Capsazepine

Catalog No.S8137 Batch:S813703

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Technical Data

Formula

C19H21ClN2O2S
Molecular Weight 376.90 CAS No. 138977-28-3
Solubility (25°C)* In vitro DMSO 75 mg/mL (198.99 mM)
Ethanol 38 mg/mL (100.82 mM)
Water Insoluble
In vivo (Add solvents to the product individually and in order)
Clear solution
5%DMSO Corn oil
1.25mg/ml Taking the 1 mL working solution as an example, add 50 μL of 25 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description Capsazepine acts as a competitive antagonist of capsaicin and a transient receptor potential vanilloid type 1(TRPV1) antagonist. If you want to do cell experiments, please select batch 01.
Targets
TRPV1 [2] Na,K-ATPase [3]
12 μM(EC50)
In vitro

Capsazepine(CPZ) at a concentration of 94.2 µg/ml (IC50 concentration of capsazepine) exhibits a statistically significant inhibition of osteoclast growth and proliferation[2]. Capsazepine converts the NKA into Na-ATPase. CPZ inhibits K+-dependent activity but allows Na-ATPase associated with Na+ transport. CPZ has no effect on Na-ATPase measured in the absence of K+. CPZ also inhibits para-nitrophenyl phosphatase activity, albeit with a lower affinity. CPZ strongly reduces the steady-state EP level and the Na+ affinity for phosphorylation decreased 3-fold after CPZ treatment. In summary, CPZ blocks an Na+/K+ cycle in the NKA but leaves an Na+ cycle intact, reducing the transport stoichiometry of the pump[3]. Capsazepine inhibits osteoclast formation and bone resorption in a dose dependent manner in bone marrow-osteoblast co-cultures and RANKL generated osteoclast cultures. Capsazepine also suppresses RANKL induced IκB and ERK1/2 phosphorylation and causes apoptosis of mature osteoclasts and also inhibits alkaline phosphatase activity and bone nodule formation in calvarial osteoblast cultures[4].
In vivo

Capsazepine pre-treatment prevents the increase in respiratory system resistance and decreases the increase in tissue damping during endotoxemia. Capsazepine also attenuates lung injury by a reduction in the collapsed area of the lung parenchyma induced by lipopolysaccharide (LPS).

Protocol (from reference)

Cell Assay:

[2]
  • Cell lines

    Murine macrophage cell line RAW 264.7

  • Concentrations

    94.2 µg/ml

  • Incubation Time

    72 h

  • Method

    The cells are plated and treated with different concentrations of the test compounds and allowed to proliferate for 72 h. After 72 h of proliferation the cells are fixed in 10% formalin saline (50 μl/well) for 30 min. Then the cells are stained with crystal violet (0.05% w/v) for 30 min. The wells are then washed thoroughly with distilled water to remove any unbound dye and destained with Sorenson's buffer (0.1 M sodium citrate in 50% ethanol, pH 4.2). The absorbance of the extracted stain is measured at 540 nm.

Selleck's Capsazepine has been cited by 8 publications

Investigation of the anti-inflammatory, anti-pruritic, and analgesic effects of sophocarpine inhibiting TRP channels in a mouse model of inflammatory itch and pain [ J Ethnopharmacol, 2024, 337(Pt 2):118882] PubMed: 39366497
Mechanical manipulation of cancer cell tumorigenicity via heat shock protein signaling [ Sci Adv, 2023, 9(27):eadg9593] PubMed: 37418519
Microglial Piezo1 senses Aβ fibril stiffness to restrict Alzheimer's disease [ Neuron, 2022, S0896-6273(22)00954-0] PubMed: 36368316
The effect of Ma-Xin-Gan-Shi decoction on asthma exacerbated by respiratory syncytial virus through regulating TRPV1 channel [ J Ethnopharmacol, 2022, 291:115157] PubMed: 35247474
Generation of GCaMP6s-Expressing Zebrafish to Monitor Spatiotemporal Dynamics of Calcium Signaling Elicited by Heat Stress [ Int J Mol Sci, 2021, 22(11)5551] PubMed: 34074030
Evodiamine induces ROS-Dependent cytotoxicity in human gastric cancer cells via TRPV1/Ca2+ pathway [ Chem Biol Interact, 2021, 351:109756] PubMed: 34808100
Ca2+-permeable TRPV1 pain receptor knockout rescues memory deficits and reduces amyloid-β and tau in a mouse model of Alzheimer's disease. [ Hum Mol Genet, 2020, 29(2):228-237] PubMed: 31814000
Dual-targeting Rutaecarpine-NO donor hybrids as novel anti-hypertensive agents by promoting release of CGRP [Ma J Eur J Med Chem, 2019, 168:146-153] PubMed: 30818175

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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