1. Membrane Transporter/Ion Channel
  2. TRP Channel

Capsazepine 

Cat. No.: HY-15640 Purity: >99.0%
Handling Instructions

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

For research use only. We do not sell to patients.

Capsazepine Chemical Structure

Capsazepine Chemical Structure

CAS No. : 138977-28-3

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10 mM * 1 mL in DMSO USD 99 In-stock
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Estimated Time of Arrival: December 31
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    Capsazepine purchased from MCE. Usage Cited in: Clin Exp Pharmacol Physiol. 2017 Jul;44(7):803-814.

    Western blot analysis showing that the CAP (0.5 mg/kg) injection inhibits the increase of p65 expression and phosphorylation at 24 h after I/R injury. The effects of Capsaicin (CAP) are prevented during the pretreatment of the SST depletor Cysteamine (Cys).

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

    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.
    • Biological Activity

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References

    Description

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

    IC50 & Target

    TRPV1 receptor[1]

    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].

    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].

    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 50 mg/mL (132.66 mM)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 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
    10 mM 0.2653 mL 1.3266 mL 2.6532 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      Capsazepine (CPZ) is dissolved in a vehicle containing Tween 80, ethanol and saline, with a proportion of 1:1:8[4].

    References
    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 with pancuronium bromide 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.

    References
    Molecular Weight

    376.90

    Formula

    C₁₉H₂₁ClN₂O₂S

    CAS No.

    138977-28-3

    SMILES

    S=C(N1CCCC2=CC(O)=C(O)C=C2C1)NCCC3=CC=C(Cl)C=C3

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Shipping

    Room temperature in continental US; may vary elsewhere

    Purity: >99.0%

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    Product Name:
    Capsazepine
    Cat. No.:
    HY-15640
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    Capsazepine

    Cat. No.: HY-15640