Saredutant
Based on 4 publication(s) in Google Scholar
Saredutant is a selective NK2 receptor antagonist.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 98.09%
- CAS. Nr.: 142001-63-6
- Formel: C31H35Cl2N3O2
- Molecular Weight:552.53
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Protokoll
- Reinheit & Dokumentation
- Verweise
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Publications Citing Use of MedChemExpress (MCE) Saredutant
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Biologische Aktivität
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NK2R |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO | IC50 |
0.13 nM
Compound: SR-48968
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Inhibition of cloned human NK2 (Neurokinin 2) receptor, stably expressed in chinese hamster ovary (CHO) cells was determined
Inhibition of cloned human NK2 (Neurokinin 2) receptor, stably expressed in chinese hamster ovary (CHO) cells was determined
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[PMID: 9873524] |
| CHO | IC50 |
0.8 nM
Compound: (+/-)-1
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Binding affinity was determined against human NK2 receptor in CHO cells using [125I]neurokinin A as radioligand
Binding affinity was determined against human NK2 receptor in CHO cells using [125I]neurokinin A as radioligand
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10.1016/0960-894X(96)00075-3 |
| CHO | IC50 |
800 nM
Compound: SR-48968
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Inhibition of cloned human NK1 (Neurokinin 1) receptor, stably expressed in chinese hamster ovary (CHO) cells was determined
Inhibition of cloned human NK1 (Neurokinin 1) receptor, stably expressed in chinese hamster ovary (CHO) cells was determined
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[PMID: 9873524] |
| IM-9 | IC50 |
593 nM
Compound: SR-48968
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Binding affinity against Neurokinin 1(NK1) receptor from human IM-9 cells using [I]-Bolton Hunter labeled SP
Binding affinity against Neurokinin 1(NK1) receptor from human IM-9 cells using [I]-Bolton Hunter labeled SP
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10.1016/0960-894X(96)00148-5 |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS. Nr. 142001-63-6
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Appearance Solid
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Molecular Weight 552.53
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Formel C31H35Cl2N3O2
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Color White to off-white
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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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Synonyms
SR 48968; SR 48968C
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (4)
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Journal Impact Factor
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Most Recent
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Nature
2024 Nov;635(8040):987-1000. PMID: 39537932 -
Free Radic Biol Med
H2O2 enhances the spontaneous phasic contractions of isolated human-bladder strips via activation of TRPA1 channels on sensory nerves and the release of substance P and PGE2. [Abstract]2023 Oct 5;209(Pt 1):1-8. PMID: 37802373 -
Respir Physiol Neurobiol
Neurokinin 1 and 2 receptors are involved in PGE2- and citric acid-induced cough and ventilatory responses. [Abstract]2022 Dec:306:103952. PMID: 35905863 -
Lösungsmittel & Löslichkeit
DMSO : 250 mg/mL (452.46 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (3.76 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (3.76 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protokoll
Rats[1]
In the first experiment the dose-related effects of Saredutant are investigated. The Flinders Sensitive Line (FSL) rats (n=8) are treated with one of the following: vehicle (carboxymethylcellulose-CMC) or 1, 3, or 10 mg/kg Saredutant, or 5 mg/kg Desipramine as a positive control. Saredutant is injected at 1 mL/kg. The Flinders Resistant Line (FRL) rats are given CMC or 3 mg/kg Saredutant. All injections are i.p. and are given for 14 consecutive days. Approximately 22 h after the last injections the rats are placed in the social interaction chamber with similarly treated rats for a 5-min recording. Then about 2 h later the rats are individually tested in the forced swim test for a single 5-min session[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Reinheit & Dokumentation
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Data Sheet (275 KB)
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SDS (419 KB)
- English - EN (419 KB)
- Français - FR (419 KB)
- Deutsch - DE (419 KB)
- Norwegian - NO (419 KB)
- Español - ES (419 KB)
- Swedish - SV (419 KB)
- Italian - IT (419 KB)
- Korean - KR (419 KB)
- Portuguese - PT (419 KB)
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Handling Instructions (2659 KB)
Verweise
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.8099 mL | 9.0493 mL | 18.0986 mL | 45.2464 mL |
| 5 mM | 0.3620 mL | 1.8099 mL | 3.6197 mL | 9.0493 mL | |
| 10 mM | 0.1810 mL | 0.9049 mL | 1.8099 mL | 4.5246 mL | |
| 15 mM | 0.1207 mL | 0.6033 mL | 1.2066 mL | 3.0164 mL | |
| 20 mM | 0.0905 mL | 0.4525 mL | 0.9049 mL | 2.2623 mL | |
| 25 mM | 0.0724 mL | 0.3620 mL | 0.7239 mL | 1.8099 mL | |
| 30 mM | 0.0603 mL | 0.3016 mL | 0.6033 mL | 1.5082 mL | |
| 40 mM | 0.0452 mL | 0.2262 mL | 0.4525 mL | 1.1312 mL | |
| 50 mM | 0.0362 mL | 0.1810 mL | 0.3620 mL | 0.9049 mL | |
| 60 mM | 0.0302 mL | 0.1508 mL | 0.3016 mL | 0.7541 mL | |
| 80 mM | 0.0226 mL | 0.1131 mL | 0.2262 mL | 0.5656 mL | |
| 100 mM | 0.0181 mL | 0.0905 mL | 0.1810 mL | 0.4525 mL |
Saredutant Related Classifications
HY-106910 Related Classifications
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