网站主页 >> CAS数据库列表 >> 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-CARBONYL-TYR-ALA-LEU-PRO-LEU-NH2
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- CAS号:
- 185413-30-3
- 英文名:
- AF12198
- 英文别名:
- AF12198;AF12198（TFA）;Ac-FEWTPGWYQ（Aze）YALPL-NH2;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-
- 中文名:
- AC-PHE-GLU-TRP-THR-PRO-GLY-TRP-TYR-GLN-L-AZETIDINE-2-CARBONYL-TYR-ALA-LEU-PRO-LEU-NH2
- 中文别名:
- I型IL-1受体拮抗剂多肽;AF12198,人类I型白介素受体拮抗剂;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
- CBNumber:
- CB5268870
- 分子式:
- C96H123N19O22
- 分子量:
- 1895.12
- MOL File:
- 185413-30-3.mol
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AC-PHE-GLU-TRP-THR-PRO-GLY-TRP-TYR-GLN-L-AZETIDINE-2-CARBONYL-TYR-ALA-LEU-PRO-LEU-NH2化学性质
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熔点:
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>179°C (dec.)
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密度:
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1.353±0.06 g/cm3(Predicted)
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储存条件:
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−20°C
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溶解度:
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DMSO (Slightly), Methanol (Slightly), Water (Very Slightly)
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酸度系数(pKa):
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4.44±0.10(Predicted)
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形态:
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solid
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颜色:
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White to Off-White
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AC-PHE-GLU-TRP-THR-PRO-GLY-TRP-TYR-GLN-L-AZETIDINE-2-CARBONYL-TYR-ALA-LEU-PRO-LEU-NH2性质、用途与生产工艺
AF12198 是针对人类I型白介素-1 受体 (IL1R1) (IC50=8 nM) 的有效，选择性和特异性肽拮抗剂，但不是针对人类 II 型受体 (IC50=6.7 µM) 或鼠 I 型受体 (IC50>200 µM)。AF12198 抑制 IL-1 诱导的 IL-8 产生 (IC50=25 nM) 和 IL-1诱导的细胞间粘附分子 1 (ICAM-1) 表达 (IC50=9 nM)。AF12198 具有抗炎活性，并在体内阻断了对 IL-1 的反应。
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.
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Animal Model:
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Male Wistar rats
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Dosage:
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16 mg/kg
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Administration:
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Intravenous infusion; 30 min before LPS intravenous injection
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Result:
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Decreased pulmonary microvascular leakage in rats.
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AC-PHE-GLU-TRP-THR-PRO-GLY-TRP-TYR-GLN-L-AZETIDINE-2-CARBONYL-TYR-ALA-LEU-PRO-LEU-NH2
上下游产品信息
上游原料
下游产品
| 更新日期 | 产品编号 | 产品名称 | CAS编号 | 包装 | 价格 |
|---|
| 2024/04/30 | 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 |
| 2024/04/30 | 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 |
AC-PHE-GLU-TRP-THR-PRO-GLY-TRP-TYR-GLN-L-AZETIDINE-2-CARBONYL-TYR-ALA-LEU-PRO-LEU-NH2
生产厂家
185413-30-3, AC-PHE-GLU-TRP-THR-PRO-GLY-TRP-TYR-GLN-L-AZETIDINE-2-CARBONYL-TYR-ALA-LEU-PRO-LEU-NH2 相关搜索:
- 药靶配体
- 目录肽
- 标准品
- C96H123N19O22
- I型IL-1受体拮抗剂多肽
- AF12198,人类I型白介素受体拮抗剂
- 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
- 185413-30-3
- AF12198（TFA）
- Ac-FEWTPGWYQ（Aze）YALPL-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-PHE-GLU-TRP-THR-PRO-GLY-TRP-TYR-GLN-L-AZETIDINE-2-CARBOXYLIC ACID-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-AZE-TYR-ALA-LEU-PRO-LEU-NH2
- AF12198