TAN-452
Based on 1 Customer Validation
TAN-452 is an orally active, selective peripherally acting δ-opioid receptor (DOR) antagonist with a Ki of 0.47 nM and a Kb of 0.21 nM. TAN-452 is an antagonist for μ-opioid receptor (MOR; Ki=36.56 nM and Kb=9.43 nM) and κ-opioid receptor (KOR; Ki=5.31 nM and Kb=7.18 nM). TAN-452, a derivative of Naltrindole, demonstrates low brain penetrability and attenuates morphine-induced side effects without affecting pain control.
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- Pureté: 99.16%
- CAS No.: 892039-23-5
- Formule: C29H30N2O5
- Masse moléculaire:486.56
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
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δ Opioid Receptor/DOR |
TAN-452 (30 mg/kg/2 mL for PO or 3 mg/kg/mL for IV) has a T1/2 of 2.1 hours[1].
TAN-452 suppresses morphine-induced small intestinal transit (SIT) inhibition in a dose-dependent manner. Administration of TAN-452 at 30 mg/kg alone does not affect SIT[1].
TAN-452 (10, 30 mg/kg; s.c.) significantly suppresses morphine-induced antinociception 30 min after administration. TAN-452 (po) produces no effect up to 300 mg/kg[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male ferrets (1.3-1.9 kg)[1]
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Dosage:1, 3, 10 mg/kg (p.o.) or 0.3, 1, 3 mg/kg (s.c.)
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Administration:PO or SC; before morphine
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Result:Prevented morphine-induced emesis in half of the animals with orally administered of 1 mg/kg and completely abolished emesis at 3 and 10 mg/kg.
Completely abolished emesis by subcutaneous injection at 0.3, 1, and 3 mg/kg.
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Animal Model:Crj:CD(SD) IGS male rats (7 weeks old)[1]
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Dosage:30 mg/kg/2 mL for PO or 3 mg/kg/mL for IV (Pharmacokinetic Analysis)
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Administration:Orally or intravenously
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Result:Had a T1/2 of 2.1 hours, a CL of 78.1 mL/min•kg, a Vss of 12.1 L/kg, and a Cmax of 526 ng/mL.
Chemical Information
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CAS No. 892039-23-5
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Appearance Solid
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Masse moléculaire 486.56
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Formule C29H30N2O5
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Color White to off-white
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SMILES
O=C(C1=CC2=C(C=C1)C3=C([C@@](OC4=C(O)C=CC(C5)=C46)([H])[C@]76[C@@]([C@]5([H])N(CC8CC8)CC7)(O)C3)N2)OCC
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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 6 months -20°C 1 month
Solvant et solubilité
DMSO : 100 mg/mL (205.52 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 (5.14 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 (5.14 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.
Pureté et documentation
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Fiche technique (280 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 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 | 2.0552 mL | 10.2762 mL | 20.5524 mL | 51.3811 mL |
| 5 mM | 0.4110 mL | 2.0552 mL | 4.1105 mL | 10.2762 mL | |
| 10 mM | 0.2055 mL | 1.0276 mL | 2.0552 mL | 5.1381 mL | |
| 15 mM | 0.1370 mL | 0.6851 mL | 1.3702 mL | 3.4254 mL | |
| 20 mM | 0.1028 mL | 0.5138 mL | 1.0276 mL | 2.5691 mL | |
| 25 mM | 0.0822 mL | 0.4110 mL | 0.8221 mL | 2.0552 mL | |
| 30 mM | 0.0685 mL | 0.3425 mL | 0.6851 mL | 1.7127 mL | |
| 40 mM | 0.0514 mL | 0.2569 mL | 0.5138 mL | 1.2845 mL | |
| 50 mM | 0.0411 mL | 0.2055 mL | 0.4110 mL | 1.0276 mL | |
| 60 mM | 0.0343 mL | 0.1713 mL | 0.3425 mL | 0.8564 mL | |
| 80 mM | 0.0257 mL | 0.1285 mL | 0.2569 mL | 0.6423 mL | |
| 100 mM | 0.0206 mL | 0.1028 mL | 0.2055 mL | 0.5138 mL |
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