1. GPCR/G Protein Neuronal Signaling
  2. CGRP Receptor
  3. Olcegepant

Olcegepant  (Synonyms: BIBN-4096; BIBN 4096BS)

目录号: HY-10095 纯度: 99.83%
Data Sheet SDS COA 产品使用指南 技术支持

Olcegepant (BIBN-4096) 是有效和选择性的降钙素基因相关肽1 (CGRP1) 受体 拮抗剂,IC50Ki 分别为0.03 nM,14.4 pM。

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Olcegepant Chemical Structure

Olcegepant Chemical Structure

CAS No. : 204697-65-4

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10 mM * 1 mL in DMSO ¥2793
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Customer Review

Other Forms of Olcegepant:

MCE 顾客使用本产品发表的 35 篇科研文献

WB

    Olcegepant purchased from MCE. Usage Cited in: Cell Physiol Biochem. 2017;41(4):1457-1467.  [Abstract]

    In terms of the p-ERK1/2 expressions, there is no significant difference between the model and the NC groups, however, rats in the model and NC groups show substantially higher p-ERK1/2 levels than those in the sham surgery group (P < 0.05). The level of p-ERK1/2 in rats in the NPY inhibitors group and CGRP inhibitors group are significantly lower compared with the model group (P < 0.05).
    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    Olcegepant (BIBN-4096) is a potent and selective non-peptide antagonist of the calcitonin gene-related peptide 1 (CGRP1) receptor with IC50 of 0.03 nM and Ki of 14.4 pM for human CGRP[1][2].

    IC50 & Target

    IC50: 0.03 nM (CGRP1)[1]
    Ki: 14.4 pM (hCGRP)[2]

    细胞效力
    (Cellular Effect)
    Cell Line Type Value Description References
    SK-N-MC IC50
    0.004 μM
    Compound: BIBN4096
    Antagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assay
    Antagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assay
    [PMID: 24405707]
    SK-N-MC EC50
    0.026 nM
    Compound: 1, BIBN-4096BS
    Antagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of alpha-CGRP-induced c-AMP formation after 15 mins by radioimmunoassay
    Antagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of alpha-CGRP-induced c-AMP formation after 15 mins by radioimmunoassay
    [PMID: 24794104]
    体外研究
    (In Vitro)

    Olcegepant 对人类 CGRP 受体的亲和力比内源性配体 CGRP 更高,与肽类拮抗剂 CGRP8-37 相比,亲和力高 150 倍。Olcegepant 可逆转 CGRP 介导的人类脑血管扩张,并抑制偏头痛病理生理替代动物模型中的神经源性血管扩张[1]。Olcegepant (BIBN4096BS) 对灵长类 CGRP 受体具有极强的效力,对人类 CGRP 受体的亲和力 (Ki) 为 14.4±6.3 (n=4) pM[2]。多项证据表明,降钙素基因相关肽 (CGRP) 受体拮抗剂可作为一种新型的偏头痛中止疗法。 Olcegepant (BIBN4096BS) 对 SK-N-MC 细胞中存在的 CGRP 受体表现出竞争性拮抗作用。使用灵敏的肌动图技术研究了分离的人类脑动脉、冠状动脉和网膜动脉。CGRP 诱导浓度依赖性松弛,而 Olcegepant 以竞争性方式拮抗该松弛[3]

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

    体内研究
    (In Vivo)

    剂量在 1 至 30 μg/kg(静脉注射)之间的 Olcegepant (BIBN4096BS) 可抑制三叉神经节刺激释放的 CGRP 对狨猴面部血流的影响[2]。预先用 Olcegepant (900 μg/kg) 治疗可抑制辣椒素诱导的整个脊髓三叉神经核中 Fos 的表达 57%。相反,三叉神经节中磷酸化的细胞外信号调节激酶的表达不会因 Olcegepant 预先治疗而改变[4]。Olcegepant(0.3 至 0.9 mg/kg,静脉注射)可显著减轻 CCI-ION 大鼠的机械性异常性疼痛。 Olcegepant(0.6 mg/kg,静脉注射)显著减少三叉神经脊核中 c-Fos 免疫标记细胞的数量和 ATF3 转录本(神经元损伤标志物)的上调,但没有减少 CCI-ION 大鼠三叉神经节中白细胞介素 6 的数量[5]

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

    Clinical Trial
    NCT NumberSponsorConditionStart DatePhase
    NCT02198352Boehringer Ingelheim
    Healthy
    June 1998Phase 1
    NCT02194322Boehringer Ingelheim
    Healthy
    November 2001Phase 1
    NCT02194348Boehringer Ingelheim
    Healthy
    February 2000Phase 1
    分子量

    869.65

    Formula

    C38H47Br2N9O5

    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 6 months
    -20°C 1 month
    溶解性数据
    细胞实验: 

    DMSO 中的溶解度 : ≥ 50 mg/mL (57.49 mM; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

    1M HCl 中的溶解度 : 50 mg/mL (57.49 mM; 超声助溶; 酸性条件溶解 (HCL 调节,pH≈1))

    * "≥" means soluble, but saturation unknown.

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 1.1499 mL 5.7494 mL 11.4989 mL
    5 mM 0.2300 mL 1.1499 mL 2.2998 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, 6 months; -20°C, 1 month。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

    • 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 (2.87 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。

      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 (2.87 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。

      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。

    扫码获得
    动物溶解方案

    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

    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 PEG300/PEG400Tween 80,均可在 MCE 网站选购。
    纯度 & 产品资料

    纯度: 99.83%

    参考文献
    Kinase Assay
    [2]

    125I-hCGRP is used as the radioligand. The incubation buffer contained (in mM): Tris 50, NaCl 150, MgCl25 and EDTA 1, (ethylene diamine tetra-acetic acid) pH 7.4. Membrane homogenates are incubated for 180 min at room temperature with 50 pM 125I -hCGRP and increasing concentrations of Olcegepant (BIBN4096BS). The incubation is terminated by filtration through GF/B glass fibre filters using a cell harvester. The protein-bound radioactivity is determined in a gamma counter. The nonspecific binding is defined as radioactivity bound in the presence of 1 μM CGRP. The IC50 values are obtained by non-linear regression analysis on the basis of a one binding site model [2].

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

    Cell Assay
    [3]

    Cells are washed with phosphate-buffered saline then pre-incubated with 300 μM isobutylmethylxanthine in serum-free MEM for 30 min at 37 °C α-CGRP-(S-37) or Olcegepant (BIBN4096BS) is added and the cells are incubated for 10 min before the addition of CGRP. The incubation is continued for another 15 min, then the cells are washed with PBS and processed for cAMP determination. Maximal stimulation over basal is defined by using 100 nM CGRP. Dose–response curves are generated by using Prism[3].

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

    Animal Administration
    [5]

    Rats are treated acutely with Olcegepant (0.3, 0.6, and 0.9 mg/kg, intravenously [i.v.] in a tail vein), GR-85548A (0.1 and 0.3 mg/kg subcutaneously [s.c.]), or their respective vehicle. For combined treatment, Olcegepant (0.3 mg/kg, i.v.) is administered 30 minutes before GR-85548A (0.1 mg/kg, s.c.). The doses and routes of administration are based on previous reports.
    For subchronic treatment, CCI-ION and sham-operated rats are injected twice per day for 4 days (at 10 am and 6 pm) with Olcegepant (0.6 mg/kg, i.v.) or its vehicle, starting on the 15th day after ligature. A further injection of Olcegepant (0.6 mg/kg, i.v.) or vehicle is performed at 10 am the subsequent day (19th day after ligature), just before von Frey filament testing.

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

    参考文献

    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, 6 months; -20°C, 1 month。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

    可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
    DMSO / 1M HCl 1 mM 1.1499 mL 5.7494 mL 11.4989 mL 28.7472 mL
    5 mM 0.2300 mL 1.1499 mL 2.2998 mL 5.7494 mL
    10 mM 0.1150 mL 0.5749 mL 1.1499 mL 2.8747 mL
    15 mM 0.0767 mL 0.3833 mL 0.7666 mL 1.9165 mL
    20 mM 0.0575 mL 0.2875 mL 0.5749 mL 1.4374 mL
    25 mM 0.0460 mL 0.2300 mL 0.4600 mL 1.1499 mL
    30 mM 0.0383 mL 0.1916 mL 0.3833 mL 0.9582 mL
    40 mM 0.0287 mL 0.1437 mL 0.2875 mL 0.7187 mL
    50 mM 0.0230 mL 0.1150 mL 0.2300 mL 0.5749 mL

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