产品
编 号：F620872
分子式：C13H15FN2O
分子量：234.27
分子式：C13H15FN2O
分子量：234.27
产品类型
规格
价格
是否有货
1mg
询价
询价
5mg
询价
询价
10mg
询价
询价
结构图
CAS No: 2100285-41-2
产品详情
生物活性：
AZ8838 is a potent, competitive, allosteric, orally active non-peptide small molecule antagonist of PAR2 with a pKi of 6.4 for hPAR2.
体内研究：
AZ8838 (10?mg/kg; p.o.; 2?h prior) is anti-inflammatory in a PAR2 agonist-induced rat paw oedema model.Animal Model:Wistar rats, PAR2 agonist 2f-LIGRLO-NH2 induced acute oedema model
Dosage:10 mg/kg
Administration:Oral administration, once, 2?h prior
Result:Showed 60% reduction of paw swelling. Inhibited 2f-LIGRLO-NH2 induced activated mast cells, inhibited 2f-LIGRLO-NH2 decreased tryptase-positive (AA1+ve) intact mast cells in paw, blocked histamine release.
体外研究：
AZ8838 binds in an occluded pocket.AZ8838 is a potent antagonist against SLIGRL-NH2 in the Ca2+ assay with a pIC50 of 5.70?±?0.02.AZ8838 shows a potency trend when inhibiting IP1 production (pIC50 = 5.84?±?0.02).AZ8838 attenuates both peptide-induced phosphorylation of ERK1/2 (pIC50 = 5.7?±?0.1) and β-arrestin-2 recruitment (pIC50 = 6.1?±?0.1).
AZ8838 is a potent, competitive, allosteric, orally active non-peptide small molecule antagonist of PAR2 with a pKi of 6.4 for hPAR2.
体内研究：
AZ8838 (10?mg/kg; p.o.; 2?h prior) is anti-inflammatory in a PAR2 agonist-induced rat paw oedema model.Animal Model:Wistar rats, PAR2 agonist 2f-LIGRLO-NH2 induced acute oedema model
Dosage:10 mg/kg
Administration:Oral administration, once, 2?h prior
Result:Showed 60% reduction of paw swelling. Inhibited 2f-LIGRLO-NH2 induced activated mast cells, inhibited 2f-LIGRLO-NH2 decreased tryptase-positive (AA1+ve) intact mast cells in paw, blocked histamine release.
体外研究：
AZ8838 binds in an occluded pocket.AZ8838 is a potent antagonist against SLIGRL-NH2 in the Ca2+ assay with a pIC50 of 5.70?±?0.02.AZ8838 shows a potency trend when inhibiting IP1 production (pIC50 = 5.84?±?0.02).AZ8838 attenuates both peptide-induced phosphorylation of ERK1/2 (pIC50 = 5.7?±?0.1) and β-arrestin-2 recruitment (pIC50 = 6.1?±?0.1).
产品资料
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