC5)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Solvent & Solubility
In Vitro: 

DMSO : 250 mg/mL (553.66 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2146 mL 11.0732 mL 22.1464 mL
5 mM 0.4429 mL 2.2146 mL 4.4293 mL
10 mM 0.2215 mL 1.1073 mL 2.2146 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (4.61 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (4.61 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

PyrintegrinIntegrinAdipogenicembryonicstemcellspodocyte-protectiveβ1-integrinnephropathyproteinuriaPPARγC/EBPαECMInhibitorinhibitorinhibit

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Pyrintegrin
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HY-13306
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