Osanetant
Based on 1 Customer Validation
Osanetant (SR142801) is a selective NK3 receptor antagonist. Osanetant produces anxiolytic- and antidepressant-like effects and is researched for schizophrenia.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- Pureté: 98.11%
- CAS No.: 160492-56-8
- Formule: C35H41Cl2N3O2
- Masse moléculaire:606.62
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Stockage:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
Activité biologique
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NK3R |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO | IC50 |
0.21 nM
Compound: SR-142801
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Compound was tested for binding affinity against human Tachykinin receptor 3 in CHO cells
Compound was tested for binding affinity against human Tachykinin receptor 3 in CHO cells
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10.1016/0960-894X(95)00313-I |
| CHO | IC50 |
0.8 nM
Compound: SR-142801
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Tachykinin receptor 3 binding affinity was determined by incubation with CHO cells expressing human NK3 receptors
Tachykinin receptor 3 binding affinity was determined by incubation with CHO cells expressing human NK3 receptors
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10.1016/S0960-894X(97)00064-4 |
| HeLa | IC50 |
9.65 μM
Compound: Osanetant
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Inhibition of Ebolavirus glycoprotein/matrix protein VP40 entry in human HeLa cells after 4.5 hrs beta-lactamase reporter assay
Inhibition of Ebolavirus glycoprotein/matrix protein VP40 entry in human HeLa cells after 4.5 hrs beta-lactamase reporter assay
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[PMID: 29624387] |
Osanetant (ip; 5 and 10 mg/kg; 30 min before testing) decreases immobility time[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male Mongolian gerbils of 7 weeks old (50-60 g)[1]
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Dosage:1, 3 and 10 mg/kg
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Administration:Po; 60 min before testing
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Result:Significantly increased social interaction time.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 160492-56-8
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Appearance Solid
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Masse moléculaire 606.62
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Formule C35H41Cl2N3O2
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Color White to off-white
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SMILES
O=C(N1C[C@@](CCCN2CCC(N(C(C)=O)C)(C3=CC=CC=C3)CC2)(C4=CC=C(Cl)C(Cl)=C4)CCC1)C5=CC=CC=C5
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Synonyms
SR142801
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Solvant et solubilité
DMSO : 66.67 mg/mL (109.90 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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: ≥ 2.5 mg/mL (4.12 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
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.
Pureté et documentation
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Fiche technique (275 KB)
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SDS (392 KB)
- English - EN (392 KB)
- Français - FR (392 KB)
- Deutsch - DE (392 KB)
- Norwegian - NO (392 KB)
- Español - ES (392 KB)
- Swedish - SV (392 KB)
- Italian - IT (392 KB)
- Korean - KR (392 KB)
- Portuguese - PT (392 KB)
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Instruction de manipulation (2659 KB)
Références
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.6485 mL | 8.2424 mL | 16.4848 mL | 41.2120 mL |
| 5 mM | 0.3297 mL | 1.6485 mL | 3.2970 mL | 8.2424 mL | |
| 10 mM | 0.1648 mL | 0.8242 mL | 1.6485 mL | 4.1212 mL | |
| 15 mM | 0.1099 mL | 0.5495 mL | 1.0990 mL | 2.7475 mL | |
| 20 mM | 0.0824 mL | 0.4121 mL | 0.8242 mL | 2.0606 mL | |
| 25 mM | 0.0659 mL | 0.3297 mL | 0.6594 mL | 1.6485 mL | |
| 30 mM | 0.0549 mL | 0.2747 mL | 0.5495 mL | 1.3737 mL | |
| 40 mM | 0.0412 mL | 0.2061 mL | 0.4121 mL | 1.0303 mL | |
| 50 mM | 0.0330 mL | 0.1648 mL | 0.3297 mL | 0.8242 mL | |
| 60 mM | 0.0275 mL | 0.1374 mL | 0.2747 mL | 0.6869 mL | |
| 80 mM | 0.0206 mL | 0.1030 mL | 0.2061 mL | 0.5151 mL | |
| 100 mM | 0.0165 mL | 0.0824 mL | 0.1648 mL | 0.4121 mL |