2. GPCR/G Protein Neuronal Signaling
  3. Cannabinoid Receptor
  4. AM251

AM251是选择性大麻素1 (CB1) 受体拮抗剂，IC50 为8 nM。AM251也是 GPR55 的激动剂，EC50为39 nM。

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AM251 Chemical Structure

AM251 Chemical Structure

CAS No. : 183232-66-8

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥586
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1 mg ￥240
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5 mg ￥480
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10 mg ￥850
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50 mg ￥2860
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200 mg   询价  

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Customer Review

AM251 相关抗体

Top Publications Citing Use of Products

    AM251 purchased from MCE. Usage Cited in: Clin Exp Pharmacol Physiol. 2018 Aug;45(8):832-840.  [Abstract]

    Pretreatment of AM251 (10 nM, for 30 minutes) reverses the Spermidine (Spd)-provided suppression on the high glucose (HG)-induced upregulations of p16INK4a in HT-22 cells.

    查看 Cannabinoid Receptor 亚型特异性产品:

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    CB1 CB2

    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    AM251 is a selective cannabinoid 1 (CB1) receptor antagonist with an IC50 of 8 nM. AM251 also acts as a potent GPR55 agonist with an EC50 of 39 nM[1][2][3].

    IC50 & Target

    IC50: 8 nM (CB1 receptor)[1]
    细胞效力
    (Cellular Effect)
    Cell Line Type Value Description References
    HEK293 EC50
    0.63 μM
    Compound: AM251
    Agonist activity at human GPR55 expressed in HEK293 cells assessed as increase in oscillation Ca2+ transients by fura-2 dye based fluorescence analysis
    Agonist activity at human GPR55 expressed in HEK293 cells assessed as increase in oscillation Ca2+ transients by fura-2 dye based fluorescence analysis
    		10.1039/C3MD00394A
    Sf9 EC50
    0.07 μM
    Compound: AM251
    Inverse agonist activity at human CB1 receptor expressed in Sf9 cells coexpressing Gbeta1gamma2 and RSG4 assessed as degradation of [gamma-33P]GTP after 20 mins by steady-state GTPase assay
    Inverse agonist activity at human CB1 receptor expressed in Sf9 cells coexpressing Gbeta1gamma2 and RSG4 assessed as degradation of [gamma-33P]GTP after 20 mins by steady-state GTPase assay
    		[PMID: 25096297]
    体外研究
    (In Vitro)

    AM251 is a CB1 receptor antagonist/inverse agonist. AM251 produces an agonist response in HEK293 cells, similar to that found in the yeast expression system[2].
    ? AM-251 reduces cholesteryl ester synthesis in unstimulated and acetylated LDL-stimulated Raw 264.7 macrophages, CB2+/+ and CB2-/- peritoneal macrophages[3].

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

    AM251 相关抗体:
    体内研究
    (In Vivo)

    The CB1 antagonist AM251 (3 mg/kg, i.p.) decreases capsaicin-evoked nocifensive behavior. This suppressive effect is genotype dependent, and the interaction between the effects of genotype and AM251 approached significance. Planned comparisons reveal that AM251 reduces nocifensive behaviors in fatty-acid amide hydrolase (FAAH) KO mice (p<0.01) but fails to alter nocifensive behavior in WT mice (p>0.2) relative to their respective vehicle controls. AM251 (3 mg/kg, i.p.) reduces the duration of heat hypersensitivity in FAAH KO (F1,9=21.43, p<0.01) but not WT mice (p>0.3). AM251 suppresses capsaicin-evoked heat hypersensitivity in a time-dependent manner in FAAH KO (F5,9=4.349, p<0.01) but not in WT mice (p>0.3). Post-hoc analysis reveals that FAAH KO mice receiving vehicle (i.p.) display heightened thermal hypersensitivity at 30 (p<0.05), 60 (p<0.05), and 90 (p<0.001) minutes post-capsaicin in comparison to FAAH KO animals receiving AM251)[4].
    ? One-way ANOVA shows that AM251 (AM-251) injected into the rats significantly decreases both of the percentage of entries in the open arms and time spent in the open arms, compare to controls. The Tukey-Kramer test analysis reveals a significant reduction for the doses of 1 mg/kg (P<0.05) and 5 mg/kg (P<0.01) compare to control rats in the time spent in the open arms. Also, AM251 significantly decreases percentage of entries in the open arms for the doses of 1 and 5 mg/kg (P<0.05)[5].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    分子量

    555.24

    Formula

    C22H21Cl2IN4O
    CAS 号
    性状

    固体

    颜色

    White to off-white

    运输条件

    Room temperature in continental US; may vary elsewhere.
    储存方式
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    溶解性数据
    细胞实验： 

    DMSO 中的溶解度 : 25 mg/mL (45.03 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 1.8010 mL 9.0051 mL 18.0102 mL
    5 mM 0.3602 mL 1.8010 mL 3.6020 mL
    查看完整储备液配制表

    * 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，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, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

    • 摩尔计算器

    • 稀释计算器

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    质量
    =
    浓度
    ×
    体积
    ×
    分子量 *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    浓度 (start)

    C1

    ×
    体积 (start)

    V1

    =
    浓度 (final)

    C2

    ×
    体积 (final)

    V2

    动物实验：

    请根据您的 实验动物和给药方式 选择适当的溶解方案。

    以下溶解方案都请先按照 In Vitro 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

    • 方案 一

      请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.5 mg/mL (4.50 mM); 澄清溶液

      此方案可获得 ≥ 2.5 mg/mL（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；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水 定容至 1 mL。

      生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。
    • 方案 二

      请依序添加每种溶剂： 10% DMSO    90% Corn Oil

      Solubility: ≥ 2.5 mg/mL (4.50 mM); 澄清溶液

      此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液，此方案实验周期在半个月以上的动物实验酌情使用。

      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。

    动物溶解方案计算器
    请输入动物实验的基本信息：

    给药剂量

    mg/kg

    动物的平均体重

    g

    每只动物的给药体积

    μL

    动物数量

    只
    由于实验过程有损耗，建议您多配一只动物的量
    请输入您的动物体内配方组成：
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    如果您的动物是免疫缺陷鼠或者体弱鼠，建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
    方案所需 助溶剂 包括：DMSO， ，均可在 MCE 网站选购。 ，Tween 80，均可在 MCE 网站选购。
    计算结果
    工作液所需浓度 : mg/mL
    储备液配制方法 : mg 药物溶于 μL  DMSO（母液浓度为 mg/mL）。
    您所需的储备液浓度超过该产品的实测溶解度，以下方案仅供参考，如有需要，请与 MCE 中国技术支持联系。
    动物实验体内工作液的配制方法 : 取 μL DMSO 储备液，加入 μL 。 μL ，混合均匀至澄清，再加 μL Tween 80，混合均匀至澄清，再加 μL 生理盐水。
    连续给药周期超过半月以上，请谨慎选择该方案。
    请确保第一步储备液溶解至澄清状态，从左到右依次添加助溶剂。您可采用超声加热 （超声清洗仪，建议频次 20-40 kHz），涡旋吹打等方式辅助溶解。
    纯度 & 产品资料

    纯度: 99.25%

    COA (199 KB) HNMR (255 KB) LCMS (100 KB)

    产品使用指南 (1538 KB)
    参考文献
    Kinase Assay
    [3]

    Macrophages are seeded (2×106/well) in 12-well culture plates. AM-251 or SR144528 are added from 4 mM stock solutions prepared in DMSO, 1h prior to the addition of 7-ketocholesterol (7KC) from a 2 mg/mL ethanol stock solution. Controls are adjusted to receive equivalent volumes of DMSO and ethanol. After 16 h, caspase-3 activity is determined. All treatments are done in triplicate and the data presented as the mean RFLU/mg protein±SD[3].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [4][5]

    Mice[4]
    A total of 246 mice weighing 17-48 g are used in these experiments. Following determination of baseline responding, mice receive a single i.p injection (5 mL/kg) of AMG9810 (3 mg/kg, n=5 per group), AM251 (3 mg/kg, n=5 per group), or vehicle (n=6 per group). I.p. injections are performed 30 min prior to i.pl. capsaicin or vehicle administration. Paw withdrawal latencies are assessed before and 10, 30, 60, 90 and 120 min after intradermal injection of capsaicin or vehicle. Paw withdrawal latencies are measured in duplicate in each paw at each time point, and are reported as the mean of the two duplicate determinations from each animal, averaged across subjects.
    Rats[5]
    Male Wistar rats weighting 250-350 are used.The following agents are used: CB1 receptor agonist, Win-55212 (0.3, 1 and 5 mg/kg, i.p. ); CB1 receptor antagonist, AM251 (0.3, 1 and 5 mg/kg, i.p.); endocannabinoid breakdown inhibitor, URB-597 (0.03, 0.1 and 0.3 mg/kg, i.p.) in the study. Physiological saline (0.9% sodium chloride) is used as the vehicle. All drugs are prepared freshly and administered intraperitoneally (i.p.) in a volume of 0.1 mL per 10 g of body weight of the rats. All substances are dissolved in physiological saline and are administrated 30 min before elevated plus-maze test.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    参考文献

    AM251 相关分类

    完整储备液配制表

    * 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，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, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

    可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 1.8010 mL 9.0051 mL 18.0102 mL 45.0256 mL
    5 mM 0.3602 mL 1.8010 mL 3.6020 mL 9.0051 mL
    10 mM 0.1801 mL 0.9005 mL 1.8010 mL 4.5026 mL
    15 mM 0.1201 mL 0.6003 mL 1.2007 mL 3.0017 mL
    20 mM 0.0901 mL 0.4503 mL 0.9005 mL 2.2513 mL
    25 mM 0.0720 mL 0.3602 mL 0.7204 mL 1.8010 mL
    30 mM 0.0600 mL 0.3002 mL 0.6003 mL 1.5009 mL
    40 mM 0.0450 mL 0.2251 mL 0.4503 mL 1.1256 mL
    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    AM251183232-66-8AM 251AM-251Cannabinoid ReceptorInhibitorinhibitorinhibit

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    目录号：
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