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]. |
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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. |
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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. |
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运输条件 | Room temperature in continental US; may vary elsewhere. |
储存方式 | Powder | -20°C | 3 years | | 4°C | 2 years | In solvent | -80°C | 6 months | | -20°C | 1 month |
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溶解性数据 | In Vitro: DMSO : 250 mg/mL(553.66 mM;Need ultrasonic) 配制储备液 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 |
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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。 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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