AC-PHE-GLU-TRP-THR-PRO-GLY-TRP-TYR-GLN-L-AZETIDINE-2-CARBONYL-TYR-ALA-LEU-PRO-LEU-NH2
| 中文名称 | AC-PHE-GLU-TRP-THR-PRO-GLY-TRP-TYR-GLN-L-AZETIDINE-2-CARBONYL-TYR-ALA-LEU-PRO-LEU-NH2 |
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| 中文同义词 | N-乙酰基-L-苯基丙氨酰基-L-Α-谷氨酰基-L-色氨酰基-L-苏氨酰基-L-脯氨酰甘氨酰基-L-色氨酰基-L-酪氨酰基-L-谷氨酰胺基-(2S)-2-氮杂环丁烷羰基-L-酪氨酰基-L-丙氨酰基-L-亮氨酰基-L-脯氨酰基-L-亮氨酸酰胺;I型IL-1受体拮抗剂多肽;AF12198,人类I型白介素受体拮抗剂 |
| 英文名称 | AF12198 |
| 英文同义词 | AF12198;AC-PHE-GLU-TRP-THR-PRO-GLY-TRP-TYR-GLN-AZE-TYR-ALA-LEU-PRO-LEU-NH2;AC-PHE-GLU-TRP-THR-PRO-GLY-TRP-TYR-GLN-L-AZETIDINE-2-CARBONYL-TYR-ALA-LEU-PRO-LEU-NH2;AC-PHE-GLU-TRP-THR-PRO-GLY-TRP-TYR-GLN-L-AZETIDINE-2-CARBOXYLIC ACID-TYR-ALA-LEU-PRO-LEU-NH2;L-Leucinamide, N-acetyl-L-phenylalanyl-L-α-glutamyl-L-tryptophyl-L-threonyl-L-prolylglycyl-L-tryptophyl-L-tyrosyl-L-glutaminyl-(2S)-2-azetidinecarbonyl-L-tyrosyl-L-alanyl-L-leucyl-L-prolyl-;Ac-FEWTPGWYQ（Aze）YALPL-NH2;AF12198（TFA） |
| CAS号 | 185413-30-3 |
| 分子式 | C96H123N19O22 |
| 分子量 | 1895.12 |
| EINECS号 | |
| 相关类别 | 标准品 |
| Mol文件 | 185413-30-3.mol |
| 结构式 |  |
AC-PHE-GLU-TRP-THR-PRO-GLY-TRP-TYR-GLN-L-AZETIDINE-2-CARBONYL-TYR-ALA-LEU-PRO-LEU-NH2 性质
| 熔点 | >179°C (dec.) |
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| 密度 | 1.353±0.06 g/cm3(Predicted) |
| 储存条件 | −20°C |
| 溶解度 | DMSO（微溶）、甲醇（微溶）、水（微溶） |
| 酸度系数(pKa) | 4.44±0.10(Predicted) |
| 形态 | 固体 |
| 颜色 | 白色至类白色 |
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IL1R1 8 mM (IC 50 ) |
AF12198 competes for binding of 125 I-IL-1α with an IC 50 of 8.0 nM, nearly equal to that of IL-1ra, IC 50 of 4.0 nM for the type I receptor.AF12198 (0-5 ng; 8 hours) inhibits IL-6 induction with an IC 50 of 15 μM whereas IL-1ra inhibits with an IC 50 of 2 nM in heparinized human primate blood. Meanwhile, With blood from cynomolgus monkeys, the IC 50 values are 17 μM for AF12198 and 30 nM for IL-1ra. Additionally, AF12198 or IL-1RA alone does not induce IL-6 in blood from either humans or cynomolgus monkeys.
AF12198 (intravenous infusion; 16 mg/kg; 30 min before LPS intravenous injection) significantly attenuates the increase in lung MPO activity induced by LPS in acute lung inflammation and it reduces the lung microvascular leakage from rats inflamed with LPS at the 4 h (32.6%), 12 h (50.1%) and 24 h (65.3%) after LPS.
| Animal Model: | Male Wistar rats |
| Dosage: | 16 mg/kg |
| Administration: | Intravenous infusion; 30 min before LPS intravenous injection |
| Result: | Decreased pulmonary microvascular leakage in rats. |
安全信息
| WGK Germany | 3 |
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| 提供商 | 语言 |
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英文
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| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2024/08/19 | HY-P1110 | AC-PHE-GLU-TRP-THR-PRO-GLY-TRP-TYR-GLN-L-AZETIDINE-2-CARBONYL-TYR-ALA-LEU-PRO-LEU-NH2 AF12198 | 185413-30-3 | 1mg | 1200元 |
| 2024/08/19 | HY-P1110 | AC-PHE-GLU-TRP-THR-PRO-GLY-TRP-TYR-GLN-L-AZETIDINE-2-CARBONYL-TYR-ALA-LEU-PRO-LEU-NH2 AF12198 | 185413-30-3 | 5mg | 3500元 |