GR103545 fumarate
GR103545 fumarate is a κ opioid receptor (KOR) selective PET radiotracer and functional agonist with blood-brain barrier permeability and comparable peripheral and central antinociceptive efficacy, with an IC50 of 0.02 nM for KOR agonistic activity. GR103545 fumarate selectively binds to KORs in the brain. GR103545 fumarate induces antinociceptive effects. GR103545 fumarate can be used in research related to neurological disorders such as depression and Alzheimer's disease.
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- No. CAS: 126766-43-6
- Fòrmula: C23H29Cl2N3O7
- Peso molecular:530.40
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Almacenamiento:
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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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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Actividad biológica
Descripciòn
IC50 & Target
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κ Opioid Receptor/KOR 0.02 nM (IC50) |
In Vivo
GR103545 (compound 2) (in vitro rabbit vas deferens tissue) fumarate acts as potent competitive kappa opioid receptor (KOR) agonist with IC50 = 0.02 nM and Log D = 3.14; its s.c./i.c.v. antinociceptive potency ratio is 1.5, showing strong blood-brain barrier penetration[2].
11C-GR103545 (i.v.; bolus injection) fumarate exhibits specific, KOR-selective binding in healthy rhesus monkey brain with high BPND values but slow tissue kinetics that delay equilibrium[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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No. CAS 126766-43-6
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Appearance Solid
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Peso molecular 530.40
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Fòrmula C23H29Cl2N3O7
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Color White to off-white
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SMILES
OC(/C=C/C(O)=O)=O.ClC(C=C1CC(N2[C@@H](CN(CC2)C(OC)=O)CN3CCCC3)=O)=C(C=C1)Cl
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvente y solubilidad
In Vitro:
DMSO : 100 mg/mL (188.54 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). 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). 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)
In Vivo:
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 (4.71 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 (4.71 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.
In Vivo Dissolution Calculator
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)
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 (274 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Placzek MS, et al. Immediate and Persistent Effects of Salvinorin A on the Kappa Opioid Receptor in Rodents, Monitored In Vivo with PET. Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology. 2015 Dec;40(13):2865-72. [Content Brief]
[3]. Li S, et al. Development and In Vivo Evaluation of a κ-Opioid Receptor Agonist as a PET Radiotracer with Superior Imaging Characteristics. Journal of nuclear medicine : official publication, Society of Nuclear Medicine. 2019 Jul;60(7):1023-1030. [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). 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 | 1.8854 mL | 9.4268 mL | 18.8537 mL | 47.1342 mL |
| 5 mM | 0.3771 mL | 1.8854 mL | 3.7707 mL | 9.4268 mL | |
| 10 mM | 0.1885 mL | 0.9427 mL | 1.8854 mL | 4.7134 mL | |
| 15 mM | 0.1257 mL | 0.6285 mL | 1.2569 mL | 3.1423 mL | |
| 20 mM | 0.0943 mL | 0.4713 mL | 0.9427 mL | 2.3567 mL | |
| 25 mM | 0.0754 mL | 0.3771 mL | 0.7541 mL | 1.8854 mL | |
| 30 mM | 0.0628 mL | 0.3142 mL | 0.6285 mL | 1.5711 mL | |
| 40 mM | 0.0471 mL | 0.2357 mL | 0.4713 mL | 1.1784 mL | |
| 50 mM | 0.0377 mL | 0.1885 mL | 0.3771 mL | 0.9427 mL | |
| 60 mM | 0.0314 mL | 0.1571 mL | 0.3142 mL | 0.7856 mL | |
| 80 mM | 0.0236 mL | 0.1178 mL | 0.2357 mL | 0.5892 mL | |
| 100 mM | 0.0189 mL | 0.0943 mL | 0.1885 mL | 0.4713 mL |
GR103545 fumarate Related Classifications
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