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

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 99 In-stock
10 mg USD 90 In-stock
50 mg USD 390 In-stock
100 mg USD 580 In-stock
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

  • 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].

References
Preparing Stock Solutions
Concentration Volume 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.
Cell Assay
[1]

Capsazepine is dissolved in DMSO (50 mM).

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]

Capsazepine is dissolved in a solution containing 0.9% NaCl, Tween and DMSO at a ratio of 8:1:1.

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

376.9

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

Solvent & Solubility

DMSO: ≥ 50 mg/mL

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

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

References

Purity: >99.0%

Inquiry Online

Your information is safe with us. * Required Fields.

Product name

 

Salutation

Applicant name *

 

Email address *

Phone number *

 

Organization name *

Country *

 

Requested quantity *

Remarks

Bulk Inquiry

Inquiry Information

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