Synonym
Pyrintegrin; PTN;
IUPAC/Chemical Name
N-Cyclopropylmethyl-4-[4-(6-hydroxy-3,4-dihydro-2H-quinolin-1-yl)-pyrimidin-2-ylamino]-benzenesulfonamide
InChi Key
QRJTZIJWDLJKQO-UHFFFAOYSA-N
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)
SMILES Code
O=S(C1=CC=C(NC2=NC=CC(N3CCCC4=C3C=CC(O)=C4)=N2)C=C1)(NCC5CC5)=O
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO
Shelf Life
>2 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
Biological target:
Pyrintegrin significantly boosts human embryonic stem cell (hESC) survival by over 30-fold at a concentration of 2 µM. It enhances integrin-dependent hESC attachment to various extracellular matrices like Matrigel™ and laminin, all while not notably affecting cell proliferation. Pyrintegrin also intensifies the binding of the activated β1 integrin-specific antibody HUTS-21 and amplifies the phosphorylation of several growth factor receptors along with their downstream kinases, such as PI3K and MAPK.
In vitro activity:
Pyrintegrin stimulated human adipose tissue derived ASCs 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.
Reference: Sci Rep. 2017 Jan 27;7:36402. doi: 10.1038/srep36402. https://pubmed.ncbi.nlm.nih.gov/28128224/
In vivo activity:
Pyrintegrin protected mice from LPS-induced podocyte foot process effacement and proteinuria. Cotreatment with pyrintegrin prevented LPS-induced reduction of active β1 integrin in the podocytes. In rats, pyrintegrin reduced peak proteinuria caused by puromycin aminonucleoside-induced nephropathy.
Reference: J Am Soc Nephrol. 2015 Nov;26(11):2741-52. https://pubmed.ncbi.nlm.nih.gov/25858967/
|
Solvent |
mg/mL |
mM |
comments |
| Solubility |
| DMF |
50.0 |
110.73 |
|
| DMSO |
30.0 |
66.44 |
|
| Ethanol |
1.0 |
2.21 |
|
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.
Preparing Stock Solutions
The following data is based on the
product
molecular weight
451.54
Batch specific molecular weights may vary
from batch to batch
due to the degree of hydration, which will
affect the solvent
volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass |
1 mg |
5 mg |
10 mg |
| 1 mM |
1.15 mL |
5.76 mL |
11.51 mL |
| 5 mM |
0.23 mL |
1.15 mL |
2.3 mL |
| 10 mM |
0.12 mL |
0.58 mL |
1.15 mL |
| 50 mM |
0.02 mL |
0.12 mL |
0.23 mL |
Formulation protocol:
1. Shah BS, Chen M, Suzuki T, Embree M, Kong K, Lee CH, He L, Xiang L, Ahn JA, Ding S, Mao JJ. Pyrintegrin Induces Soft Tissue Formation by Transplanted or Endogenous Cells. Sci Rep. 2017 Jan 27;7:36402. doi: 10.1038/srep36402. PMID: 28128224; PMCID: PMC5269584.
2. Lee HW, Khan SQ, Faridi MH, Wei C, Tardi NJ, Altintas MM, Elshabrawy HA, Mangos S, Quick KL, Sever S, Reiser J, Gupta V. A Podocyte-Based Automated Screening Assay Identifies Protective Small Molecules. J Am Soc Nephrol. 2015 Nov;26(11):2741-52. doi: 10.1681/ASN.2014090859. Epub 2015 Apr 9. PMID: 25858967; PMCID: PMC4625676.
In vitro protocol:
1. Shah BS, Chen M, Suzuki T, Embree M, Kong K, Lee CH, He L, Xiang L, Ahn JA, Ding S, Mao JJ. Pyrintegrin Induces Soft Tissue Formation by Transplanted or Endogenous Cells. Sci Rep. 2017 Jan 27;7:36402. doi: 10.1038/srep36402. PMID: 28128224; PMCID: PMC5269584.
2. Lee HW, Khan SQ, Faridi MH, Wei C, Tardi NJ, Altintas MM, Elshabrawy HA, Mangos S, Quick KL, Sever S, Reiser J, Gupta V. A Podocyte-Based Automated Screening Assay Identifies Protective Small Molecules. J Am Soc Nephrol. 2015 Nov;26(11):2741-52. doi: 10.1681/ASN.2014090859. Epub 2015 Apr 9. PMID: 25858967; PMCID: PMC4625676.
In vivo protocol:
1. Shah BS, Chen M, Suzuki T, Embree M, Kong K, Lee CH, He L, Xiang L, Ahn JA, Ding S, Mao JJ. Pyrintegrin Induces Soft Tissue Formation by Transplanted or Endogenous Cells. Sci Rep. 2017 Jan 27;7:36402. doi: 10.1038/srep36402. PMID: 28128224; PMCID: PMC5269584.
2. Lee HW, Khan SQ, Faridi MH, Wei C, Tardi NJ, Altintas MM, Elshabrawy HA, Mangos S, Quick KL, Sever S, Reiser J, Gupta V. A Podocyte-Based Automated Screening Assay Identifies Protective Small Molecules. J Am Soc Nephrol. 2015 Nov;26(11):2741-52. doi: 10.1681/ASN.2014090859. Epub 2015 Apr 9. PMID: 25858967; PMCID: PMC4625676.
1: Shah BS, Chen M, Suzuki T, Embree M, Kong K, Lee CH, He L, Xiang L, Ahn JA, Ding S, Mao JJ. Pyrintegrin Induces Soft Tissue Formation by Transplanted or Endogenous Cells. Sci Rep. 2017 Jan 27;7:36402. doi: 10.1038/srep36402. PubMed PMID: 28128224; PubMed Central PMCID: PMC5269584.
2: Lee HW, Khan SQ, Faridi MH, Wei C, Tardi NJ, Altintas MM, Elshabrawy HA, Mangos S, Quick KL, Sever S, Reiser J, Gupta V. A Podocyte-Based Automated Screening Assay Identifies Protective Small Molecules. J Am Soc Nephrol. 2015 Nov;26(11):2741-52. doi: 10.1681/ASN.2014090859. Epub 2015 Apr 9. PubMed PMID: 25858967; PubMed Central PMCID: PMC4625676.
