SR 49059
Based on 3 publication(s) in Google Scholar
SR 49059 (SR-49059) is a potent, orally active, selective vasopressin V1a antagonist with a Ki vaule of 1.4 nM.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.33%
- No. CAS: 150375-75-0
- Fòrmula: C28H27Cl2N3O7S
- Peso molecular:620.50
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Almacenamiento:
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) SR 49059
MoreVer todos los productos específicos de isoformas Vasopressin Receptor
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Actividad biológica
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V1a Receptor |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO | IC50 |
13 nM
Compound: 1
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Antagonist activity at human V1A receptor expressed in CHO cells assessed as inhibition of AVP-induced intracellular calcium release after 30 seconds by FLIPR assay
Antagonist activity at human V1A receptor expressed in CHO cells assessed as inhibition of AVP-induced intracellular calcium release after 30 seconds by FLIPR assay
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[PMID: 21885275] |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male Wistar rats, weighing 300 to 350 g, cerebral focal ischemia model[2]
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Dosage:2 mg/kg and 30 mg/kg dissolved in 10% dimethyl sulfoxide
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Administration:Intraperitoneal injection, once
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Result:Significantly reduced infarction volume measured at 48 hours after the arterial occlusion. Reduced neurological deficits and ischemic brain edema.
Chemical Information
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No. CAS 150375-75-0
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Appearance Solid
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Peso molecular 620.50
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Fòrmula C28H27Cl2N3O7S
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Color White to off-white
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SMILES
ClC1=C([C@@]2(O)C3=CC(Cl)=CC=C3N(S(=O)(C4=CC(OC)=C(OC)C=C4)=O)[C@]2(C(N5[C@H](C(N)=O)CCC5)=O)[H])C=CC=C1
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
Publications (3)
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Journal Impact Factor
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Most Recent
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Nat Commun
Oxytocinergic input from the paraventricular nucleus to the nucleus accumbens core modulates methamphetamine-conditioned place preference. [Abstract]2025 May 23;16(1):4808. PMID: 40410135 -
Br J Pharmacol
Upregulation of the oxytocin receptors on peripheral sensory neurons mediated analgesia in chemotherapy-induced neuropathic pain. [Abstract]2023 Jul;180(13):1730-1747. PMID: 36702458 -
Solvente y solubilidad
DMSO : 100 mg/mL (161.16 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 (sealed storage, away from moisture and light). 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 (sealed storage, away from moisture and light). 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 (4.03 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. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
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.
Pureza y Documentación
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Ficha de datos (289 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Serradeil-Le Gal C, et al. Effect of SR-49059, a vasopressin V1a antagonist, on human vascular smooth muscle cells. Am J Physiol. 1995 Jan;268(1 Pt 2):H404-10. [Content Brief]
[2]. Shuaib A, et al. Effects of nonpeptide V(1) vasopressin receptor antagonist SR-49059 on infarction volume and recovery of function in a focal embolic stroke model. Stroke. 2002 Dec;33(12):3033-7. [Content Brief]
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 (sealed storage, away from moisture and light). 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 | 1.6116 mL | 8.0580 mL | 16.1160 mL | 40.2901 mL |
| 5 mM | 0.3223 mL | 1.6116 mL | 3.2232 mL | 8.0580 mL | |
| 10 mM | 0.1612 mL | 0.8058 mL | 1.6116 mL | 4.0290 mL | |
| 15 mM | 0.1074 mL | 0.5372 mL | 1.0744 mL | 2.6860 mL | |
| 20 mM | 0.0806 mL | 0.4029 mL | 0.8058 mL | 2.0145 mL | |
| 25 mM | 0.0645 mL | 0.3223 mL | 0.6446 mL | 1.6116 mL | |
| 30 mM | 0.0537 mL | 0.2686 mL | 0.5372 mL | 1.3430 mL | |
| 40 mM | 0.0403 mL | 0.2015 mL | 0.4029 mL | 1.0073 mL | |
| 50 mM | 0.0322 mL | 0.1612 mL | 0.3223 mL | 0.8058 mL | |
| 60 mM | 0.0269 mL | 0.1343 mL | 0.2686 mL | 0.6715 mL | |
| 80 mM | 0.0201 mL | 0.1007 mL | 0.2015 mL | 0.5036 mL | |
| 100 mM | 0.0161 mL | 0.0806 mL | 0.1612 mL | 0.4029 mL |
SR 49059 Related Classifications
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