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| 5mg |
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Pyrintegrin, a β1-integrin agonist, is a potent and cell-permeable promoter of the adhesion of individually dissociated hESCs on matrigel- or laminin-, but not gelatin-coated surfaces, substantially reducing trypsinization-induced apoptosis.
| ln Vitro |
In a dose-dependent manner (IC50 of 1.14 μM), pyrintegrin (0-10 μM; 1 hour; hASC) administration suppresses BMP4-mediated phosphorylation of BMP-responsive SMAD1/5 [1]. Pyrintegrin induces human adipose stem/progenitor cells (hASC) to differentiate into lipid adipocytes in vitro by upregulating CCAAT/enhancer binding protein-α (C/EBPα) and peroxisome proliferator-activated receptor (PPARγ). Additionally, the secretion of adiponectin, leptin, glycerol, and total triglycerides increases in differentiated cells. By phosphorylating SMAD1/5 through BMP, pyrintegrin reduces Runx2 and Osx [1]. In cultured cells, pyrintegrin administration reduces injury-induced declines in focal adhesions, F-actin stress fibers, and active β1-integrin levels [2]. Western blot examination
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| ln Vivo |
Pyrintegrin (10 mg/kg; i.p.; once; C57BL/6J mice) treatment protected mice from LPS-induced podocyte foot process effacement and proteinuria. Analysis of mouse glomeruli showed that LPS administration reduced active β1 integrin levels in podocytes, and co-treatment with Pyrintegrin prevented this [2]. ? In rats, Pyrintegrin reduces peak proteinuria caused by puromycin aminonucleoside-induced nephropathy [2]. ? Pyrintegrin induces transplanted adipose stem/progenitor cells (ASCs) and recruits endogenous cells to form postnatal adipose tissue in vivo. In vivo, Pyrintegrin-treated human adipose stem/progenitor cells (ASCs) in 3D bioprinted scaffolds generated ectopically formed adipose tissue expressing human PPARγ when transplanted into the back of athymic mice. Notably, Pyrintegrin-adsorbed collagen gel implanted in the inguinal fat pad promoted adipogenesis formed by host endogenous cells, demonstrating its ability to induce in situ adipogenesis without the need for cell transplantation [1].
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| Cell Assay |
Western blot analysis
Cell Types: Human adipose stem/progenitor cells (hASC)[2] Tested Concentrations: 0 µM, 0.2 µM, 0.5 µM, 1 µM, 2 µM, 5 µM, 10 µM Incubation Duration: 1 hour Experimental Results: BMP4- Inhibition mediates phosphorylation of BMP-responsive SMAD1/5 in a dose-dependent manner. |
| Animal Protocol |
Animal/Disease Models: Female wild-type C57BL/6J mice (10 weeks old) were injected with LPS [2]
Doses: 10 mg/kg Route of Administration: intraperitoneal (ip) injection; Experimental Results: These animals were provided with significant protection against Effects of LPS-induced proteinuria and foot process (FP) effacement. |
| References |
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| Exact Mass |
451.167
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|---|---|
| CAS # |
1228445-38-2
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| Related CAS # |
1228445-38-2;
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| PubChem CID |
46223724
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| Appearance |
Off-white to light yellow solid powder
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| Density |
1.4±0.1 g/cm3
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| Boiling Point |
729.3±70.0 °C at 760 mmHg
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| Flash Point |
394.9±35.7 °C
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| Vapour Pressure |
0.0±2.5 mmHg at 25°C
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| Index of Refraction |
1.679
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| LogP |
3.26
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
32
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| Complexity |
720
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| Defined Atom Stereocenter Count |
0
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| SMILES |
S(C1C=CC(=CC=1)NC1=NC=CC(=N1)N1C2C=CC(=CC=2CCC1)O)(NCC1CC1)(=O)=O
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| InChi Key |
QRJTZIJWDLJKQO-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C23H25N5O3S/c29-19-7-10-21-17(14-19)2-1-13-28(21)22-11-12-24-23(27-22)26-18-5-8-20(9-6-18)32(30,31)25-15-16-3-4-16/h5-12,14,16,25,29H,1-4,13,15H2,(H,24,26,27)
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| Chemical Name |
N-Cyclopropylmethyl-4-[4-(6-hydroxy-3,4-dihydro-2H-quinolin-1-yl)-pyrimidin-2-ylamino]-benzenesulfonamide
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| Synonyms |
Pyrintegrin PTN
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~250 mg/mL (~553.66 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.61 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (4.61 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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