Biological Activity
Potent α2β1 integrin inhibitor (IC50 values for the inhibition of human platelet adhesion to type I collagen are 12 and 715 nM for platelets under static conditions and under flow, respectively). Displays selectivity for α2β1 over αvβ3, α5β1, α6β1 and αIIbβ3 at concentrations exceeding 1000 nM. Reduces collagen IV production in mesangial cells. Active in vivo; prevents ferric chloride-induced clot formation in mice.
Licensing Information
Sold under license from the University of Pennsylvania.
Compound Libraries
TC-I 15 is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 520.62 |
| Formula | C23H28N4O6S2 |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 916734-43-5 |
| PubChem ID | 90488948 |
| InChI Key | XKLHCUGVLCGKKX-RBUKOAKNSA-N |
| Smiles | CC1(C)SCN(S(C3=CC=CC=C3)(=O)=O)[C@@H]1[C@@](N[C@H](C(O)=O)CNC(NCC2=CC=CC=C2)=O)=O |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| 1.1eq. NaOH | 13.02 | 25 | |
| DMSO | 52.06 | 100 | |
| ethanol | 52.06 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 520.62. Batch specific molecular weights may vary from batch to batch due to solvent 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 | 1.92 mL | 9.6 mL | 19.21 mL |
| 5 mM | 0.38 mL | 1.92 mL | 3.84 mL |
| 10 mM | 0.19 mL | 0.96 mL | 1.92 mL |
| 50 mM | 0.04 mL | 0.19 mL | 0.38 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Borza et al (2012) Inhibition of integrin α2β1 ameliorates glomerular injury. J.Am.Soc.Nephrol. 23 1027 PMID: 22440900
Miller et al (2009) Small-molecule inhibitors of integrin α2β1 that prevent pathological thrombus formation via an allosteric mechanism. Proc.Natl.Acad.Sci.U.S.A. 106 719 PMID: 19141632
Keywords: TC-I 15, supplier, TC-I15, integrins, receptors, a2b1, alpha2beta1, α2β1, inhibitors, inhibits, potent, selective, active, in, vivo, antithrombotics, collagen, Integrins, Cell, Adhesion, Molecules, Integrins, Tocris Bioscience
