Capsazepine

Name: Capsazepine
Brand: MedChemExpress
SKU: HY-15640
Rating: 5.0 (35 reviews)

Cat. No.: HY-15640 Purity: 98.14%: FAQs
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Capsazepine is a synthetic analogue of the sensory neurone excitotoxin, and an antagonist of TRPV1 receptor with an IC₅₀ of 562 nM.

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

Capsazepine Chemical Structure

CAS No. : 138977-28-3

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10 mM * 1 mL in DMSO ready for reconstitution	USD 105	In-stock	Estimated Time of Arrival: December 31
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10 mM * 1 mL in DMSO	USD 105	In-stock	Estimated Time of Arrival: December 31
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Based on 35 publication(s) in Google Scholar

34 Publications Citing Use of MCE Capsazepine

: Capsazepine purchased from MedChemExpress. 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.

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TRPC TRPM TRPV TRPA TRPML

Biological Activity
Protocol
Purity & Documentation
References
Customer Review

Description

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]

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]

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].

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

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].

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

Molecular Weight

376.90

Formula

C₁₉H₂₁ClN₂O₂S

CAS No.

138977-28-3

Appearance

Solid

Color

Off-white to yellow

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvent & Solubility

In Vitro:

DMSO : ≥ 100 mg/mL (265.32 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" 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

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molarity Calculator
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 5 mg/mL (13.27 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 5 mg/mL (13.27 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 5% DMSO 40% PEG300 5% Tween-80 50% Saline
Solubility: ≥ 2.87 mg/mL (7.61 mM); Clear solution
Protocol 4

Add each solvent one by one: 5% DMSO 95% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.87 mg/mL (7.61 mM); Clear solution

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: ≥99.0%

Select Batch:

Data Sheet (278 KB) SDS (393 KB)

COA (247 KB)

Handling Instructions (2659 KB)

References

[1]. Sung B, et al. Capsazepine, a TRPV1 antagonist, sensitizes colorectal cancer cells to apoptosis by TRAIL through ROS-JNK-CHOP-mediated upregulation of death receptors. Free Radic Biol Med. 2012 Nov 15;53(10):1977-87. [Content Brief]

[2]. Santicioli P, et al. Effect of capsazepine on the release of calcitonin gene-related peptide-like immunoreactivity (CGRP-LI) induced by low pH, capsaicin and potassium in rat soleus muscle. Br J Pharmacol. 1993 Oct;110(2):609-12. [Content Brief]

[3]. Cabral LD, et al. The Transient Receptor Potential Vanilloid 1 Antagonist Capsazepine Improves the Impaired Lung Mechanics during Endotoxemia. Basic Clin Pharmacol Toxicol. 2016 Nov;119(5):421-427. [Content Brief]

[4]. Wang J, et al. Anti-inflammatory and retinal protective effects of capsaicin on ischaemia-induced injuries through the release of endogenous somatostatin. Clin Exp Pharmacol Physiol. 2017 Jul;44(7):803-814. [Content Brief]

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.
References	[1]. Sung B, et al. Capsazepine, a TRPV1 antagonist, sensitizes colorectal cancer cells to apoptosis by TRAIL through ROS-JNK-CHOP-mediated upregulation of death receptors. Free Radic Biol Med. 2012 Nov 15;53(10):1977-87. [Content Brief] [2]. Santicioli P, et al. Effect of capsazepine on the release of calcitonin gene-related peptide-like immunoreactivity (CGRP-LI) induced by low pH, capsaicin and potassium in rat soleus muscle. Br J Pharmacol. 1993 Oct;110(2):609-12. [Content Brief] [3]. Cabral LD, et al. The Transient Receptor Potential Vanilloid 1 Antagonist Capsazepine Improves the Impaired Lung Mechanics during Endotoxemia. Basic Clin Pharmacol Toxicol. 2016 Nov;119(5):421-427. [Content Brief] [4]. Wang J, et al. Anti-inflammatory and retinal protective effects of capsaicin on ischaemia-induced injuries through the release of endogenous somatostatin. Clin Exp Pharmacol Physiol. 2017 Jul;44(7):803-814. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	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

Capsazepine Related Classifications

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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:

Capsazepine138977-28-3TRP ChannelApoptosisTransient receptor potential channelsInhibitorinhibitorinhibit

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Capsazepine

Customer Review

Capsazepine Related Antibodies

34 Publications Citing Use of MCE Capsazepine

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References

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Capsazepine Related Antibodies

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Complete Stock Solution Preparation Table

Capsazepine Related Classifications

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