Art. -Nr.: HY-N2333

Resiniferatoxin

(Synonyms: (+)-Resiniferatoxin)

13 Cited Publications

Kundenbewertung

Based on 13 publication(s) in Google Scholar

Resiniferatoxin ((+)-Resiniferatoxin), is a selective agonist of transient receptor potential vanilloid 1 (TRPV1) receptor agonist. Resiniferatoxin can be isolated from the Euphorbia resinifera plant. Resiniferatoxin eliminates TRPV1+ primary sensory afferents and blunt cardiac sympathetic afferent reflex for a relatively long period.

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Reinheit: 99.77%
CAS. Nr.: 57444-62-9
Formel: C₃₇H₄₀O₉
Molecular Weight:628.71

Speicherung:

-20°C, protect from light

* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Resiniferatoxin Chemical Structure

CAS. Nr.: 57444-62-9

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Biologische Aktivität
- Beschreibung
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (13)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

Alle TRP Channel Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
5637	IC₅₀	19.9 μM Compound: 5; RTX	Antiproliferative activity against human 5637 cells assessed as inhibition of cell growth measured after 24 hrs by MTT assay Antiproliferative activity against human 5637 cells assessed as inhibition of cell growth measured after 24 hrs by MTT assay	[PMID: 37000154]
CHO	EC₅₀	0.27 nM Compound: 1, RTX	Agonist activity at rat TRPV1 expressed in CHO cells assessed as 45Ca2+ uptake Agonist activity at rat TRPV1 expressed in CHO cells assessed as 45Ca2+ uptake	[PMID: 21111618]
CHO	EC₅₀	0.27 nM Compound: RTX	Agonist activity at rat TRPV1 receptor expressed in CHO cells assessed as calcium uptake Agonist activity at rat TRPV1 receptor expressed in CHO cells assessed as calcium uptake	[PMID: 19135377]
CHO	EC₅₀	0.92 nM Compound: 1, RTX	Agonist activity at human TRPV1 expressed in CHO cells assessed as stimulation of Ca2+ uptake Agonist activity at human TRPV1 expressed in CHO cells assessed as stimulation of Ca2+ uptake	[PMID: 23981530]
CHO	EC₅₀	0.92 nM Compound: 1, RTX	Agonist activity at human TRPV1 expressed in CHO cells assessed as 45Ca2+ uptake after 20 mins by liquid scintillation counting analysis Agonist activity at human TRPV1 expressed in CHO cells assessed as 45Ca2+ uptake after 20 mins by liquid scintillation counting analysis	[PMID: 24321344]
HEK293	EC₅₀	0.019 nM Compound: 1a, RTX	Agonist activity at human recombinant TRPV1 expressed in human HEK293 cells Agonist activity at human recombinant TRPV1 expressed in human HEK293 cells	[PMID: 17046253]
HEK293	EC₅₀	1.9 nM Compound: 1	Induced [Ca2+] influx in Vanilloid receptor subtype 1 expressing HEK 293 cells Induced [Ca2+] influx in Vanilloid receptor subtype 1 expressing HEK 293 cells	[PMID: 11934585]
HEK293	EC₅₀	19 pM Compound: 2a, RTX	Agonist activity at human TRPV1 expressed in HEK293 cells assessed as increase in intracellular calcium level Agonist activity at human TRPV1 expressed in HEK293 cells assessed as increase in intracellular calcium level	[PMID: 19951840]
MT4	EC₅₀	22.6 μM Compound: 29	Antiviral activity against HIV2 ROD infected in MT4 cells assessed as cell viability after 5 days by MTT assay Antiviral activity against HIV2 ROD infected in MT4 cells assessed as cell viability after 5 days by MTT assay	[PMID: 25970561]
MT4	EC₅₀	26 μM Compound: 29	Antiviral activity against HIV1 3B infected in MT4 cells assessed as cell viability after 5 days by MTT assay Antiviral activity against HIV1 3B infected in MT4 cells assessed as cell viability after 5 days by MTT assay	[PMID: 25970561]
T-24	IC₅₀	~21.4 μM Compound: 5; RTX	Antiproliferative activity against human T24 cells assessed as inhibition of cell growth measured after 24 hrs by MTT assay Antiproliferative activity against human T24 cells assessed as inhibition of cell growth measured after 24 hrs by MTT assay	[PMID: 37000154]
Vero	EC₅₀	1.8 μM Compound: 29	Antiviral activity against chikungunya virus Indian ocean strain 899 infected in Vero cells assessed as virus-induced cytopathic effect after 6 to 7 days Antiviral activity against chikungunya virus Indian ocean strain 899 infected in Vero cells assessed as virus-induced cytopathic effect after 6 to 7 days	[PMID: 25970561]

In Vitro

Resiniferatoxin causes extremely prolonged channel opening and calcium influx, which results in cytotoxicity to the TRPV1-positive pain fibers or cell bodies^[1].

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

In Vivo

Resiniferatoxin (2 μg/10 μl; injected intrathecally into the T2/T3 interspace; four weeks after coronary artery occlusion to induce heart failure in rats) significantly and selectively abolishes the afferent markers expression (TRPV1 and calcitonin gene-related peptide) in dorsal horn and reduced overactivated CSNA. Resiniferatoxin significantly reverses the prolongation of action potential duration (APD) and APD alternan, reduces the inducibilities of ventricular arrhythmias^[2].

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

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 57444-62-9
Appearance Solid
Molecular Weight 628.71
Formel C₃₇H₄₀O₉
SMILES

C[C@H]1[C@]23[C@](C=C(C[C@]4([C@@]3([H])C=C(C4=O)C)O)COC(CC5=CC(OC)=C(C=C5)O)=O)([H])[C@]6([H])[C@](C1)(O[C@](O2)(O6)CC7=CC=CC=C7)C(C)=C
Synonyms

(+)-Resiniferatoxin
Structure Classification
- Phenols
- Monophenols
Initial Source
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

-20°C, protect from light

* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Publications (13)

All In Vivo Efficacy StudyIHCWBRT-PCR

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Journal Impact Factor

Cell

Cancer cells co-opt an inter-organ neuroimmune circuit to escape immune surveillance. [Abstract]

2025 Nov 26;188(24):6754-6773.e29. PMID: 41138728
Adv Sci (Weinh)

Nociceptive Nerve-Derived CGRP Exacerbates Uterine Fibrogenesis in Adenomyosis by Promoting CD140b+ CD146+ Fibroblast Differentiation. [Abstract]

2025 Sep 23:e07128. PMID: 40985151

Resiniferatoxin purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2025 Sep 23:e07128. [Abstract]

Representative images of IHC staining of uteri from mice with PGP9.5. Scale bar, 50 μm. Red arrows: positive PGP9.5 staining. Twenty‐four female mice were randomly assigned to four groups (n = 6 per group): 1) Control (vehicle + vehicle), 2) RTX‐C (vehicle + RTX), 3) M (tamoxifen + vehicle), and 4) RTX‐M (tamoxifen + RTX). Sensory denervation was induced by intraperitoneal injection of RTX (Resiniferatoxin) at 150 µg/kg every 5 days, beginning on day 42. All mice were euthanized on day 63.

Resiniferatoxin purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2025 Sep 23:e07128. [Abstract]

RH&E, Masson trichrome staining of mice uteri at Day 63 and the corresponding horizon of multiple IF staining of E‐CAD (green), αSMA (red), and nucleus (DAPI, Blue). The yellow dotted circle showed the location of the ectopic lesion. The black dotted frame was the zoomed‐out version of the middle picture. Twenty‐four female mice were randomly assigned to four groups (n = 6 per group): 1) Control (vehicle + vehicle), 2) RTX‐C (vehicle + RTX), 3) M (tamoxifen + vehicle), and 4) RTX‐M (tamoxifen + RTX). Sensory denervation was induced by intraperitoneal injection of RTX (Resiniferatoxin) at 150 µg/kg every 5 days, beginning on day 42. All mice were euthanized on day 63.

Resiniferatoxin purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2025 Sep 23:e07128. [Abstract]

Twenty‐four female mice were randomly assigned to four groups (n = 6 per group): 1) Control (vehicle + vehicle), 2) RTX‐C (vehicle + RTX), 3) M (tamoxifen + vehicle), and 4) RTX‐M (tamoxifen + RTX). Sensory denervation was induced by intraperitoneal injection of RTX (Resiniferatoxin) at 150 µg/kg every 5 days, beginning on day 42. All mice were euthanized on day 63.

Resiniferatoxin purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2025 Sep 23:e07128. [Abstract]

Relative expression levels of Fn, Col1a1, Acta2 (gene name of αSMA) in Control, RTX-C, M and RTX-M groups detected by qPCR. Twenty‐four female mice were randomly assigned to four groups (n = 6 per group): 1) Control (vehicle + vehicle), 2) RTX‐C (vehicle + RTX), 3) M (tamoxifen + vehicle), and 4) RTX‐M (tamoxifen + RTX). Sensory denervation was induced by intraperitoneal injection of RTX (Resiniferatoxin) at 150 µg/kg every 5 days, beginning on day 42. All mice were euthanized on day 63.
Int J Biol Macromol

Born with Silurian global warming: Defensive role of TRPV1 in caudal neurosecretory system (CNSS) in flounder. [Abstract]

2025 May 9:144092. PMID: 40350111
Br J Pharmacol

Synthesis and evaluation of a novel inhibitor for the α5-GABAA receptor in the treatment of peripheral neuralgia: Evidence from MD simulation and in vivo studies. [Abstract]

2025 Aug 9. PMID: 40782001
Cell Rep

Nociceptive neurons protect cancer cells against oxidative stress. [Abstract]

2026 Mar 24;45(3):117086. PMID: 41831232
Cell Rep

ILC2-derived CGRP triggers acute inflammation and nociceptive responses in bacterial cystitis. [Abstract]

2024 Oct 15;43(10):114859. PMID: 39412984
Life Sci

Sensory nerve desensitisation exerts differential effects on the severity of acute pancreatitis in rodent models. [Abstract]

2026 Aug 1:398:124435. PMID: 42107689
Invest Ophthalmol Vis Sci

Corneal Nerves Promote Alkali Burn Repair by Modulating Macrophages and Neutrophils via Calcitonin Gene-Related Peptide. [Abstract]

2026 Apr 1;67(4):60. PMID: 42041175
iScience

Stimulation of TRPV1+ peripheral somatosensory nerves suppress inflammation via the somato-autonomic reflex. [Abstract]

2025 Jan 17;28(2):111831. PMID: 39967868

Resiniferatoxin purchased from MedChemExpress. Usage Cited in: iScience. 2025 Jan 17;28(2):111831. [Abstract]

RTX was dissolved in 2% DMSO with 0.15% Tween 80 in PBS. 4-week-old C57BL/6J male mice were injected s.c. in the flank on consecutive days with three increasing doses of RTX (Resiniferatoxin, 30, 70, and 100 μg/kg). Control mice were treated with vehicle alone. Mice were rested for 4 weeks before experiments.
Sci Rep

PTPRK promotes resiniferatoxin-induced postherpetic neuralgia via activating DUSP1/p38 MAPK signaling pathway in dorsal root ganglia. [Abstract]

2025 Nov 18;15(1):40630. PMID: 41253902
J Mol Histol

Shentong Zhuyu decoction ameliorates postherpetic neuralgia in rats by regulating cAMP/PKA/p-CREB signaling. [Abstract]

2025 Oct 22;56(6):348. PMID: 41123684
Cytotechnology

S1P receptor 1 antagonist ponesimod alleviates postherpetic neuralgia in rats by normalizing spinal TRPV1 expression and inhibiting MAPK-mediated glial activation. [Abstract]

2025 Aug;77(4):141. PMID: 40642600
Biochem Genet

Saikosaponin D Attenuates Postherpetic Neuralgia and Reduces Inflammation by Regulating Gut Microbiota in a Rodent Model. [Abstract]

2026 May 8. PMID: 42101756

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 50 mg/mL (79.53 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.5906 mL

7.9528 mL

15.9056 mL

5 mM

0.3181 mL

1.5906 mL

3.1811 mL

10 mM

0.1591 mL

0.7953 mL

1.5906 mL

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, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

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

Stock Solution Working Solution

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: ≥ 1.25 mg/mL (1.99 mM); Clear solution

This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 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.

Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 1.25 mg/mL (1.99 mM); Clear solution

This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

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

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

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (284 KB)
SDS (641 KB)
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COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Brown DC. Resiniferatoxin: The Evolution of the "Molecular Scalpel" for Chronic Pain Relief. Pharmaceuticals (Basel). 2016;9(3):47. Published 2016 Aug 11. [Content Brief]

[2]. Wu Y, et al. Resiniferatoxin reduces ventricular arrhythmias in heart failure via selectively blunting cardiac sympathetic afferent projection into spinal cord in rats. Eur J Pharmacol. 2020;867:172836. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.5906 mL	7.9528 mL	15.9056 mL	39.7640 mL
	5 mM	0.3181 mL	1.5906 mL	3.1811 mL	7.9528 mL
	10 mM	0.1591 mL	0.7953 mL	1.5906 mL	3.9764 mL
	15 mM	0.1060 mL	0.5302 mL	1.0604 mL	2.6509 mL
	20 mM	0.0795 mL	0.3976 mL	0.7953 mL	1.9882 mL
	25 mM	0.0636 mL	0.3181 mL	0.6362 mL	1.5906 mL
	30 mM	0.0530 mL	0.2651 mL	0.5302 mL	1.3255 mL
	40 mM	0.0398 mL	0.1988 mL	0.3976 mL	0.9941 mL
	50 mM	0.0318 mL	0.1591 mL	0.3181 mL	0.7953 mL
	60 mM	0.0265 mL	0.1325 mL	0.2651 mL	0.6627 mL

Keywords

Resiniferatoxin

13 Cited Publications

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Resiniferatoxin

MCE Bioactive Compound Library

Natural Product Library Plus

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Biotoxin Library

Publications Citing Use of MedChemExpress (MCE) Resiniferatoxin

Alle TRP Channel Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (13)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Resiniferatoxin

MCE Bioactive Compound Library

Natural Product Library Plus

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Biotoxin Library

Publications Citing Use of MedChemExpress (MCE) Resiniferatoxin

Alle TRP Channel Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (13)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Resiniferatoxin Related Classifications

HY-N2333 Related Classifications