Biological Activity
TRPA1 channel blocker that antagonizes AITC- and 4-HNE-evoked calcium influx (IC50 values are 14.3 and 18.7μM respectively). Attenuates diabetic hypersensitivity in an in vivo rat model.
Compound Libraries
TCS 5861528 is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 369.42 |
| Formula | C19H23N5O3 |
| Storage | Store at RT |
| Purity | ≥98% (HPLC) |
| CAS Number | 332117-28-9 |
| PubChem ID | 2873523 |
| InChI Key | ZUTUWJYMCADJHD-UHFFFAOYSA-N |
| Smiles | O=C1C2=C(N=CN2CC(NC3=CC=C(C(C)CC)C=C3)=O)N(C)C(N1C)=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 | |||
| DMSO | 36.94 | 100 | |
| ethanol | 3.69 | 10 |
Preparing Stock Solutions
The following data is based on the product molecular weight 369.42. 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 | 2.71 mL | 13.53 mL | 27.07 mL |
| 5 mM | 0.54 mL | 2.71 mL | 5.41 mL |
| 10 mM | 0.27 mL | 1.35 mL | 2.71 mL |
| 50 mM | 0.05 mL | 0.27 mL | 0.54 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Wei et al (2009) Attenuation of mechanical hypersensitivity by an antagonist of the TRPA1 ion channel in diabetic animals. Anesthesiology 111 147 PMID: 19512877
Wei et al (2010) Roles of cutaneous versus spinal TRPA1 channels in mechanical hypersensitivity in the diabetic or mustard oil-treated non-diabetic rat. Neuropharmacology. 58 578 PMID: 20004676
Wei et al (2010) Spinal TRPA1 ion channels contribute to the cutaneous neurogenic inflammation in the rat. Neurosci.Letts. 479 253 PMID:
Keywords: TCS 5861528, supplier, Selective, TRPA1, blockers, antagonists, Channels, Transient, Receptor, Potential, HC030031, TCS5861528, TRPA1, TRPA1, Tocris Bioscience
