| Size | Price | Stock | Qty |
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| 1mg |
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| Other Sizes |
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Purity: ≥98%
Resiniferatoxin is a naturally occuring capsaicin analog extracted from some plants of the genus Euphorbia, including E. resinifera. Resiniferatoxin modulates the Th1 immune response and protects the host during intestinal nematode infection. Intraluminal Administration of Resiniferatoxin Protects against Clostridium difficile Toxin A-Induced Colitis.
| ln Vitro |
Resiniferatoxin promotes inflow and prolongs channel opening, which causes TRPV1 fibers or cell bodies to undergo acute pain-inducing cytotoxicity [1].
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| ln Vivo |
Resiniferatoxin (2 μg/10 μl; intrathecally into the T2/T3 area; causes cardiomyopathy 4 weeks post-coronary blockage) reduces overactivated CSNA and dramatically and indirectly abolishes marker expression in the dorsal horn (TRPV1 and nortonin-inducible gene-related peptide). Resiniferatoxin decreases the susceptibility of ventricular arrhythmias and dramatically reverses the lengthening of action episode duration (APD) and APD alternation [2].
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| References |
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| Additional Infomation |
Resiniferatoxin is a heteropentacyclic compound found in Euphorbia poissonii with molecular formula C37H40O9. It is an agonist of the transient receptor potential cation channel subfamily V member 1 (TrpV1). It has a role as a TRPV1 agonist, a plant metabolite, a neurotoxin and an analgesic. It is a diterpenoid, an ortho ester, a tertiary alpha-hydroxy ketone, a member of phenols, a monomethoxybenzene, an organic heteropentacyclic compound, a carboxylic ester and an enone.
Resiniferatoxin (RTX) is a naturally occurring, ultrapotent capsaicin analog that activates the vanilloid receptor in a subpopulation of primary afferent sensory neurons involved in nociception (the transmission of physiological pain). Resiniferatoxin has been reported in Euphorbia unispina and Euphorbia resinifera with data available. Resiniferatoxin is a naturally occurring capsaicin analog found in the latex of the cactus Euphorbia resinifera with analgesic activity. Resiniferatoxin (RTX) binds to and activates the transient receptor potential vanilloid 1 (TRPV1), a non-selective cation channel in the plasma membrane of primary afferent sensory neurons. This increases the permeability to cations, and leads to an influx of calcium and sodium ions. This results in membrane depolarization, causing an irritant effect, followed by desensitization of the sensory neurons thereby inhibiting signal conduction in afferent pain pathways and causing analgesia. TRPV1, a member of the transient receptor potential channel (TRP) superfamily, is a heat- and chemo-sensitive calcium/sodium ion channel that is selectively expressed in a subpopulation of pain-sensing primary afferent neurons. Drug Indication Investigated for use/treatment in interstitial cystitis and urinary incontinence. |
| Exact Mass |
628.267
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|---|---|
| CAS # |
57444-62-9
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| PubChem CID |
5702546
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| Appearance |
White to off-white solid powder
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| Density |
1.35g/cm3
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| Boiling Point |
768.7ºC at 760mmHg
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| Flash Point |
240.3ºC
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| Index of Refraction |
1.643
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| LogP |
4.744
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
9
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| Rotatable Bond Count |
9
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| Heavy Atom Count |
46
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| Complexity |
1330
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| Defined Atom Stereocenter Count |
8
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| SMILES |
O1C2(C([H])([H])C3C([H])=C([H])C([H])=C([H])C=3[H])O[C@@]3(C(=C([H])[H])C([H])([H])[H])C([H])([H])[C@@]([H])(C([H])([H])[H])[C@]41[C@]1([H])C([H])=C(C([H])([H])[H])C([C@]1(C([H])([H])C(C([H])([H])OC(C([H])([H])C1C([H])=C([H])C(=C(C=1[H])OC([H])([H])[H])O[H])=O)=C([H])[C@@]4([H])[C@@]3([H])O2)O[H])=O
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| InChi Key |
DSDNAKHZNJAGHN-MXTYGGKSSA-N
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| InChi Code |
InChI=1S/C37H40O9/c1-21(2)35-17-23(4)37-27(33(35)44-36(45-35,46-37)19-24-9-7-6-8-10-24)14-26(18-34(41)30(37)13-22(3)32(34)40)20-43-31(39)16-25-11-12-28(38)29(15-25)42-5/h6-15,23,27,30,33,38,41H,1,16-20H2,2-5H3/t23-,27+,30-,33-,34-,35-,36-,37-/m1/s1
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| Chemical Name |
[(1R,2R,6R,10S,11R,13S,15R,17R)-13-benzyl-6-hydroxy-4,17-dimethyl-5-oxo-15-prop-1-en-2-yl-12,14,18-trioxapentacyclo[11.4.1.01,10.02,6.011,15]octadeca-3,8-dien-8-yl]methyl 2-(4-hydroxy-3-methoxyphenyl)acetate
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~50 mg/mL (~79.53 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1.25 mg/mL (1.99 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 12.5 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 1.25 mg/mL (1.99 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 12.5 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT05695339 | RECRUITING | Drug: Resiniferatoxin | Morton's Neuroma | National Institutes of Health Clinical Center (CC) | 2024-07-23 | Phase 1 |
| NCT02522611 | NOT YET RECRUITING | Drug: Resiniferatoxin | Intractable Pain Palliative Care |
National Institute of Neurological Disorders and Stroke (NINDS) | 2024-10-01 | Phase 1 Phase 2 |
| NCT05067257 | SUSPENDED | Drug: Resiniferatoxin Drug: Placebo |
Pain Pain Cancer Pain, Intractable |
Sorrento Therapeutics, Inc | 2025-09 | Phase 2 |
| NCT03226574 | COMPLETED | Drug: Resiniferatoxin | Intractable Cancer Pain | Sorrento Therapeutics, Inc | 2017-09-01 | Phase 1 |
| NCT03542838 | COMPLETED | Drug: Resiniferatoxin Drug: Saline |
Osteoarthritis, Knee Pain, Knee |
Sorrento Therapeutics, Inc | 2018-07-12 | Phase 1 |
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