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| 1mg |
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| Targets |
Saredutant targets the neurokinin-2 (NK2) receptor, a G protein-coupled receptor that is activated by the neuropeptide neurokinin A (NKA). NK2 receptors are widely expressed in the respiratory tract, gastrointestinal tract, and central nervous system. Activation of NK2 receptors by NKA mediates various effects, including smooth muscle contraction, mucus secretion, and inflammation. Saredutant is a potent and selective NK2 receptor antagonist. By blocking NK2 receptors, Saredutant inhibits NKA-mediated bronchoconstriction, mucus secretion, and inflammation, making it a potential therapeutic agent for respiratory and gastrointestinal disorders.
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| ln Vitro |
In vitro, Saredutant is a potent and selective NK2 receptor antagonist. Its activity is typically measured using receptor binding assays and functional assays. Receptor binding assays determine the compound's affinity (Ki) for the NK2 receptor. Functional assays measure the compound's ability to inhibit NKA-induced signaling, such as calcium mobilization or smooth muscle contraction. These in vitro studies confirm Saredutant's activity as a NK2 receptor antagonist.
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| ln Vivo |
In animal models of depression, serodutant, an NK2 receptor antagonist, has synergistic effects with desipramine and antidepressant-like effects. The effect of saredutant on immobility during swimming tests varies with dose; immobility is not affected at low doses of 1 mg/kg, but is dramatically reduced at doses of 3 and 10 mg/kg [1].
In vivo, Saredutant has been shown to inhibit citric acid-induced airway hyperresponsiveness in guinea pigs. This finding supports its potential as a therapeutic agent for asthma and other respiratory diseases. Saredutant has been investigated in clinical trials for the treatment of asthma, COPD, and irritable bowel syndrome. However, its development may have been discontinued due to efficacy or safety concerns. Saredutant is a research compound that has been investigated in clinical trials. |
| Enzyme Assay |
In vitro receptor binding assays for Saredutant measure its affinity for the NK2 receptor. Membranes from cells expressing the NK2 receptor are incubated with a radiolabeled NK2 ligand and varying concentrations of Saredutant. The Ki is determined from competition binding curves. Functional assays measure the compound's ability to inhibit NKA-induced signaling in cells expressing the NK2 receptor. Calcium mobilization or cAMP accumulation assays are commonly used. These assays confirm Saredutant's activity as a NK2 receptor antagonist.
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| Cell Assay |
In vitro cell-based assays for Saredutant are used to study its effects on NK2 receptor signaling. Cells expressing the NK2 receptor are treated with NKA in the presence or absence of Saredutant. The inhibition of NKA-induced calcium mobilization or cAMP accumulation is measured. These assays confirm the compound's antagonist activity at the NK2 receptor.
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| Animal Protocol |
In vivo animal experiments for Saredutant have been conducted in guinea pig models of airway hyperresponsiveness. In a typical study, Saredutant is administered to guinea pigs, and airway responsiveness to citric acid is assessed. The compound's ability to inhibit airway hyperresponsiveness is measured. Saredutant has also been studied in animal models of gastrointestinal disorders. These studies confirm the in vivo efficacy of Saredutant as a NK2 receptor antagonist.
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| ADME/Pharmacokinetics |
Saredutant has a molecular weight of 552.53 g/mol and a molecular formula of C31H35Cl2N3O2. It has a CAS number of 142001-63-6. It is a solid compound. For storage, it is recommended to keep the powder at -20°C. Pharmacokinetic properties such as absorption, distribution, metabolism, and excretion (ADME) have been characterized in the context of clinical development. Saredutant is a small molecule drug that has been investigated in clinical trials.
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| Toxicity/Toxicokinetics |
Detailed toxicity data for Saredutant is not provided in standard product descriptions. As a compound that has been investigated in clinical trials, its safety profile has been evaluated in human studies. However, specific toxicity data, such as adverse effects or organ toxicity, are not detailed. As with all research chemicals, standard laboratory safety precautions should be followed when handling Saredutant. Its use is limited to research applications.
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| References | |
| Additional Infomation |
Saredutant (SR 48968) is a neurokinin-2 antagonist developed by Sanofi-Aventis and used as an antidepressant and anti-anxiety medication.
Drug Indications It is being investigated for the treatment of depression and anxiety disorders. Mechanism of Action Saredutant works by blocking the action of neurokinin A on NK-2 receptors. Saredutant (SR 48968) is a research compound that has been investigated for the treatment of respiratory and gastrointestinal disorders. It is a potent and selective non-peptide antagonist of the neurokinin-2 (NK2) receptor. Saredutant inhibits citric acid-induced airway hyperresponsiveness in guinea pigs. It has been investigated in clinical trials for the treatment of asthma, COPD, and irritable bowel syndrome. However, its development may have been discontinued. Saredutant is a valuable research tool for studying NK2 receptor function and its role in respiratory and gastrointestinal diseases. |
| Exact Mass |
551.211
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| CAS # |
142001-63-6
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| PubChem CID |
104974
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| Appearance |
White to off-white solid powder
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| Density |
1.26g/cm3
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| Boiling Point |
734.7ºC at 760mmHg
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| Flash Point |
398.1ºC
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| Vapour Pressure |
1.91E-21mmHg at 25°C
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| Index of Refraction |
1.628
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| LogP |
6.695
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
9
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| Heavy Atom Count |
38
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| Complexity |
760
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| Defined Atom Stereocenter Count |
1
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| SMILES |
CC(NC1(C2=CC=CC=C2)CCN(CC[C@@H](C3=CC(Cl)=C(Cl)C=C3)CN(C)C(C4=CC=CC=C4)=O)CC1)=O
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| InChi Key |
PGKXDIMONUAMFR-AREMUKBSSA-N
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| InChi Code |
InChI=1S/C31H35Cl2N3O2/c1-23(37)34-31(27-11-7-4-8-12-27)16-19-36(20-17-31)18-15-26(25-13-14-28(32)29(33)21-25)22-35(2)30(38)24-9-5-3-6-10-24/h3-14,21,26H,15-20,22H2,1-2H3,(H,34,37)/t26-/m1/s1
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| Chemical Name |
(S)-N-(4-(4-acetamido-4-phenylpiperidin-1-yl)-2-(3,4-dichlorophenyl)butyl)-N-methylbenzamide
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| Synonyms |
SR-48968 SR489686 SR 489686
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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 : ~250 mg/mL (~452.46 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (3.76 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 20.8 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: ≥ 2.08 mg/mL (3.76 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 20.8 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: ≥ 2.08 mg/mL (3.76 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT00429260 | COMPLETED | Drug: Saredutant | Depressive Disorder | Sanofi | 2007-01 | Phase 3 |
| NCT00250614 | COMPLETED | Drug: Saredutant succinate (SR48968C) | Depressive Disorder | Sanofi | 2005-04 | Phase 3 |
| NCT00250601 | COMPLETED | Drug: Saredutant succinate (SR48968C) | Depressive Disorder | Sanofi | 2005-04 | Phase 3 |
| NCT00390650 | COMPLETED | Drug: Saredutant | Anxiety | Sanofi | 2006-10 | Phase 3 |
| NCT00256113 | COMPLETED | Drug: Saredutant succinate (SR48968C) | Depressive Disorder | Sanofi | 2004-12 | Phase 3 |
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