Fuscoside
Based on 1 publication(s) in Google Scholar
Fuscoside (OPC-21268) is an orally effective, nonpeptide, vasopressin V1 receptor antagonist with an IC50 of 0.4 μM.
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- Pureté: ≥98.0%
- CAS No.: 131631-89-5
- Formule: C26H31N3O4
- Masse moléculaire:449.54
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Fuscoside
MoreVoir tous les produits spécifiques à Isoform Vasopressin Receptor
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Activité biologique
IC50: 0.4 μM (vasopressin V1)
Ki: 0.14 μM (vasopressin V1)[1]
The concentration of Fuscoside (OPC-21268) that displaces 50% of specific AVP binding (IC50) is 0.4 μM for VI receptors and 100 μM for V2 receptors. The inhibition constant (Ki) of Fuscoside (OPC-21268) for V1 receptors (0.14 μM)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 131631-89-5
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Appearance Solid
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Masse moléculaire 449.54
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Formule C26H31N3O4
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Color White to off-white
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SMILES
O=C(CC1)N(C2CCN(C(C3=CC=C(OCCCNC(C)=O)C=C3)=O)CC2)C4=C1C=CC=C4
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Synonyms
OPC-21268
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (1)
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Journal Impact Factor
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Most Recent
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Cell J
Fuscoside Attenuates Bone Loss in Bone Defects by Regulating The Rankl/Nlrp3/Opg Pathway in Rats. [Abstract]2021 Sep;23(4):451-456. PMID: 34455721
Solvant et solubilité
DMSO : 50 mg/mL (111.22 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 (5.56 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (5.56 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 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.
Protocole
Rats[1]
Male Sprague-Dawley rats, 300 to 400 g, are injected with Fuscoside (OPC-21268) (0.1, 0.3, 1 mg/kg). Fuscoside (OPC-21268) is given 2 min before the injection of AVP at 30 mU/kg i.v., angiotensin II at 0.3 μg/kg i.v., and noradrenaline at 3 μg/kg i.v.[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureté et documentation
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Fiche technique (271 KB)
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SDS (597 KB)
- English - EN (597 KB)
- Français - FR (597 KB)
- Deutsch - DE (597 KB)
- Norwegian - NO (597 KB)
- Español - ES (597 KB)
- Swedish - SV (597 KB)
- Italian - IT (597 KB)
- Korean - KR (597 KB)
- Portuguese - PT (597 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Yamamura Y, et al. OPC-21268, an orally effective, nonpeptide vasopressin V1 receptor antagonist. Science. 1991 Apr 26;252(5005):572-4. [Content Brief]
[2]. Bemana I, et al. Treatment of brain edema with a nonpeptide arginine vasopressin V1 receptor antagonist OPC-21268 in rats. Neurosurgery. 1999 Jan;44(1):148-54. [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, 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 | 2.2245 mL | 11.1225 mL | 22.2450 mL | 55.6124 mL |
| 5 mM | 0.4449 mL | 2.2245 mL | 4.4490 mL | 11.1225 mL | |
| 10 mM | 0.2224 mL | 1.1122 mL | 2.2245 mL | 5.5612 mL | |
| 15 mM | 0.1483 mL | 0.7415 mL | 1.4830 mL | 3.7075 mL | |
| 20 mM | 0.1112 mL | 0.5561 mL | 1.1122 mL | 2.7806 mL | |
| 25 mM | 0.0890 mL | 0.4449 mL | 0.8898 mL | 2.2245 mL | |
| 30 mM | 0.0741 mL | 0.3707 mL | 0.7415 mL | 1.8537 mL | |
| 40 mM | 0.0556 mL | 0.2781 mL | 0.5561 mL | 1.3903 mL | |
| 50 mM | 0.0445 mL | 0.2224 mL | 0.4449 mL | 1.1122 mL | |
| 60 mM | 0.0371 mL | 0.1854 mL | 0.3707 mL | 0.9269 mL | |
| 80 mM | 0.0278 mL | 0.1390 mL | 0.2781 mL | 0.6952 mL | |
| 100 mM | 0.0222 mL | 0.1112 mL | 0.2224 mL | 0.5561 mL |
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