A 438079 hydrochloride
A 438079 hydrochloride is a selective antagonist of P2X7 receptor with IC50 values of 100 and 300 nM in rat and human, respectively [1].
A 438079 is a derivative of the origin compound tetrazole 5 selected out as a novel P2X7 receptor antagonist. In human 1321N1 astrocytoma cells with expressing recombinant human P2X7, A 438079 treatment suppressed the Ca 2+ flux with pIC50 value of 6.9. In the pore formation assay, A 438079 blocked the pore formation of human THP-1 cells and prevented the cells from uptaking the diiodide dye YO-PRO. Moreover, in the spinal nerve ligation model, administration of A 438079 reduced the neuropathic pain induced by the application of a von Frey hair. The ED50 value was 76 μM/kg [2].
References:
1. Nelson D W, Gregg R J, Kort M E, et al. Structure-activity relationship studies on a series of novel, substituted 1-benzyl-5-phenyltetrazole P2X7 antagonists. Journal of medicinal chemistry, 2006, 49(12): 3659-3666.
2. Donnelly-Roberts D L, Jarvis M F. Discovery of P2X7 receptor-selective antagonists offers new insights into P2X7 receptor function and indicates a role in chronic pain states. British journal of pharmacology, 2007, 151(5): 571-579.
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 342.61 |
| Cas No. | 899431-18-6 |
| Formula | C13H10Cl3N5 |
| Solubility | ≥34.3 mg/mL in DMSO; ≥49.8 mg/mL in EtOH with gentle warming and ultrasonic; ≥94 mg/mL in H2O |
| Chemical Name | 3-[[5-(2,3-dichlorophenyl)tetrazol-1-yl]methyl]pyridine;hydrochloride |
| SDF | Download SDF |
| Canonical SMILES | C1=CC(=C(C(=C1)Cl)Cl)C2=NN=NN2CC3=CN=CC=C3.Cl |
| Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
| General tips | We do not recommend long-term storage for the solution, please use it up soon. |
Quality Control & MSDS
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Chemical structure
