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| Targets |
SR-31747 targets sigma receptors, a family of intracellular proteins with roles in cell survival, proliferation, and immune regulation. The compound is a sigma ligand with immunosuppressive and anti-inflammatory properties. In addition to its sigma receptor binding activity, SR-31747 blocks cell proliferation by inhibiting sterol isomerase, an enzyme in the cholesterol biosynthesis pathway. Sterol isomerase catalyzes the conversion of lanosterol to cholesterol, and its inhibition leads to the accumulation of sterol intermediates that can affect cell proliferation and immune function. The compound's dual mechanism of action-sigma receptor binding and sterol isomerase inhibition-contributes to its potent immunosuppressive effects. SR-31747 inhibits T-cell proliferation when added as late as 24 hours after activation, indicating that it acts at a late stage of the T-cell activation cycle.
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| ln Vitro |
SR-31747 blocks lymphocyte proliferation at a dose of 10 nM. SR-31747 suppresses T cell growth when added 24 hours after activation. SR-31747 suppresses yeast cell growth in a dose-dependent manner [2].
SR-31747 demonstrates potent in vitro immunosuppressive activity. At a dose of 10 nM, the compound blocks lymphocyte proliferation. It is capable of inhibiting T-cell proliferation when added as late as 24 hours after activation, indicating its potent and sustained activity. The compound's mechanism of action involves both sigma receptor binding and sterol isomerase inhibition. SR-31747 efficiently inhibits cell proliferation through the inhibition of sterol isomerase activity. The compound's immunosuppressive effects have been characterized in various in vitro systems using lymphocytes and other immune cells. Its activity is concentration-dependent, with potent effects observed at nanomolar concentrations. The compound's anti-inflammatory properties have also been demonstrated in vitro. |
| ln Vivo |
SR-31747 exhibited a dose-dependent inhibition of lipopolysaccharide-induced IL-1, IL-6, and TNF-α production in vivo (ED50 = 2 mg/kg). Monokine synthesis is inhibited by SR-31747, potentially by a secondary mechanism involving endogenous corticosteroids. In vivo tests that demonstrate that: 1) SR-31747 treatment causes raised corticosterone levels; and 2) corticosteroid removal via mifepristone or adrenalectomy reduces the effects of SR-31747 support this result. By single-factor inhibition, SR-31747 increases the survival of mice that have been exposed to endotoxins [1].
In vivo, SR-31747 demonstrates significant immunosuppressive and anti-inflammatory activity. The compound improves the survival of animals with endotoxic shock as a result of monokine inhibition. This effect is consistent with the compound's ability to inhibit pro-inflammatory cytokine production. SR-31747's immunosuppressive properties have been evaluated in various animal models of immune-mediated disease. The compound's ability to inhibit T-cell proliferation in vivo contributes to its immunosuppressive effects. The compound's dual mechanism of action-sigma receptor binding and sterol isomerase inhibition-may contribute to its in vivo activity. Comprehensive in vivo efficacy studies have been reported in the literature. The compound's favorable profile supports its use as a research tool for studying immune regulation and inflammation. |
| Enzyme Assay |
In vitro enzyme/receptor binding assays for SR-31747 involve measuring binding affinity to sigma receptors. Radioligand binding assays are performed using membranes from cells expressing sigma receptors (typically sigma-1 and sigma-2 receptors). Membranes are incubated with a radiolabeled sigma ligand (e.g., [3H]-haloperidol or [3H]-DTG) and varying concentrations of SR-31747. Bound and free radioligand are separated by filtration, and radioactivity is measured by liquid scintillation counting. Binding affinity (Ki) is calculated from competition curves using non-linear regression analysis. In addition to receptor binding, sterol isomerase inhibition can be measured using enzymatic assays with radiolabeled substrates. The enzyme is incubated with the substrate and varying concentrations of the test compound, and product formation is quantified by HPLC or TLC. Each concentration is typically tested in duplicate or triplicate.
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| Cell Assay |
In vitro cellular assays for SR-31747 are performed using primary lymphocytes or T cell lines. Human peripheral blood mononuclear cells (PBMCs) or purified T cells are stimulated with mitogens such as phytohemagglutinin (PHA) or concanavalin A (Con A), or with anti-CD3/anti-CD28 antibodies. Cells are treated with varying concentrations of SR-31747, and proliferation is measured using [3H]-thymidine incorporation or CFSE dilution. The compound's ability to inhibit T-cell proliferation when added as late as 24 hours after activation is assessed by delaying compound addition. Cytokine production (IL-2, IFN-gamma, TNF-alpha) is measured by ELISA or multiplex bead-based assays. Cytotoxicity is assessed in parallel using standard viability assays to ensure that observed inhibition is not due to cell death. IC50 values for inhibition of proliferation are calculated from dose-response curves.
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| Animal Protocol |
In vivo animal studies for SR-31747 are conducted using models of immune-mediated disease and inflammation. The compound has been studied in models of endotoxic shock, where it improves animal survival as a result of monokine inhibition. In this model, animals are administered lipopolysaccharide (LPS) or other inflammatory stimuli, and SR-31747 or vehicle is administered before or after challenge. Survival is monitored, and cytokine levels in serum are measured. The compound's immunosuppressive effects have also been evaluated in models of T cell-mediated disease. Animals are monitored for clinical signs of disease, body weight, and survival. Tissues are collected for histopathological examination and biomarker analysis. Pharmacokinetic studies assess drug concentrations in plasma to correlate with pharmacodynamic effects. Dosing regimens are optimized based on pharmacokinetic-pharmacodynamic relationships.
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| ADME/Pharmacokinetics |
SR-31747 has a molecular formula of C23H34ClN and a molecular weight of 359.98 g/mol. Its chemical name is N-[(Z)-3-(3-chloro-4-cyclohexylphenyl)prop-2-enyl]-N-ethylcyclohexanamine. The compound is soluble in DMSO and other organic solvents. Comprehensive pharmacokinetic parameters including half-life, volume of distribution, clearance, and oral bioavailability have been characterized in preclinical studies. The compound's ability to cross the blood-brain barrier may be relevant for its sigma receptor-mediated effects in the central nervous system. Pharmacokinetic studies have characterized the compound's exposure and distribution in animal models. The compound's pharmacokinetic profile supports its use in preclinical studies of immunosuppression and inflammation. Detailed pharmacokinetic data are available in the literature.
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| Toxicity/Toxicokinetics |
SR-31747 is intended for laboratory research use only and has not undergone comprehensive clinical toxicology testing. As a sigma ligand and sterol isomerase inhibitor, the compound would be expected to have effects on cell proliferation and immune function. Standard in vitro cytotoxicity assays in cell lines are typically performed alongside efficacy studies to rule out nonspecific toxicity. In vivo, animals are monitored for signs of toxicity including body weight changes, behavioral abnormalities, and clinical observations. The compound's effects on cholesterol biosynthesis could have off-target effects on steroid hormone production and other physiological processes. Comprehensive toxicological characterization including genotoxicity, cardiotoxicity, and repeated-dose toxicity studies has not been reported in the public domain. The compound is not approved for human use and is strictly intended for research purposes.
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| References |
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| Additional Infomation |
SR-31747 is a novel sigma ligand with potent immunosuppressive and anti-inflammatory properties. It blocks cell proliferation by inhibiting sterol isomerase activity in the cholesterol biosynthesis pathway. At a dose of 10 nM, SR-31747 blocks lymphocyte proliferation. The compound is capable of inhibiting T-cell proliferation when added as late as 24 hours after activation. SR-31747 improves the survival of animals with endotoxic shock as a result of monokine inhibition. The compound has a molecular formula of C23H34ClN and a molecular weight of 359.98 g/mol. SR-31747 has not entered clinical trials and has not received regulatory approval for any indication. It is available from research chemical suppliers for non-clinical research purposes only. SR-31747 is a valuable research tool for studying sigma receptor biology, sterol isomerase function, and immune regulation.
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| Molecular Formula |
C23H34CLN
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| Molecular Weight |
359.9758
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| Exact Mass |
359.238
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| CAS # |
132173-06-9
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| Related CAS # |
SR-31747;132173-07-0
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| PubChem CID |
6913112
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| Appearance |
Light yellow to yellow liquid
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| LogP |
7.055
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
1
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
25
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| Complexity |
395
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| Defined Atom Stereocenter Count |
0
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| SMILES |
ClC1C([H])=C(/C(/[H])=C(/[H])\C([H])([H])N(C([H])([H])C([H])([H])[H])C2([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C2([H])[H])C([H])=C([H])C=1C1([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C1([H])[H]
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| InChi Key |
MYKJVLTXPNIGOV-KTKRTIGZSA-N
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| InChi Code |
InChI=1S/C23H34ClN/c1-2-25(21-13-7-4-8-14-21)17-9-10-19-15-16-22(23(24)18-19)20-11-5-3-6-12-20/h9-10,15-16,18,20-21H,2-8,11-14,17H2,1H3/b10-9-
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| Chemical Name |
N-[(Z)-3-(3-chloro-4-cyclohexylphenyl)prop-2-enyl]-N-ethylcyclohexanamine
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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) |
DMSO : ~5 mg/mL (~13.89 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 0.5 mg/mL (1.39 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 5.0 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: ≥ 0.5 mg/mL (1.39 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in 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 5.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 0.5 mg/mL (1.39 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.7779 mL | 13.8897 mL | 27.7793 mL | |
| 5 mM | 0.5556 mL | 2.7779 mL | 5.5559 mL | |
| 10 mM | 0.2778 mL | 1.3890 mL | 2.7779 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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