AC-PHE-GLU-TRP-THR-PRO-GLY-TRP-TYR-GLN-L-AZETIDINE-2-CARBONYL-TYR-ALA-LEU-PRO-LEU-NH2 CAS#: 185413-30-3

AC-PHE-GLU-TRP-THR-PRO-GLY-TRP-TYR-GLN-L-AZETIDINE-2-CARBONYL-TYR-ALA-LEU-PRO-LEU-NH2

生物活性靶点体外研究体内研究用途与合成方法 MSDS AC-PHE-GLU-TRP-THR-PRO-GLY-TRP-TYR-GLN-L-AZETIDINE-2-CARBONYL-TYR-ALA-LEU-PRO-LEU-NH2价格(试剂级) 上下游产品信息

中文名称	AC-PHE-GLU-TRP-THR-PRO-GLY-TRP-TYR-GLN-L-AZETIDINE-2-CARBONYL-TYR-ALA-LEU-PRO-LEU-NH2
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;AF12198,人TYPE I INTERLEUKIN RECEPTOR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）;AF12198, human type I interleukin receptor antagonist
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.)
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）
形态	固体
酸度系数(pKa)	4.44±0.10(Predicted)
颜色	白色至类白色
序列	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 用途与合成方法

生物活性

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。

靶点

IL1R1

8 mM (IC ₅₀ )

体外研究

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.

体内研究

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

MSDS信息

提供商	语言
SigmaAldrich	英文

AC-PHE-GLU-TRP-THR-PRO-GLY-TRP-TYR-GLN-L-AZETIDINE-2-CARBONYL-TYR-ALA-LEU-PRO-LEU-NH2 价格(试剂级)

更新日期	产品编号	产品名称	CAS号	包装	价格
2025/12/22	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	990元
2025/12/22	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	2500元

AC-PHE-GLU-TRP-THR-PRO-GLY-TRP-TYR-GLN-L-AZETIDINE-2-CARBONYL-TYR-ALA-LEU-PRO-LEU-NH2