SRX246
Based on 1 Customer Validation
SRX246 is a potent, BBB-penetrant, highly selective vasopressin 1a (V1a) receptor antagonist (Ki=0.3 nM for human V1a). SRX246 has no interaction at V1b and V2 receptors. SRX246 also displays negligible binding at 64 others receptors classes, including 35 G-proteincoupled receptors. SRX246 can be used for treatment of stress-related disorders.
For research use only. We do not sell to patients.
- Purity: 99.76%
- CAS No.: 512784-93-9
- Formula: C42H49N5O5
- Molecular Weight:703.87
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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All Vasopressin Receptor Isoforms
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Biological Activity
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V1a Receptor |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male Sprague-Dawley rats[1]
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Dosage:2 mg/kg (20 mg/kg for p.o.)
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Administration:i.v. (Pharmacokinetic Analysis)
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Result:Following i.v. administration, the plasma concentration declined steadily with a half-life (t1/2) of 6 hours. The Cmax and AUC0-∞ values are 953 ng/mL, 1141 ng ▪h/mL, 6.02 hours. Following an oral administration, the Cmax, AUC0-∞ and t1/2 values 98.4 ng/mL, 624 ng ▪h/mL and 2.38 hours, respectively.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 512784-93-9
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Appearance Solid
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Molecular Weight 703.87
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Formula C42H49N5O5
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Color White to off-white
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SMILES
O=C(N1CCC(N2CCCCC2)CC1)C[C@H](C(N[C@@H](C3=CC=CC=C3)C)=O)N4[C@@H]([C@H](N5[C@@H](C6=CC=CC=C6)COC5=O)C4=O)/C=C/C7=CC=CC=C7
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Solvent & Solubility
DMSO : 100 mg/mL (142.07 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.
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 (3.55 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.
Purity & Documentation
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Data Sheet (281 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
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Handling Instructions (2659 KB)
References
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 |
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| DMSO | 1 mM | 1.4207 mL | 7.1036 mL | 14.2072 mL | 35.5179 mL |
| 5 mM | 0.2841 mL | 1.4207 mL | 2.8414 mL | 7.1036 mL | |
| 10 mM | 0.1421 mL | 0.7104 mL | 1.4207 mL | 3.5518 mL | |
| 15 mM | 0.0947 mL | 0.4736 mL | 0.9471 mL | 2.3679 mL | |
| 20 mM | 0.0710 mL | 0.3552 mL | 0.7104 mL | 1.7759 mL | |
| 25 mM | 0.0568 mL | 0.2841 mL | 0.5683 mL | 1.4207 mL | |
| 30 mM | 0.0474 mL | 0.2368 mL | 0.4736 mL | 1.1839 mL | |
| 40 mM | 0.0355 mL | 0.1776 mL | 0.3552 mL | 0.8879 mL | |
| 50 mM | 0.0284 mL | 0.1421 mL | 0.2841 mL | 0.7104 mL | |
| 60 mM | 0.0237 mL | 0.1184 mL | 0.2368 mL | 0.5920 mL | |
| 80 mM | 0.0178 mL | 0.0888 mL | 0.1776 mL | 0.4440 mL | |
| 100 mM | 0.0142 mL | 0.0710 mL | 0.1421 mL | 0.3552 mL |
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