AF 12198|185413-30-3|-陌孚医药/Medlife

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AF 12198

目录号: PC15044 纯度: ≥98%

CAS No. :185413-30-3

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中文名称

AF 12198

英文名称

AF 12198

英文别名

L-Leucinamide,N-acetyl-L-phenylalanyl-L-a-glutamyl-L-tryptophyl-L-threonyl-L-prolylglycyl-L-tryptophyl-L-tyrosyl-L-glutaminyl-(2S)-2-azetidinecarbonyl-L-tyrosyl-L-alanyl-L-leucyl-L-prolyl-(9CI);Ac-Phe-Glu-Trp-Thr-Pro-Gly-Trp-Tyr-Gln-L-azetidine-2-carbonyl-Tyr-Ala-Leu-Pro-Leu-NH?;Ac-Phe-Glu-Trp-Thr-Pro-Gly-Trp-Tyr-Gln-L-azetidine-2-carbonyl-Tyr-Ala-Leu-Pro-Leu-NH₂;AF 12198;L-Leucinamide,N-acetyl-L-phenylalanyl-L-a-glutamyl-L-tryptophyl-L-threonyl-L-prolylglycyl-L-tr...;L-Leucinamide,N-acetyl-L-phenylalanyl-L-a-glutamyl-L-tryptophyl-L-threonyl-L-prolylglycyl-L-tryptophyl-L-tyrosyl-L-glutaminyl;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-CARBOXYLIC ACID-TYR-ALA-LEU-PRO-LEU-NH2

Cas No.

185413-30-3

分子式

C₉₆H₁₂₃N₁₉O₂₂

分子量

1895.12

包装储存

Sealed storage, away from moisture and light, under nitrogen

Powder	-80°C	2 years
	-20°C	1 year

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light, under nitrogen)

生物活性

AF12198 is a potent, selective and specific peptide antagonist for human type I interleukin-1 receptor (IL1-R1) (IC₅₀=8 nM) but not the human type II receptor (IC₅₀=6.7 μM) or the murine type I receptor (IC₅₀>200 μM). AF12198 inhibits IL-1-induced IL-8 production (IC₅₀=25 nM) and IL-1-induced intercellular adhesion molecule-1 (ICAM-1) expression (IC₅₀=9 nM) 体外研究. AF12198 has anti-inflammatory activities and blocks responses to IL-1 in vivo.

性状

Solid

IC50 & Target[1][2]

IL1R1

8 nM (IC₅₀)

体外研究(In Vitro)

AF12198 competes for binding of I-IL-1α with an IC₅₀ of 8.0 nM, nearly equal to that of IL-1ra, IC₅₀ of 4.0 nM for the type I receptor.
AF12198 (0-5 ng; 8 hours) inhibits IL-6 induction with an IC₅₀ of 15 μM whereas IL-1ra inhibits with an IC₅₀ of 2 nM in heparinized human primate blood. Meanwhile, With blood from cynomolgus monkeys, the IC₅₀ 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.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(In Vivo)

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.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

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.

运输条件

Room temperature or refrigerated transportation.

储存方式

Sealed storage, away from moisture and light, under nitrogen

Powder	-80°C	2 years
	-20°C	1 year

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light, under nitrogen)

SequenceShortening

Ac-FEWTPGWYQ-{Aze}-YALPL-NH2

Sequence

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

参考文献

[1]. F Aimbire, et al. Low level laser therapy (LLLT) decreases pulmonary microvascular leakage, neutrophil influx and IL-1beta levels in airway and lung from rat subjected to LPS-induced inflammation. Inflammation [Information]

[2]. A L Akeson, et al.AF12198, a novel low molecular weight antagonist, selectively binds the human type I interleukin (IL)-1 receptor and blocks in vivo responses to IL-1. J Biol Chem. 1996 Nov 29;271(48):30517-23. [Information]

溶解度数据

体外研究:

DMSO : 100 mg/mL (52.77 mM; Need ultrasonic)

配制储备溶液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	0.5277 mL	2.6384 mL	5.2767 mL
5 mM	0.1055 mL	0.5277 mL	1.0553 mL
10 mM	0.0528 mL	0.2638 mL	0.5277 mL

产品不同，其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液；配成溶液后，建议分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light, under nitrogen)。-80°C 储存时，建议在 6 个月内使用，-20°C 储存时，建议在 1 个月内使用。

体内研究:

建议根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都建议先按照 体外研究 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

建议依照次序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.5 mg/mL (1.32 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (1.32 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH?O 中，得到澄清透明的生理盐水溶液
2.

建议依照次序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.5 mg/mL (1.32 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (1.32 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

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产品使用指南

Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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