Capsazepine
Based on 64 publication(s) in Google Scholar
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.
- Purity: 99.05%
- CAS No.: 138977-28-3
- Formula: C19H21ClN2O2S
- Molecular Weight:376.90
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Publications Citing Use of MedChemExpress (MCE) Capsazepine
More- Signal Transduct Target Ther. 2021 Jan 25;6(1):29. [Abstract]
- Nature. 2026 Feb;650(8103):951-960. [Abstract]
- Autophagy. 2021 Nov;17(11):3592-3606. [Abstract]
- J Nanobiotechnology. 2025 Sep 3;23(1):604. [Abstract]
- Theranostics. 2020 Jun 24;10(17):7906-7920. [Abstract]
- Adv Sci (Weinh). 2024 Dec;11(47):e2405705. [Abstract]
- Cell Death Dis. 2021 Dec 14;12(12):1159. [Abstract]
- Cell Commun Signal. 2023 Dec 21;21(1):364. [Abstract]
- Phytomedicine. 2026 Aug:158:158406. [Abstract]
- Phytomedicine. 2026 Jul:156:158269. [Abstract]
- Burns Trauma. 2026 Jan 16.
- J Hazard Mater. 2026 Jul 1:512:142315. [Abstract]
- ACS Environ Au. 2025 Aug 5;5(6):573-582. [Abstract]
- Cell Rep. 2023 Dec 2;42(12):113522. [Abstract]
- Curr Biol. 2021 Jul 26;31(14):2995-3003.e4. [Abstract]
- Curr Biol. 2019 Aug 19;29(16):2597-2603.e4. [Abstract]
- Environ Pollut. 2024 Jul 15:353:124127. [Abstract]
- J Agric Food Chem. 2025 Mar 5;73(9):5300-5310. [Abstract]
- J Environ Sci. 2026 Jun 25.
- Life Sci. 2020 May 15:249:117472. [Abstract]
- Food Funct. 2018 Jan 24;9(1):344-354. [Abstract]
- Cells. 2026 Jan;15(13):1142.
- J Mol Cell Biol. 2022 Jan 21;13(11):791-807. [Abstract]
- Commun Biol. 2025 May 10;8(1):724. [Abstract]
- Commun Biol. 2023 Aug 15;6(1):848. [Abstract]
- eFood. 2026 Mar 1;7(2):e70136.
- Int Immunopharmacol. 2025 May 16:155:114657. [Abstract]
- Front Pharmacol. 2021 Dec 1:12:763089. [Abstract]
- ACS Omega. 2025 Aug 21;10(34):39192-39202. [Abstract]
- Nanoscale. 2025 Feb 6;17(6):3288-3305. [Abstract]
- Mol Med Rep. 2024 Dec;30(6):213. [Abstract]
- Sci Rep. 2026 Feb 9;16(1):7851. [Abstract]
- Cell Calcium. 2026 Mar:134:103122. [Abstract]
- Am J Pathol. 2023 May;193(5):548-557. [Abstract]
- J Cell Mol Med. 2026 Apr;30(8):e71157. [Abstract]
- Anesth Analg. 2024 May 1;138(5):1107-1119. [Abstract]
- Cell Signal. 2020 Nov:75:109733. [Abstract]
- J Inflamm Res. 2025 Jun 17:18:7907-7919. [Abstract]
- J Neurochem. 2025 Jan;169(1):e16281. [Abstract]
- J Inflamm Res. 2024 Jul 2:17:4257-4275. [Abstract]
- iScience. 2026 Jun 19;29(6).
- FASEB J. 2025 May 31;39(10):e70657. [Abstract]
- FASEB J. 2025 Jan 15;39(1):e70304. [Abstract]
- Microbiol Spectr. 2022 Dec 21;10(6):e0241022. [Abstract]
- J Biol Chem. 2020 Jul 10;295(28):9641-9649. [Abstract]
- J Photochem Photobiol B. 2019 Aug:197:111534. [Abstract]
- J Endod. 2021 Sep;47(9):1409-1416. [Abstract]
- Biochim Biophys Acta Mol Cell Biol Lipids. 2026 Jan;1871(1):159704. [Abstract]
- Mol Pain. 2025 Nov 26:17448069251392037. [Abstract]
- Mol Pain. 2024 Jan-Dec:20:17448069241272149. [Abstract]
- Integr Zool. 2025 Jul;20(4):800-804. [Abstract]
- Front Oncol. 2022 Mar 25;12:773654. [Abstract]
- Cryobiology. 2023 Dec:113:104569. [Abstract]
- Am J Physiol Regul Integr Comp Physiol. 2019 Oct 1;317(4):R576-R587. [Abstract]
- Biochem Biophys Res Commun. 2019 Aug 20;516(2):365-372. [Abstract]
- Clin Exp Pharmacol Physiol. 2017 Jul;44(7):803-814. [Abstract]
- Exp Ther Med. 2023 May 15;26(1):318. [Abstract]
- University of Pennsylvania. 2026.
- Res Sq. 2025 Oct 8.
- bioRxiv. 2025 March 10.
- Sci Total Environ. 2024 Feb 20:912:169613. [Abstract]
- Oxid Med Cell Longev. 2022 Aug 27:2022:1544244. [Abstract]
- Research Square Print. 2022 Jun.
- Biomed Pharmacother. 2019 Oct:118:109308. [Abstract]
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Biological Activity
TRPV1 receptor[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO | IC50 |
0.42 μM
Compound: Capsazepine
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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
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[PMID: 15634002] |
| CHO | IC50 |
220 nM
Compound: 4
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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
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[PMID: 17489570] |
| CHO | IC50 |
320 nM
Compound: 4
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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
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[PMID: 17489570] |
| CHO | IC50 |
39 nM
Compound: 4
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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
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[PMID: 17489570] |
| CHO | IC50 |
53 nM
Compound: 4
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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
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[PMID: 17489570] |
| CHO | IC50 |
69 nM
Compound: 4
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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
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[PMID: 17489570] |
| CHO | IC50 |
887 nM
Compound: 4
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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
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[PMID: 17489570] |
| CHO | IC50 |
>30000 nM
Compound: 4
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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
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[PMID: 17489570] |
| CHO | IC50 |
>40000 nM
Compound: 4
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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
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[PMID: 17489570] |
| DU-145 | IC50 |
54 μM
Compound: 17
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Antiproliferative activity against human DU-145 cells assessed as inhibition of cell growth
Antiproliferative activity against human DU-145 cells assessed as inhibition of cell growth
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[PMID: 37000154] |
| HEK293 | IC50 |
58 nM
Compound: capsazepine (CPZ)
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Vanilloid receptor subtype 1 antagonist activity based on its ability to block capsaicin-induced (CAP) activation of the rat VR1 channel in a HEK293 cell line
Vanilloid receptor subtype 1 antagonist activity based on its ability to block capsaicin-induced (CAP) activation of the rat VR1 channel in a HEK293 cell line
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[PMID: 14505681] |
| HEK293 | IC50 |
100 nM
Compound: CPZ (capsazepine)
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Functional antagonistic activity against human vanilloid receptor subtype 1 in HEK293 cell membranes was determined as inhibition of agonist-induced increases in intracellular [Ca2+] levels
Functional antagonistic activity against human vanilloid receptor subtype 1 in HEK293 cell membranes was determined as inhibition of agonist-induced increases in intracellular [Ca2+] levels
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[PMID: 14698197] |
| HEK293 | IC50 |
100 nM
Compound: Capsazepine
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Antagonistic activity towards human vanilloid receptor subtype 1 expressed in HEK293 cell membrane, as inhibition of agonist-induced intracellular [Ca2+] levels.
Antagonistic activity towards human vanilloid receptor subtype 1 expressed in HEK293 cell membrane, as inhibition of agonist-induced intracellular [Ca2+] levels.
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[PMID: 15149643] |
| HEK293 | IC50 |
56.2 nM
Compound: 3
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Inhibition of 100 nM capsaicin effect on intracellular [Ca2+] concentration in HEK293 cells expressing human TRPV1
Inhibition of 100 nM capsaicin effect on intracellular [Ca2+] concentration in HEK293 cells expressing human TRPV1
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[PMID: 16000002] |
| HEK-293T | IC50 |
0.15 μM
Compound: CPZ
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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
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[PMID: 24484240] |
| HeLa | IC50 |
30 μM
Compound: CPZ
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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
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[PMID: 30528162] |
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 138977-28-3
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Appearance Solid
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Molecular Weight 376.90
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Formula C19H21ClN2O2S
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Color Off-white to yellow
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SMILES
S=C(N1CCCC2=CC(O)=C(O)C=C2C1)NCCC3=CC=C(Cl)C=C3
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (64)
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Journal Impact Factor
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Most Recent
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Signal Transduct Target Ther
2021 Jan 25;6(1):29. PMID: 33487631
Capsazepine purchased from MedChemExpress. Usage Cited in: Signal Transduct Target Ther. 2021 Jan 25;6(1):29. [Abstract]
Capsazepine (CPZ) (10 μM, 1 h) notably inhibited NM-stimulated Ca2+ influx and CaMKKβ activation.
Capsazepine purchased from MedChemExpress. Usage Cited in: Signal Transduct Target Ther. 2021 Jan 25;6(1):29. [Abstract]
Capsazepine (CPZ) pretreatment increased ROS levels. DCFH-DA fluorescence intensity was measured by a ZEISS LSM 780 confocal laser scanning microscope.
Capsazepine purchased from MedChemExpress. Usage Cited in: Signal Transduct Target Ther. 2021 Jan 25;6(1):29. [Abstract]
Capsazepine (CPZ) (5 mg/kg, i.p.) treatment abolished the effect of NM on the TRPV1 signaling pathway thereby attenuating NM-induced autophagy, which, subsequently, ameliorated NM-caused skin injury by H&E staining.
Capsazepine purchased from MedChemExpress. Usage Cited in: Signal Transduct Target Ther. 2021 Jan 25;6(1):29. [Abstract]
Capsazepine (CPZ) (5 mg/kg, i.p.) treatment abolished the effect of NM on the TRPV1 signaling pathway thereby attenuating NM-induced autophagy. The expression of COX2 and MMP9 was measured by western blotting.
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Nature
2026 Feb;650(8103):951-960. PMID: 41501451 -
Autophagy
Cannabidiol inhibits human glioma by induction of lethal mitophagy through activating TRPV4. [Abstract]2021 Nov;17(11):3592-3606. PMID: 33629929 -
J Nanobiotechnology
Separable cryo-microneedle patches delivery with capsaicin integrated mesoporous dopamine for obesity treatment. [Abstract]2025 Sep 3;23(1):604. PMID: 40903781 -
Theranostics
Therapeutic potential of targeting MKK3-p38 axis with Capsaicin for Nasopharyngeal Carcinoma. [Abstract]2020 Jun 24;10(17):7906-7920. PMID: 32685028 -
Adv Sci (Weinh)
Piezo1 Regulates Stiffness-Dependent DRG Axon Regeneration via Modifying Cytoskeletal Dynamics. [Abstract]2024 Dec;11(47):e2405705. PMID: 39514408 -
Cell Death Dis
2021 Dec 14;12(12):1159. PMID: 34907173
Capsazepine purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2021 Dec 14;12(12):1159. [Abstract]
IL-1β secretion was obviously blocked by Capsazepine (CPZ) (10 μM, 1 h) measured using ELISA method.
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Cell Commun Signal
Capsaicin orchestrates metastasis in gastric cancer via modulating expression of TRPV1 channels and driving gut microbiota disorder. [Abstract]2023 Dec 21;21(1):364. PMID: 38129926 -
Phytomedicine
Bioactive compound emodin from clinical formula Zhi-Lou-Xun-Xi decoction exerts rapid analgesic effects by targeting TRPV1. [Abstract]2026 Aug:158:158406. PMID: 42275875 -
Phytomedicine
Dietary capsaicin attenuates aortic dissection by inhibiting M1 macrophage polarisation and modulating the gut microbiota. [Abstract]2026 Jul:156:158269. PMID: 42102790 -
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J Hazard Mater
2026 Jul 1:512:142315. PMID: 42107411 -
ACS Environ Au
Machine Learning-Assisted Recognition of Environmental Sulfur-Containing Chemicals in Nontargeted Mass Spectrometry Analysis of Inadequate Mass Resolution. [Abstract]2025 Aug 5;5(6):573-582. PMID: 41277996 -
Cell Rep
Cell-cell and cell-matrix adhesion regulated by Piezo1 is critical for stiffness-dependent DRG neuron aggregation. [Abstract]2023 Dec 2;42(12):113522. PMID: 38048221 -
Curr Biol
Molecular sensors for temperature detection during behavioral thermoregulation in turtle embryos. [Abstract]2021 Jul 26;31(14):2995-3003.e4. PMID: 34015251 -
Curr Biol
2019 Aug 19;29(16):2597-2603.e4. PMID: 31378606 -
Environ Pollut
High humidity and NO2 co-exposure exacerbates allergic asthma by increasing oxidative stress, inflammatory and TRP protein expressions in lung tissue. [Abstract]2024 Jul 15:353:124127. PMID: 38759746 -
J Agric Food Chem
Capsaicin Mitigates Reverb α-Involved Lipid Metabolism Disorder in HepG2 Cells and Obese Mice through a Trpv1-Dependent Mechanism. [Abstract]2025 Mar 5;73(9):5300-5310. PMID: 39993721 -
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Life Sci
Effects of inhalation of sevoflurane at different concentrations on TRPV1 in airways of rats at different developmental stages. [Abstract]2020 May 15:249:117472. PMID: 32112870 -
Food Funct
Capsaicin inhibits the metastasis of human papillary thyroid carcinoma BCPAP cells through the modulation of the TRPV1 channel. [Abstract]2018 Jan 24;9(1):344-354. PMID: 29185571
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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J Mol Cell Biol
Capsaicin restores sodium iodine symporter-mediated radioiodine uptake through bypassing canonical TSH‒TSHR pathway in anaplastic thyroid carcinoma cells. [Abstract]2022 Jan 21;13(11):791-807. PMID: 34751390 -
Commun Biol
2025 May 10;8(1):724. PMID: 40348921 -
Commun Biol
Behavioral thermoregulation by reptile embryos promotes hatching success and synchronization. [Abstract]2023 Aug 15;6(1):848. PMID: 37582884 -
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Int Immunopharmacol
Activating TRPV1 by evodiamine attenuates atherosclerosis by inhibiting endothelial microparticle release. [Abstract]2025 May 16:155:114657. PMID: 40239331 -
Front Pharmacol
Toxic Peptide From Palythoa caribaeorum Acting on the TRPV1 Channel Prevents Pentylenetetrazol-Induced Epilepsy in Zebrafish Larvae. [Abstract]2021 Dec 1:12:763089. PMID: 34925021 -
ACS Omega
2025 Aug 21;10(34):39192-39202. PMID: 40918390 -
Nanoscale
Capsaicin-induced Ca2+ overload and ablation of TRPV1-expressing axonal terminals for comfortable tumor immunotherapy. [Abstract]2025 Feb 6;17(6):3288-3305. PMID: 39688368 -
Mol Med Rep
MUC1‑ND interacts with TRPV1 to promote corneal epithelial cell proliferation in diabetic dry eye mice by partly activating the AKT signaling pathway. [Abstract]2024 Dec;30(6):213. PMID: 39370807 -
Sci Rep
2026 Feb 9;16(1):7851. PMID: 41663512 -
Cell Calcium
A NOX2-independent mechanism of Hv1 channel activation promotes inflammatory cytokine release from BV-2 microglia via intracellular Ca2+ mobilisation. [Abstract]2026 Mar:134:103122. PMID: 41581267 -
Am J Pathol
TRPV1 dysfunction impairs gastric nitrergic neuromuscular relaxation in high fat diet induced diabetic gastroparesis mice. [Abstract]2023 May;193(5):548-557. PMID: 36740184 -
J Cell Mol Med
Capsaicin Receptor TRPV1 Delays Aortic Aging in Atherosclerotic Mice by Inhibiting the ISG15-p53 Pathway. [Abstract]2026 Apr;30(8):e71157. PMID: 42033162 -
Anesth Analg
Protein Arginine Methyltransferase 5 Contributes to Paclitaxel-Induced Neuropathic Pain by Activating Transient Receptor Potential Vanilloid 1 Epigenetic Modification in Dorsal Root Ganglion. [Abstract]2024 May 1;138(5):1107-1119. PMID: 37390022 -
Cell Signal
Capsaicin induces mitochondrial dysfunction and apoptosis in anaplastic thyroid carcinoma cells via TRPV1-mediated mitochondrial calcium overload. [Abstract]2020 Nov:75:109733. PMID: 32771398 -
J Inflamm Res
Neural-Inflammation Mechanism of Spinal Palmitic Acid Promoting Atopic Dermatitis in Mice. [Abstract]2025 Jun 17:18:7907-7919. PMID: 40546406 -
J Neurochem
Neuronal TRPV1-CGRP axis regulates peripheral nerve regeneration through ERK/HIF-1 signaling pathway. [Abstract]2025 Jan;169(1):e16281. PMID: 39792906 -
J Inflamm Res
2024 Jul 2:17:4257-4275. PMID: 38979434 -
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FASEB J
Capsazepine Inhibits Astrocyte Activation and Attenuates Neuroinflammation by Targeting Syntaxin 7. [Abstract]2025 May 31;39(10):e70657. PMID: 40386937 -
FASEB J
Mechanosensitive Ca2+ channel TRPV1 activated by low-intensity pulsed ultrasound ameliorates acute kidney injury through Notch1-Akt-eNOS signaling. [Abstract]2025 Jan 15;39(1):e70304. PMID: 39785696 -
Microbiol Spectr
C-Fiber Degeneration Enhances Alveolar Macrophage-Mediated IFN-α/β Response to Respiratory Syncytial Virus. [Abstract]2022 Dec 21;10(6):e0241022. PMID: 36350149 -
J Biol Chem
A specialized pore turret in the mammalian cation channel TRPV1 is responsible for distinct and species-specific heat activation thresholds. [Abstract]2020 Jul 10;295(28):9641-9649. PMID: 32461255 -
J Photochem Photobiol B
Novel design of NIR-triggered plasmonic nanodots capped mesoporous silica nanoparticles loaded with natural capsaicin to inhibition of metastasis of human papillary thyroid carcinoma B-CPAP cells in thyroid cancer chemo-photothermal therapy. [Abstract]2019 Aug:197:111534. PMID: 31279897 -
J Endod
Activation of Transient Receptor Potential Ankyrin 1 and Vanilloid 1 Channels Promotes Odontogenic Differentiation of Human Dental Pulp Cells. [Abstract]2021 Sep;47(9):1409-1416. PMID: 34126160 -
Biochim Biophys Acta Mol Cell Biol Lipids
Melatonin ameliorates ox-LDL-induced lipid accumulation and enhances ABCA1 expression in VSMCs via inhibition of the TRPV1-Ca2+-calpain signaling pathway. [Abstract]2026 Jan;1871(1):159704. PMID: 41213324 -
Mol Pain
EXPRESS: Evodiamine attenuates chemotherapy-induced peripheral neuropathy by mediating macrophage M2 polarization and inhibiting the upregulation of the p38 MAPK-TRPV1 axis in rat dorsal root ganglia. [Abstract]2025 Nov 26:17448069251392037. PMID: 41294237 -
Mol Pain
Histamine H4 receptor and TRPV1 mediate itch induced by cadaverine, a metabolite of the microbiome. [Abstract]2024 Jan-Dec:20:17448069241272149. PMID: 39079948 -
Integr Zool
Does embryonic behavioral thermoregulation enhance thermoregulatory capacity of turtle hatchlings?. [Abstract]2025 Jul;20(4):800-804. PMID: 39245877 -
Front Oncol
Transient Receptor Potential Cation Channel Subfamily V Member 1 Expression Promotes Chemoresistance in Non-Small-Cell Lung Cancer. [Abstract]2022 Mar 25;12:773654. PMID: 35402237 -
Cryobiology
Effects of spray cryotherapy on cough receptors and airway microenvironment in a canine model of chronic bronchitis. [Abstract]2023 Dec:113:104569. PMID: 37597598 -
Am J Physiol Regul Integr Comp Physiol
Blocking the transient receptor potential vanilloid-1 does not reduce the exercise pressor reflex in healthy rats. [Abstract]2019 Oct 1;317(4):R576-R587. PMID: 31365302 -
Biochem Biophys Res Commun
2019 Aug 20;516(2):365-372. PMID: 31213294 -
Clin Exp Pharmacol Physiol
Anti-inflammatory and retinal protective effects of capsaicin on ischaemia-induced injuries through the release of endogenous somatostatin. [Abstract]2017 Jul;44(7):803-814. PMID: 28429852 -
Exp Ther Med
Potential mechanism of transient receptor potential cation channel subfamily V member 1 combined with an ATP‑sensitive potassium channel in severe preeclampsia. [Abstract]2023 May 15;26(1):318. PMID: 37273761 -
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Sci Total Environ
The IL-31/TRPV1 pathway mediates allergic asthma exacerbated by DINP dermal exposure in OVA-sensitized Balb/c mice. [Abstract]2024 Feb 20:912:169613. PMID: 38154627 -
Oxid Med Cell Longev
TRPV1 Modulator Ameliorates Alzheimer-Like Amyloid- β Neuropathology via Akt/Gsk3 β-Mediated Nrf2 Activation in the Neuro-2a/APP Cell Model. [Abstract]2022 Aug 27:2022:1544244. PMID: 36065437 -
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Biomed Pharmacother
Anesthetic propofol blunts remote preconditioning of trauma-induced cardioprotection via the TRPV1 receptor. [Abstract]2019 Oct:118:109308. PMID: 31401396
Solvent & Solubility
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.
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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.
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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Protocol
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (279 KB)
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SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
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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]
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.
| 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
HY-15640 Related Classifications
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