| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg |
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| Other Sizes |
| Targets |
S1RA HCl targets the sigma-1 receptor (σ1R) with high affinity, exhibiting a Ki of 17 nM. It is highly selective for σ1R over the sigma-2 receptor (σ2R, Ki > 1000 nM) and against a panel of other 170 receptors, enzymes, transporters, and ion channels. By antagonizing σ1R, it modulates pain signaling pathways.
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| ln Vitro |
In vitro, S1RA HCl demonstrates potent and selective binding to the sigma-1 receptor. Its high affinity (Ki = 17 nM) and excellent selectivity profile make it a valuable tool for studying the role of σ1R in pain and other neurological conditions. Its activity is confirmed in functional assays where it antagonizes σ1R-mediated effects, such as the modulation of calcium signaling.
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| ln Vivo |
In vivo, S1RA HCl has been shown to be effective in preclinical models of pain. It has demonstrated efficacy in various pain models, including diabetic neuropathies, chemotherapy-induced neuropathic pain, postherpetic neuralgia, and postoperative pain. These studies support its potential as a non-opioid analgesic for the treatment of chronic pain conditions.
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| Enzyme Assay |
The in vitro receptor binding assay for S1RA HCl involves competitive binding studies. Membranes from cells expressing the sigma-1 receptor are incubated with a radiolabeled ligand, such as [3H]-pentazocine, in the presence of varying concentrations of the antagonist. The amount of radioligand displaced is measured to determine the binding affinity (Ki).
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| Cell Assay |
In vitro cell-based functional assays for S1RA HCl utilize cells expressing the sigma-1 receptor. The compound's antagonist activity can be measured by its ability to reverse σ1R agonist-induced effects, such as the modulation of inositol phosphate production or calcium mobilization. The IC50 is determined from the concentration-response curve.
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| Animal Protocol |
In vivo animal experiments for S1RA HCl involve various pain models. For example, in a model of neuropathic pain, the compound is administered orally to rats with a nerve injury. Pain hypersensitivity is assessed by measuring mechanical allodynia using von Frey filaments or thermal hyperalgesia using a paw withdrawal test. A reduction in pain sensitivity indicates efficacy.
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| ADME/Pharmacokinetics |
S1RA HCl is a small molecule with good oral bioavailability. It is soluble in DMSO and water. For in vivo studies, it is formulated in suitable vehicles. It is typically stored as a powder at room temperature or -20°C. Its half-life and metabolic profile have been characterized in preclinical studies, supporting its development as a therapeutic agent.
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| Toxicity/Toxicokinetics |
Toxicological data from preclinical studies indicate that S1RA HCl is generally well-tolerated. As a sigma-1 receptor antagonist, it does not exhibit the typical side effects associated with opioid analgesics, such as respiratory depression, physical dependence, or abuse potential. This favorable safety profile has been a key factor in its clinical development.
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| References |
Br J Pharmacol.2012 Aug;166(8):2289-306;J Med Chem.2012 Oct 11;55(19):8211-24.
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| Additional Infomation |
S1RA HCl (E-52862) has been investigated in clinical trials for the treatment of various pain conditions. While it has shown promise in preclinical studies, its clinical development has faced challenges. It represents a novel class of non-opioid analgesics targeting the sigma-1 receptor, and its research has contributed significantly to understanding the role of this receptor in pain modulation.
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| Related CAS # |
878141-96-9; 1265917-14-3 (HCl)
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| Appearance |
Typically exists as solid at room temperature
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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 |
| 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) |
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.) |
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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