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| Targets |
SR-31747 targets sigma receptors, functioning as a peripheral sigma receptor ligand. Additionally, it inhibits sterol isomerase, an enzyme involved in cholesterol biosynthesis, thereby blocking cell proliferation. SR-31747 binds to four proteins in human cells and acts as a sigma receptor antagonist.
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| ln Vitro |
At 10 nM, SR-31747 inhibits the growth of lymphocytes. Twenty-four hours after activation, SR-31747 is administered, and this decreases T cell growth. SR-31747 inhibits the growth of yeast cells in a manner that is dependent on dosage [2].
SR-31747 inhibits the growth of lymphocytes. Twenty-four hours after activation, SR-31747 is administered, and this decreases T cell growth. At a concentration of 10 nM, SR-31747 inhibits lymphocyte growth. The compound's immunosuppressive and anti-inflammatory properties are mediated through sigma receptor binding and sterol isomerase inhibition. |
| 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].
SR-31747 improves survival in endotoxin shock models, highlighting its in vivo anti-inflammatory activity. As a sigma ligand with immunosuppressive properties, it modulates immune responses in vivo. Specific animal model data and dosing regimens are not extensively detailed in standard reference sources. |
| Enzyme Assay |
The receptor binding affinity of SR-31747 can be assessed using radioligand binding assays with membrane preparations from cells expressing sigma receptors. Competition binding experiments are performed with increasing concentrations of SR-31747 against a fixed concentration of a radiolabeled sigma receptor ligand. Non-specific binding is determined in the presence of an excess of a reference sigma ligand.
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| Cell Assay |
The cellular activity of SR-31747 is evaluated in lymphocyte proliferation assays. Primary lymphocytes are activated with mitogens (e.g., PHA or ConA) and treated with increasing concentrations of SR-31747. Cell proliferation is measured by [³H]-thymidine incorporation or by using a colorimetric cell proliferation assay. The effect on sterol isomerase activity can be assessed by measuring cholesterol biosynthesis intermediates.
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| Animal Protocol |
In animal models of inflammation, such as endotoxin shock, SR-31747 is administered via intraperitoneal or oral routes. Survival rates, inflammatory cytokine levels (e.g., TNF-α, IL-6), and organ pathology are assessed to evaluate the compound's anti-inflammatory efficacy.
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| ADME/Pharmacokinetics |
SR-31747 HCl has a molecular formula of C23H33Cl2N and a molecular weight of 394.42. Its CAS Type 1 name is Cyclohexanamine, N-((2Z)-3-(3-chloro-4-cyclohexylphenyl)-2-propen-1-yl)-N-ethyl-, hydrochloride (1:1). Specific pharmacokinetic parameters are not extensively detailed.
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| Toxicity/Toxicokinetics |
The toxicity profile of SR-31747 is not extensively documented. As an immunosuppressive agent, potential adverse effects may include increased susceptibility to infections. Specific LD50 values and organ-specific toxicity data are not readily available.
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| References |
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| Additional Infomation |
Arylacenamide (SR31747) is a peripheral σ ligand that binds to four proteins in human cells: SRBP-1, σ-2, HSI, and its associated protein SRBP-2. It is a drug with dual immunomodulatory and antiproliferative activities.
Drug Indications It has been investigated for the treatment of cancer/tumor (not specified), immunosuppression, and prostate cancer. Mechanism of Action SR31747 inhibits human lymphocyte proliferation, regulates the expression of pro-inflammatory and anti-inflammatory cytokines, and has been shown to protect animals in vivo from acute and chronic inflammation, such as acute graft-versus-host disease, lethal infections induced by staphylococcal enterotoxin B and lipopolysaccharide, or rheumatoid arthritis. In addition to these immunomodulatory activities, this molecule also inhibits the proliferation of various tumor cell lines in vitro in a time- and concentration-dependent manner. SR-31747 HCl (CAS# 132173-07-0) is a peripheral sigma receptor ligand with immunosuppressive and anti-inflammatory properties. It inhibits sterol isomerase and blocks cell proliferation. The compound is a research tool for studying sigma receptor biology, immunosuppression, and inflammation. |
| Molecular Formula |
C23H34NCL.HCL
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|---|---|
| Molecular Weight |
396.4367
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| Exact Mass |
395.215
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| CAS # |
132173-07-0
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| Related CAS # |
SR-31747 free base;132173-06-9
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| PubChem CID |
6439330
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| Appearance |
White to off-white solid powder
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| Boiling Point |
479.9ºC at 760 mmHg
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| Flash Point |
244.1ºC
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| Vapour Pressure |
2.26E-09mmHg at 25°C
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| LogP |
7.857
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
1
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
26
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| Complexity |
395
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CCN(C/C=C\C1=CC(=C(C=C1)C2CCCCC2)Cl)C3CCCCC3.Cl
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| InChi Key |
HKHPCMBPASXYGP-KVVVOXFISA-N
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| InChi Code |
InChI=1S/C23H34ClN.ClH/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;1H/b10-9-;
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| Chemical Name |
N-[(Z)-3-(3-chloro-4-cyclohexylphenyl)prop-2-enyl]-N-ethylcyclohexanamine;hydrochloride
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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: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| 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 : ~15.62 mg/mL (~39.40 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1.56 mg/mL (3.94 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 15.6 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: ≥ 1.56 mg/mL (3.94 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 15.6 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: ≥ 1.56 mg/mL (3.94 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 | 2.5224 mL | 12.6122 mL | 25.2245 mL | |
| 5 mM | 0.5045 mL | 2.5224 mL | 5.0449 mL | |
| 10 mM | 0.2522 mL | 1.2612 mL | 2.5224 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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