| 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 |
recently completed phase II clinical trial of vocacapsaicin showed that the drug significantly reduced pain in patients undergoing total knee arthroplasty (TKA). The study was randomized, double-blind, placebo-controlled. All TKA patients received standard treatment, including spinal anesthesia, ketorolac, acetaminophen, and ropivacaine (administered via intra-articular block, femoral nerve block, and IPACK block, respectively). Two intervention groups received 36 mg vocacapsaicin (n = 61) and 60 mg vocacapsaicin (n = 62), respectively, via surgical site infiltration. The control group (n = 64) received standard treatment and, as needed, opioid analgesia. The primary efficacy endpoint was pain reduction recorded using the Numerical Rating Scale (NRS). The NRS uses an 11-point scale, with 0 indicating no pain and 10 indicating unbearable pain. Patients verbally selected a number based on their pain level over the past 24 hours. Table I shows pain relief at rest after administration of 36 mg vocacapsaicin. Table II shows pain relief during activity after administration of 36 mg vocacapsaicin. Opioid usage was significantly reduced in the vocacapsaicin 36 mg group at 96 and 168 hours post-administration. Concentric Analgesics noted that the 36 mg vocacapsaicin was consistently more effective than the 60 mg vocacapsaicin. Regarding side effects, parameters appeared consistent between the intervention and control groups. No local or systemic safety issues were observed in the Phase II trial.¹⁴ As this research paper has not yet been published, further data interpretation, including inclusion and exclusion criteria, AUC definition, specific adverse events, and their incidence, is not available. We welcome further information to fully evaluate the use of this therapy.
|
| Molecular Formula |
C26H41N3O4
|
|---|---|
| Molecular Weight |
459.62
|
| Exact Mass |
459.309
|
| Elemental Analysis |
C, 67.94; H, 8.99; N, 9.14; O, 13.92
|
| CAS # |
1931116-86-7
|
| Related CAS # |
Vocacapsaicin hydrochloride;1931116-92-5
|
| PubChem CID |
121349852
|
| Appearance |
Typically exists as solid at room temperature
|
| LogP |
4.2
|
| Hydrogen Bond Donor Count |
2
|
| Hydrogen Bond Acceptor Count |
5
|
| Rotatable Bond Count |
13
|
| Heavy Atom Count |
33
|
| Complexity |
610
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
CC(C)/C=C/CCCCC(=O)NCC1=CC(=C(C=C1)OC(=O)N2CCCCC2CNC)OC
|
| InChi Key |
BXAQOVOOXOHMFY-ICKBMGCOSA-N
|
| InChi Code |
InChI=1S/C26H41N3O4/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)/b11-7+/t22-/m1/s1
|
| Chemical Name |
rac-2-methoxy-4-{[(6E)-8-methylnon-6-enamido]methyl}phenyl (2R)-2-[(methylamino)methyl]piperidine-1-carboxylate
|
| Synonyms |
CA-008; 1931116-86-7; Vocacapsaicin (USAN); Vocacapsaicin [USAN]; VOCACAPSAICIN [INN]; CHEMBL4594294; SCHEMBL17767309;
|
| HS Tariff Code |
2934.99.9001
|
| 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
|
|---|---|
| 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 | 2.1757 mL | 10.8786 mL | 21.7571 mL | |
| 5 mM | 0.4351 mL | 2.1757 mL | 4.3514 mL | |
| 10 mM | 0.2176 mL | 1.0879 mL | 2.1757 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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