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  2. Membrane Transporter/Ion Channel Neuronal Signaling Apoptosis
  3. TRP Channel Apoptosis
  4. Capsazepine

Capsazepine  (Synonyms: 辣椒平)

目錄號: HY-15640 純度: 98.14%
COA 產(chǎn)品使用指南

Capsazepine是感覺神經(jīng)元興奮毒素的合成類似物，和TRPV1 受體拮抗劑，其中IC50 為562 nM。

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Capsazepine Chemical Structure

Capsazepine Chemical Structure

CAS No. : 138977-28-3

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規(guī)格 價格 是否有貨 數(shù)量
10 mM * 1 mL in DMSO ￥869
In-stock
5 mg ￥493
In-stock
10 mg ￥790
In-stock
50 mg ￥3200
In-stock
100 mg ￥5800
In-stock
200 mg   詢價  
500 mg   詢價  

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Customer Review

MCE 顧客使用本產(chǎn)品發(fā)表的 34 篇科研文獻

WB

    Capsazepine purchased from MCE. Usage Cited in: Food Funct. 2018 Jan 24;9(1):344-354.  [Abstract]

    Capsaicin-induced decrease in the expression of MMP-9 and Twist1 is restored by Capsazepine (CPZ). The protein levels of MMP-9 and Twist1 were determined by western blotting. Actin is used as a loading control.

    查看 TRP Channel 亞型特異性產(chǎn)品:

    • 生物活性

    • 實驗參考方法

    • 純度 & 產(chǎn)品資料

    • 參考文獻

    生物活性

    Capsazepine is a synthetic analogue of the sensory neurone excitotoxin, and an antagonist of TRPV1 receptor with an IC50 of 562 nM.

    IC50 & Target

    TRPV1 receptor[1]
    細胞效力
    (Cellular Effect)
    Cell Line Type Value Description References
    CHO IC50
    > 30000 nM
    Compound: 4
    Antagonist activity at rat TRPV1 expressed in CHO cells assessed as blockade of acid-induced receptor activation by aequorin based assay
    Antagonist activity at rat TRPV1 expressed in CHO cells assessed as blockade of acid-induced receptor activation by aequorin based assay
    		[PMID: 17489570]
    CHO IC50
    > 40000 nM
    Compound: 4
    Antagonist activity at rat TRPV1 expressed in CHO cells assessed as blockade of acid-induced receptor activation by [45Ca2+] uptake assay
    Antagonist activity at rat TRPV1 expressed in CHO cells assessed as blockade of acid-induced receptor activation by [45Ca2+] uptake assay
    		[PMID: 17489570]
    CHO IC50
    0.42 μM
    Compound: Capsazepine
    Inhibition of capsaicin-induced calcium uptake by transient receptor potential vanilloid type 1 expressed in CHO cells
    Inhibition of capsaicin-induced calcium uptake by transient receptor potential vanilloid type 1 expressed in CHO cells
    		[PMID: 15634002]
    CHO IC50
    220 nM
    Compound: 4
    Antagonist activity at rat TRPV1 expressed in CHO cells assessed as blockade of capsaicin-induced receptor activation by aequorin based assay
    Antagonist activity at rat TRPV1 expressed in CHO cells assessed as blockade of capsaicin-induced receptor activation by aequorin based assay
    		[PMID: 17489570]
    CHO IC50
    320 nM
    Compound: 4
    Antagonist activity at human TRPV1 expressed in CHO cells assessed as blockade of acid-induced receptor activation by aequorin based assay
    Antagonist activity at human TRPV1 expressed in CHO cells assessed as blockade of acid-induced receptor activation by aequorin based assay
    		[PMID: 17489570]
    CHO IC50
    39 nM
    Compound: 4
    Antagonist activity at human TRPV1 expressed in CHO cells assessed as blockade of capsaicin-induced receptor activation by aequorin based assay
    Antagonist activity at human TRPV1 expressed in CHO cells assessed as blockade of capsaicin-induced receptor activation by aequorin based assay
    		[PMID: 17489570]
    CHO IC50
    53 nM
    Compound: 4
    Antagonist activity at human TRPV1 expressed in CHO cells assessed as blockade of capsaicin-induced receptor activation by [45Ca2+] uptake assay
    Antagonist activity at human TRPV1 expressed in CHO cells assessed as blockade of capsaicin-induced receptor activation by [45Ca2+] uptake assay
    		[PMID: 17489570]
    CHO IC50
    69 nM
    Compound: 4
    Antagonist activity at human TRPV1 expressed in CHO cells assessed as blockade of acid-induced receptor activation by [45Ca2+] uptake assay
    Antagonist activity at human TRPV1 expressed in CHO cells assessed as blockade of acid-induced receptor activation by [45Ca2+] uptake assay
    		[PMID: 17489570]
    CHO IC50
    887 nM
    Compound: 4
    Antagonist activity at rat TRPV1 expressed in CHO cells assessed as blockade of capsaicin-induced receptor activation by [45Ca2+] uptake assay
    Antagonist activity at rat TRPV1 expressed in CHO cells assessed as blockade of capsaicin-induced receptor activation by [45Ca2+] uptake assay
    		[PMID: 17489570]
    HEK-293T IC50
    0.15 μM
    Compound: CPZ
    Antagonist activity at human brain TRPV1 expressed in HEK293T cells assessed as inhibition of CAP-induced intracellular Ca2+ influx by fluorescence-based assay
    Antagonist activity at human brain TRPV1 expressed in HEK293T cells assessed as inhibition of CAP-induced intracellular Ca2+ influx by fluorescence-based assay
    		[PMID: 24484240]
    HeLa IC50
    30 μM
    Compound: CPZ
    Antiproliferative activity against human HeLa cells after 24 hrs by cell titer 96 aqueous non-radioactive cell proliferation assay
    Antiproliferative activity against human HeLa cells after 24 hrs by cell titer 96 aqueous non-radioactive cell proliferation assay
    		[PMID: 30528162]
    體外研究
    (In Vitro)

    Capsazepine (50 μM) optimally enhances the upregulation of (death receptors) DRs without affecting cell viability HCT116 cells. Capsazepine (30-50 μM) induces ROS generation and ROS mediate Capsazepine-induced DR5 upregulation in HCT116 cells[1]. Capsazepine (1-100 μM, 45 min preincubation) inhibits the evoked CGRP-LI release. Capsazepine (3-100 μM) prevents low pH- and capsaicin-induced CGRP-LI release from rat soleus muscle at concentrations which do not affect the release evoked by KCl. Capsazepine (3-100 μM, without 10 μM) produces a nonspecific inhibitory effect on CGRP-LI release from peripheral endings of the capsaicin-sensitive primary afferent neurone[2].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    體內(nèi)研究
    (In Vivo)

    Capsazepine (15 mg/kg, s.c.) prevents the increase in respiratory system resistance and decreases the increase in tissue damping during endotoxemia. Capsazepine attenuates lung injury evidenced by reduction on collapsed area of the lung parenchyma induced by LPS[3].

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

    376.90

    Formula

    C19H21ClN2O2S
    CAS 號
    性狀

    固體

    顏色

    Off-white to yellow

    中文名稱

    辣椒平
    運輸條件

    Room temperature in continental US; may vary elsewhere.
    儲存方式
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    溶解性數(shù)據(jù)
    細胞實驗： 

    DMSO 中的溶解度 : ≥ 100 mg/mL (265.32 mM; 吸濕的 DMSO 對產(chǎn)品的溶解度有顯著影響，請使用新開封的 DMSO)

    * "≥" means soluble, but saturation unknown.

    配制儲備液
    濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg
    1 mM 2.6532 mL 13.2661 mL 26.5322 mL
    5 mM 0.5306 mL 2.6532 mL 5.3064 mL
    查看完整儲備液配制表

    * 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復凍融造成的產(chǎn)品失效。
    儲備液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C儲存時，請在2年內(nèi)使用， -20°C儲存時，請在1年內(nèi)使用。

    • 摩爾計算器

    • 稀釋計算器

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

    質(zhì)量
    =
    濃度
    ×
    體積
    ×
    分子量 *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    濃度 (start)

    C1

    ×
    體積 (start)

    V1

    =
    濃度 (final)

    C2

    ×
    體積 (final)

    V2

    動物實驗：

    請根據(jù)您的 實驗動物和給藥方式 選擇適當?shù)娜芙夥桨浮?

    以下溶解方案都請先按照 In Vitro 方式配制澄清的儲備液，再依次添加助溶劑：
    ——為保證實驗結(jié)果的可靠性，澄清的儲備液可以根據(jù)儲存條件，適當保存；體內(nèi)實驗的工作液，建議您現(xiàn)用現(xiàn)配，當天使用；
    以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的方式助溶

    • 方案 一

      請依序添加每種溶劑： 10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 5 mg/mL (13.27 mM); 澄清溶液

      此方案可獲得 ≥ 5 mg/mL（飽和度未知）的澄清溶液。

      以 1 mL 工作液為例，取 100 μL 50.0 mg/mL 的澄清 DMSO 儲備液加到 400 μL PEG300 中，混合均勻；再向上述體系中加入 50 μL Tween-80，混合均勻；然后再繼續(xù)加入 450 μL 生理鹽水 定容至 1 mL。

      生理鹽水的配制：將 0.9 g 氯化鈉，溶解于 ddH?O 并定容至 100 mL，可以得到澄清透明的生理鹽水溶液。
    • 方案 二

      請依序添加每種溶劑： 10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 5 mg/mL (13.27 mM); 澄清溶液

      此方案可獲得 ≥ 5 mg/mL（飽和度未知）的澄清溶液。

      以 1 mL 工作液為例，取 100 μL 50.0 mg/mL 的澄清 DMSO 儲備液加到 900 μL 20% 的 SBE-β-CD 生理鹽水水溶液 中，混合均勻。

      2 g SBE-β-CD（磺丁基醚 β-環(huán)糊精）粉末定容于 10 mL 的生理鹽水中，完全溶解至澄清透明。
    動物溶解方案計算器
    請輸入動物實驗的基本信息：

    給藥劑量

    mg/kg

    動物的平均體重

    g

    每只動物的給藥體積

    μL

    動物數(shù)量

    只
    由于實驗過程有損耗，建議您多配一只動物的量
    請輸入您的動物體內(nèi)配方組成：
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    如果您的動物是免疫缺陷鼠或者體弱鼠，建議 DMSO 中的在最后工作液體系中的占比盡量不超過 2%。
    方案所需 助溶劑 包括：DMSO， ，均可在 MCE 網(wǎng)站選購。 ，Tween 80，均可在 MCE 網(wǎng)站選購。
    計算結(jié)果
    工作液所需濃度 : mg/mL
    儲備液配制方法 : mg 藥物溶于 μL  DMSO（母液濃度為 mg/mL）。
    您所需的儲備液濃度超過該產(chǎn)品的實測溶解度，以下方案僅供參考，如有需要，請與 MCE 中國技術(shù)支持聯(lián)系。
    動物實驗體內(nèi)工作液的配制方法 : 取 μL DMSO 儲備液，加入 μL 。 μL ，混合均勻至澄清，再加 μL Tween 80，混合均勻至澄清，再加 μL 生理鹽水。
    連續(xù)給藥周期超過半月以上，請謹慎選擇該方案。
    請確保第一步儲備液溶解至澄清狀態(tài)，從左到右依次添加助溶劑。您可采用超聲加熱 （超聲清洗儀，建議頻次 20-40 kHz），渦旋吹打等方式輔助溶解。
    純度 & 產(chǎn)品資料

    純度: ≥99.0%

    參考文獻
    Cell Assay
    [1]

    To assay intracellular ROS, HCT116 cells are preincubated with 20 μM dichlorofluorescein diacetate (DCF DA) for 15 min at 37°C and then treated with Capsazepine. After 1 h of incubation, the increase in fluorescence resulting from the oxidation of DCF DA to DCF is measured by flow cytometry. The mean fluorescence intensity at 530 nm is calculated for at least 10,000 cells at a flow rate of 250-300 cells/s.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [3]

    To verify the role of TRPV1 on lung mechanics during LPS-induced ALI, the animals (n = 10 per group) are pre-treated with vehicle or Capsazepine (15 mg/kg; s.c.), then receive saline or LPS (5 mg/kg, i.p.) after 10 min. Thus, the mice are randomly divided into four groups with 10 mice in each group: (i) control (vehicle + saline), (ii) Capsazepine + saline, (iii) vehicle + LPS and (iv) Capsazepine + LPS. After a 24-hr treatment with saline or LPS, the mice are anaesthetized and paralysed and lung mechanics function is evaluated. Afterwards, the lungs are removed for histology.

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

    完整儲備液配制表

    * 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復凍融造成的產(chǎn)品失效。
    儲備液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C儲存時，請在2年內(nèi)使用， -20°C儲存時，請在1年內(nèi)使用。

    可選溶劑 濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.6532 mL 13.2661 mL 26.5322 mL 66.3306 mL
    5 mM 0.5306 mL 2.6532 mL 5.3064 mL 13.2661 mL
    10 mM 0.2653 mL 1.3266 mL 2.6532 mL 6.6331 mL
    15 mM 0.1769 mL 0.8844 mL 1.7688 mL 4.4220 mL
    20 mM 0.1327 mL 0.6633 mL 1.3266 mL 3.3165 mL
    25 mM 0.1061 mL 0.5306 mL 1.0613 mL 2.6532 mL
    30 mM 0.0884 mL 0.4422 mL 0.8844 mL 2.2110 mL
    40 mM 0.0663 mL 0.3317 mL 0.6633 mL 1.6583 mL
    50 mM 0.0531 mL 0.2653 mL 0.5306 mL 1.3266 mL
    60 mM 0.0442 mL 0.2211 mL 0.4422 mL 1.1055 mL
    80 mM 0.0332 mL 0.1658 mL 0.3317 mL 0.8291 mL
    100 mM 0.0265 mL 0.1327 mL 0.2653 mL 0.6633 mL
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    產(chǎn)品名稱：
    Capsazepine
    目錄號：
    HY-15640
    需求量：