AZ8838
CAS No. : 2100285-41-2
| Size | Price | Stock |
|---|---|---|
| 1mg | $156 | In-stock |
| 5mg | $390 | In-stock |
| 10mg | $650 | In-stock |
| 25mg | $1250 | In-stock |
| 50mg | $2000 | In-stock |
| 100mg | $3200 | In-stock |
| 200 mg | Get quote | |
| 500 mg | Get quote | |
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| Cat. No. : | HY-123617 |
| M.Wt: | 234.27 |
| Formula: | C13H15FN2O |
| Purity: | >98 % |
| Solubility: | DMSO : 200 mg/mL (ultrasonic) |
AZ8838 is a potent, competitive, allosteric, orally active non-peptide small molecule antagonist of PAR2 with a pKi of 6.4 for hPAR2[1].
In Vitro: AZ8838 binds in an occluded pocket[1].
AZ8838 is a potent antagonist against SLIGRL-NH2 in the Ca2+ assay with a pIC50 of 5.70?±?0.02[1].
AZ8838 shows a potency trend when inhibiting IP1 production (pIC50 = 5.84?±?0.02)[1].
AZ8838 attenuates both peptide-induced phosphorylation of ERK1/2 (pIC50 = 5.7?±?0.1) and β-arrestin-2 recruitment (pIC50 = 6.1?±?0.1)[1].
In Vivo: AZ8838 (10?mg/kg; p.o.; 2?h prior) is anti-inflammatory in a PAR2 agonist-induced rat paw oedema model[1].
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