AZ8838

Name: AZ8838
Brand: TargetMol
SKU: T60319
Price: 2820 USD
Availability: InStock
Rating: 4.5 (1 reviews)

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产品编号 T60319Cas号 2100285-41-2

AZ8838 是一种有效的、竞争性的、变构的、口服活性的 PAR2非肽小分子拮抗剂，其对 hPAR2 的 pKi 值为 6.4。

还可以

产品编号 T60319Cas号 2100285-41-2

AZ8838 是一种有效的、竞争性的、变构的、口服活性的 PAR2非肽小分子拮抗剂，其对 hPAR2 的 pKi 值为 6.4。

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产品介绍

生物活性

产品描述	AZ8838 is an effective, competitive, allosteric, orally active non-peptide small molecule antagonist of PAR2 with a pK i of 6.4 for hPAR2 [1].
体外活性	AZ8838 binds in an occluded pocket [1]. AZ8838 is a potent antagonist against SLIGRL-NH 2 in the Ca 2+ assay with a pIC 50 of 5.70 ± 0.02 [1]. AZ8838 exhibits a potency trend when inhibiting IP1 production (pIC 50 = 5.84 ± 0.02) [1]. AZ8838 attenuates both peptide-induced phosphorylation of ERK1/2 (pIC 50 = 5.7 ± 0.1) and β-arrestin-2 recruitment (pIC 50 = 6.1 ± 0.1) [1].
体内活性	AZ8838 (10 mg/kg; p.o.; 2 h prior) has anti-inflammatory in a PAR2 agonist-induced rat paw oedema model [1]. Animal Model: Wistar rats, PAR2 agonist 2f-LIGRLO-NH 2 induced acute oedema model [1] Dosage: 10 mg/kg Administration: Oral administration, once, 2 h prior Result: Showed 60% reduction of paw swelling. Inhibited 2f-LIGRLO-NH 2 induced activated mast cells, inhibited 2f-LIGRLO-NH 2 decreased tryptase-positive (AA1+ve) intact mast cells in paw, blocked histamine release.