GLPBio

Resiniferatoxin

Catalog No.: GC12783Purity:>98.00%
COASDSData Sheet
Resiniferatoxin (RTX), an ultrapotent capsaicin analog, is a vanilloid agonist that binds to the transient receptor potential channel, vanilloid subfamily member 1 (TRPV1).

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Resiniferatoxin
Cas No.: 57444-62-9
10mM (in 1mL DMSO)In Stock
$866.00
1
1mgIn Stock
$348.00
1
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Citations

2 publicationsPublications from researchers using this product

Description

Resiniferatoxin (RTX), an ultrapotent capsaicin analog, is a vanilloid agonist that binds to the transient receptor potential channel, vanilloid subfamily member 1 (TRPV1).Resiniferatoxin activates TRPV1 in an irreversible manner. It also can bind and activate members of the PKC family[1-4].

Resiniferatoxin(0.1-10µM; 24 hours) can induce G0/G1 arrest in non-transformed intestinal epithelial cells[4].

Resiniferatoxin (250ng,50µL;s.c) blocks inflammatory heat hyperalgesia when applied directly to the sciatic nerve in a time and dose dependent fashion[5]. Resiniferatoxin treatment increased serum levels of IL-4, IL-10 and IL-13, and it decreases intestinal eosinophilia, however, favours the mastocytosis, promoting T spiralis intestinal expulsion[6]. Cutaneous injection of Resiniferatoxin(100 µL of RTX 0.002% (2 g); s.c in the plantar skin) completely alleviates and prevents nerve-injury-induced neuropathic pain in rat[7].

References:
[1]. Brown DC. Resiniferatoxin: The Evolution of the "Molecular Scalpel" for Chronic Pain Relief. Pharmaceuticals (Basel). 2016 Aug 11;9(3):47. doi: 10.3390/ph9030047. PMID: 27529257; PMCID: PMC5039500.
[2]. Montell C, Birnbaumer L, et,al. A unified nomenclature for the superfamily of TRP cation channels. Mol Cell. 2002 Feb;9(2):229-31. doi: 10.1016/s1097-2765(02)00448-3. PMID: 11864597.
[3]. Gunthorpe MJ, Benham CD, et,al. The diversity in the vanilloid (TRPV) receptor family of ion channels. Trends Pharmacol Sci 2002, 23:183-191.
[4]. Frey MR, Clark JA, et,al. Cell cycle- and protein kinase C-specific effects of resiniferatoxin and resiniferonol 9,13,14-ortho-phenylacetate in intestinal epithelial cells. Biochem Pharmacol. 2004 May 15;67(10):1873-86. doi: 10.1016/j.bcp.2004.02.006. PMID: 15130764.
[5]. Neubert JK, Mannes AJ, et,al. Perineural resiniferatoxin selectively inhibits inflammatory hyperalgesia. Mol Pain. 2008 Jan 16;4:3. doi: 10.1186/1744-8069-4-3. PMID: 18199335; PMCID: PMC2242785.
[6]. MuÑoz-Carrillo JL, GutiÉrrez-Coronado O, et,al. Resiniferatoxin promotes adult worm expulsion in Trichinella spiralis-infected rats by Th2 immune response modulation. Parasite Immunol. 2021 Aug;43(8):e12840. doi: 10.1111/pim.12840. Epub 2021 May 10. PMID: 33914935.
[7]. Javed H, Johnson AM, et,al. Cutaneous Injection of Resiniferatoxin Completely Alleviates and Prevents Nerve-Injury-Induced Neuropathic Pain. Cells. 2022 Dec 14;11(24):4049. doi: 10.3390/cells11244049. PMID: 36552812; PMCID: PMC9776507.

Protocol

Cell experiment [1]:

Cell lines

IEC-18 cell line

Preparation Method

Cells were treated with different concentrations of RTX for 24 hours as instructed.

Reaction Conditions

0.1-10µM Resiniferatoxin; 24 hours

Applications

Resiniferatoxin at 5-10 µM produced a prolonged cell cycle arrest in G0/G1 phase that was first evident by 6 h and sustained for at least 24 h.
Animal experiment [2]:

Animal models

Male Wistar rats

Preparation Method

Rats (weighing 240-255 g) underwent L5 spinal nerve ligation, On day 7, rats were injected with 100 µL of Resiniferatoxin 0.002% (2 g) or vehicle (10% Tween 80, 10% EtOH, 80% normal saline) in the plantar skin of the left hind paw.

Dosage form

100 µL of Resiniferatoxin 0.002% (2 g); s.c in the plantar skin

Applications

Intraplantar injection of RTX completely alleviates thermal and mechanical hypersensitivity caused by L5 nerve injury.

References:

[1].Frey MR, Clark JA, et,al.Cell cycle- and protein kinase C-specific effects of resiniferatoxin and resiniferonol 9,13,14-ortho-phenylacetate in intestinal epithelial cells. Biochem Pharmacol. 2004 May 15;67(10):1873-86. doi: 10.1016/j.bcp.2004.02.006. PMID: 15130764.
[2]. Javed H, Johnson AM,et,al. Cutaneous Injection of Resiniferatoxin Completely Alleviates and Prevents Nerve-Injury-Induced Neuropathic Pain. Cells. 2022 Dec 14;11(24):4049. doi: 10.3390/cells11244049. PMID: 36552812; PMCID: PMC9776507.

Product Documents

Purity:>98.00%Appearance:A jelly
COASDSData Sheet

Chemical Properties

CAS No.
57444-62-9
Chemical Name
((2R,3aR,3bS,6aR,9aR,9bR,10R,11aR)-2-benzyl-6a-hydroxy-8,10-dimethyl-7-oxo-11a-(prop-1-en-2-yl)-3b,6,6a,7,9a,10,11,11a-octahydro-3aH-2,9b-epoxyazuleno[5',4':3,4]benzo[1,2-d][1,3]dioxol-5-yl)methyl 2-(4-hydroxy-3-methoxyphenyl)acetate
SMILES
O[C@@]12[C@@H](C=C(C)C2=O)[C@]34O[C@@](O[C@@]5(C(C)=C)C[C@H]4C)(CC6=CC=CC=C6)O[C@@H]5[C@@H]3C=C(COC(CC(C=C7OC)=CC=C7O)=O)C1
Molecular Formula
C37H40O9
Molecular Weight
628.72
Solubility
DMSO : 50 mg/mL (79.53 mM; Need ultrasonic)
Storage
Store at -20°C, protect from light
General tips
Select a suitable solvent according to the product solubility data. Once prepared, aliquot the stock solution to avoid repeated freeze-thaw cycles.
Use stock solutions within 6 months when stored at -80°C or within 1 month when stored at -20°C.
To improve solubility, warm the tube to 37°C and sonicate it for an appropriate period.
Shipping Condition
Evaluation samples are shipped with blue ice. Other available sizes are shipped at room temperature or with blue ice upon request.

CalculatorsMolarity / Dilution / Molecular Weight / Unit Conversion / In Vivo Formulation / Solubility

g/mol

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