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Pyrintegrin
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Pyrintegrin图片
CAS NO:1228445-38-2

Pyrintegrin 是一种 β1 整合素 (β1-integrin) 激动剂,也是一种 2,4-二取代的嘧啶,可促进胚胎干细胞存活。Pyrintegrin 能增强细胞-细胞外基质 (ECM) 粘附介导的整联蛋白信号传导。Pyrintegrin 可用作足细胞保护剂,并具有强大的成脂作用。
生物活性

Pyrintegrin is anβ1-integrinagonist and a 2,4-disubstituted pyrimidine that promotes embryonic stem cells survival. Pyrintegrin enhances cell-extracellular matrix (ECM) adhesion-mediatedintegrinsignaling. Pyrintegrin can be used as a podocyte-protective agent and has robustly adipogenic[1][2][3].

IC50& Target

β1-integrin[2]

体外研究
(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.
体内研究
(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.
分子量

451.54

性状

Solid

Formula

C23H25N5O3S

CAS 号

1228445-38-2

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder-20°C3 years
4°C2 years
In solvent-80°C6 months
-20°C1 month
溶解性数据
In Vitro: 

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

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM2.2146 mL11.0732 mL22.1464 mL
5 mM0.4429 mL2.2146 mL4.4293 mL
10 mM0.2215 mL1.1073 mL2.2146 mL
*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80℃, 6 months; -20℃, 1 month。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 10% DMSO    40%PEG300   5%Tween-80   45% saline

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

    此方案可获得 ≥ 2.08 mg/mL (4.61 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH2O 中,得到澄清透明的生理盐水溶液
  • 2.

    请依序添加每种溶剂: 10% DMSO    90%corn oil

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

    此方案可获得 ≥ 2.08 mg/mL (4.61 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*以上所有助溶剂都可在本网站选购。
 
 
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