Pyrintegrin_product_DataBase

Bioactivity

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].

Target

β1-integrin

Invitro

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:

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:

Name

Pyrintegrin

CAS

1228445-38-2

Formula

C23H25N5O3S

Molar Mass

451.54

Appearance

Solid

Transport

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Reference

[1]. Shah BS, et al. Pyrintegrin Induces Soft Tissue Formation by Transplanted or Endogenous Cells. Sci Rep. 2017 Jan 27;7:36402. [2]. Lee HW, et al. A Podocyte-Based Automated Screening Assay Identifies Protective Small Molecules. J Am Soc Nephrol. 2015 Nov;26(11):2741-52. [3]. Xu Y, et al. Revealing a core signaling regulatory mechanism for pluripotent stem cell survival and self-renewal by small molecules. Proc Natl Acad Sci U S A. 2010 May 4;107(18):8129-34.

PeptideDB

Pyrintegrin

CAS: 1228445-38-2 F: C23H25N5O3S W: 451.54