Powder: -20°C for 3 years | In solvent: -80°C for 1 year
AM-0902 是有效的瞬时受体电位 A1 选择性拮抗剂,作用于rTRPA1和hTRPA1的IC50分别为 71 和 131 nM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 333 | 现货 | ||
5 mg | ¥ 778 | 现货 | ||
10 mg | ¥ 996 | 现货 | ||
25 mg | ¥ 1,660 | 现货 | ||
50 mg | ¥ 2,470 | 现货 | ||
100 mg | ¥ 3,680 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 779 | 现货 |
产品描述 | AM-0902 is a potent and specific TRPA1 antagonist (IC50s: 71/131 nM for rTRPA1 and hTRPA1). |
靶点活性 | TRPA1 (rat):71 nM, TRPA1 (human):131 nM |
体外活性 | AM-0902 is highly permeable (average Papp=44.5 μcm/s in MDCK cells), an unlikely substrate for P-gp (efflux ratio=1.3 in P-gp overexpressing MDCK cells), and demonstrates good solubility (PBS pH 7.4: 226 μM, SIF: 248 μM). AM-0902 shows good selectivity over other TRP channels, as no activity is observed against human TRPV1 or TRPV4, or rat TRPV1, TRPV3, or TRPM8, at concentrations up to 10 μM. AM-0902 inhibits 45Ca2+ flux upon activation of rat TRPA1 with methylglyoxal (IC50: 0.019 μM). |
体内活性 | AM-0902 has moderate terminal elimination half-life (t1/2=0.6 h and 2.8 h for rat (0.5 mg/kg, iv), rat (30 mg/kg, oral)). A dose-dependent reduction of allyl isothiocyanate (AITC)-induced flinching is observed for AM-0902, with a significant reduction in flinching, observed postdosing of 10 and 30 mg/kg. The unbound plasma concentrations (Cu) at 1 h for the 1, 3, 10, and 30 mg/kg doses are 0.051±0.024, 0.19±0.11, 0.58±0.35, and 2.2±0.40 μM, covering the in vitro rat TRPA1 45Ca2+ IC50 at 0.72, 2.7, 8.2, and 30.3 fold, respectively. A good exposure-response relationship is observed in this target coverage model. An unbound in vivo IC50 of 0.35 μM, which is in good agreement with the in vitro rat TRPA1 45Ca2+ IC50, and unbound in vivo IC90 of 1.7 μM are determined. It is noteworthy that at a dose of 30 mg/kg, AM-0902 engages TRPA1 at concentrations that exceed the in vivo IC90, making it a useful tool for the exploration of in vivo models of acute pain. |
细胞实验 | On the day of assay, culture media is removed and MDCK cells are incubated for 10 min at room temperature (RT) with 50 μL of AM-0902 in AM-0902 dilution buffer [HBSS containing 1 mM HEPES+0.1 mg/mL BSA] at final concentrations (2.0 nM to 40 μM, 1:3 ratio), followed by another 3 min incubation at RT. The reaction mixture is aspirated, and cells are washed three times with PBS containing 0.1 mg/mL BSA. Radioactivity is measured using a TopCount microplate scintillation counter. The activation of TRPA1 is measured by the cellular uptake of radioactive calcium. |
动物实验 | Rats are dosed orally with either vehicle (2% HPMC/1% Tween-80) or AM-0902 at 1, 3, 10, or 30 mg/kg. After 1 h, one left ventral hind paw is injected with the TRPA1 agonist AITC (0.1%). AM-0902 is also given by an intravenous (IV) injection to rats (0.5 mg/kg). |
分子量 | 370.79 |
分子式 | C17H15ClN6O2 |
CAS No. | 1883711-97-4 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 145 mg/mL (391.05 mM), Sonification and heating are recommended.
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.6969 mL | 13.4847 mL | 26.9694 mL | 67.4236 mL |
5 mM | 0.5394 mL | 2.6969 mL | 5.3939 mL | 13.4847 mL | |
10 mM | 0.2697 mL | 1.3485 mL | 2.6969 mL | 6.7424 mL | |
20 mM | 0.1348 mL | 0.6742 mL | 1.3485 mL | 3.3712 mL | |
50 mM | 0.0539 mL | 0.2697 mL | 0.5394 mL | 1.3485 mL | |
100 mM | 0.027 mL | 0.1348 mL | 0.2697 mL | 0.6742 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
AM-0902 1883711-97-4 Membrane transporter/Ion channel TRP/TRPV Channel Transient receptor potential channels TRP Channel Inhibitor inhibit AM 0902 AM0902 inhibitor