185413-30-3

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

英文名稱 AF12198

CAS 185413-30-3

分子式 C96H123N19O22

分子量 1895.12

MOL 文件 185413-30-3.mol

更新日期 2026/06/11 18:19:27

185413-30-3 結(jié)構(gòu)式

基本信息物理化學(xué)性質(zhì) 安全數(shù)據(jù) AC-PHE-GLU-TRP-THR-PRO-GLY-TRP-TYR-GLN-L-AZETIDINE-2-CARBONYL-TYR-ALA-LEU-PRO-LEU-NH2價(jià)格(試劑級(jí)) 常見(jiàn)問(wèn)題列表

基本信息

英文別名

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

物理化學(xué)性質(zhì)

熔點(diǎn)>179°C (dec.)

密度1.353±0.06 g/cm3(Predicted)

儲(chǔ)存條件−20°C

溶解度DMSO（微溶）、甲醇（微溶）、水（微溶）

酸度系數(shù)(pKa)4.44±0.10(Predicted)

形態(tài)solid

顏色白色至灰白色

序列Ac-Phe-Glu-Trp-Thr-Pro-Gly-Trp-Tyr-Gln-{Aze}-Tyr-Ala-Leu-Pro-Leu-NH2

安全數(shù)據(jù)

WGK Germany3

AC-PHE-GLU-TRP-THR-PRO-GLY-TRP-TYR-GLN-L-AZETIDINE-2-CARBONYL-TYR-ALA-LEU-PRO-LEU-NH2價(jià)格(試劑級(jí))

報(bào)價(jià)日期	產(chǎn)品編號(hào)	產(chǎn)品名稱	CAS號(hào)	包裝	價(jià)格
2026/06/05	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
2026/06/05	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
2026/06/05	HY-P1110	AF12198	185413-30-3	10 mg	4000元

常見(jiàn)問(wèn)題列表

生物活性

AF12198 是針對(duì)人類I型白介素-1 受體 (IL1R1) (IC50=8 nM) 的有效，選擇性和特異性肽拮抗劑，但不是針對(duì)人類 II 型受體 (IC50=6.7 μM) 或鼠 I 型受體 (IC50>200 μM)。AF12198 抑制 IL-1 誘導(dǎo)的 IL-8 產(chǎn)生 (IC50=25 nM) 和 IL-1誘導(dǎo)的細(xì)胞間粘附分子 1 (ICAM-1) 表達(dá) (IC50=9 nM)。AF12198 具有抗炎活性，并在體內(nèi)阻斷了對(duì) IL-1 的反應(yīng)。

靶點(diǎn)

IL1R1

8 mM (IC ₅₀ )

體外研究

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.

體內(nèi)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.