| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| Targets |
TRPV1
|
|---|---|
| ln Vitro |
Vocacapsaicin (CA-008, Conentric Analgesics) – an investigational TRPV agonist being studied for long-lasting pain – works through the same TRPV1 agonism mechanism but its localized delivery is thought to minimize activation of a large array of neurons, such as capsaicin topical products[1].
|
| ln Vivo |
When injected into surgical sites, vocacapsaicin is rapidly converted to lipophilic capsaicin and can cross the membranes to reach the desired amino acid target on TRVP1 channels[1].
|
| References |
[1]. Olivia Higgins, et al. Analgesics of the Future: The Potential of Vocacapsaicin Injections for Knee Pain. 12 Articles in Volume 21, Issue #2.
|
| Additional Infomation |
A recently completed Phase 2 clinical trial of vocacapsaicin displayed significant pain reductions in patients undergoing TKA. The study was randomized, double-blinded, and placebo-controlled.
Every TKA patient received standard of care treatment, which included spinal anesthesia, ketorolac, acetaminophen, and ropivacaine in the form of joint filtration, femoral nerve, and IPACK blocks. Two intervention arms included administration of vocacapsaicin 36 mg (n = 61) and vocacapsaicin 60 mg (n = 62), each given via infiltration to the surgical site. The control arm (n = 64) received the standard of care regimen as well as opioid rescue as needed. The primary outcome was pain reductions recorded based on the numerical rating scale (NRS). The NRS is an 11-point scale with “0” being no pain and “10” being the most intense pain imaginable. The number being selected is expressed verbally by a patient based on the pain they have experienced in the last 24 hours.
Pain reductions at rest – expressed when vocacapsaicin 36 mg was delivered – are displayed in Table I. Pain reductions with ambulation – when vocacapsaicin 36 mg was delivered – are expressed in Table II.
Opioid consumption was significantly reduced among the vocacapsaicin 36-mg arm following a period of 96 hours and 168 hours after administration. Concentric Analgesics noted consistently better results with vocacapsaicin 36 mg compared to vocacapsaicin 60 mg. In light of side effect profiles, parameters among the intervention arms and control arm appeared consistent. Neither local nor systemic safety concerns were identified in the Phase 2 trial.¹⁴ A manuscript has yet to be published so further explanations of data including exclusion and inclusion criteria, definitions of AUC, specific adverse events, and rates, are not available. Further information will be welcomed to adequately assess the utilization of this therapy.
|
| Molecular Formula |
C26H42CLN3O4
|
|---|---|
| Molecular Weight |
496.08
|
| Exact Mass |
495.28638
|
| Elemental Analysis |
C, 62.95; H, 8.53; Cl, 7.15; N, 8.47; O, 12.90
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| CAS # |
1931116-92-5
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| Related CAS # |
Vocacapsaicin;1931116-86-7
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| PubChem CID |
132169136
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| Appearance |
Typically exists as solid at room temperature
|
| InChi Key |
WOJDHHAJADLOCK-RVDQCCQOSA-N
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| InChi Code |
InChI=1S/C26H41N3O4.ClH/c1-20(2)11-7-5-6-8-13-25(30)28-18-21-14-15-23(24(17-21)32-4)33-26(31)29-16-10-9-12-22(29)19-27-3;/h7,11,14-15,17,20,22,27H,5-6,8-10,12-13,16,18-19H2,1-4H3,(H,28,30);1H/b11-7+;
|
| Chemical Name |
(E)-2-methoxy-4-((8-methylnon-6-enamido)methyl)phenyl 2-((methylamino)methyl)piperidine-1-carboxylate hydrochloride
|
| Synonyms |
Vocacapsaicin hydrochloride; CA-008 HYDROCHLORIDE; 1931116-92-5; Vocacapsaicin (hydrochloride); Vocacapsaicin hydrochloride (USAN); Vocacapsaicin hydrochloride [USAN]; CHEMBL4594295; SCHEMBL19643643;
|
| 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 |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.0158 mL | 10.0790 mL | 20.1580 mL | |
| 5 mM | 0.4032 mL | 2.0158 mL | 4.0316 mL | |
| 10 mM | 0.2016 mL | 1.0079 mL | 2.0158 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
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.
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