MB-07811
Based on 1 Customer Validation
MB-07811 (VK-2809) is an orally active HepDirect prodrug of MB07344, a liver-targeted thyroid hormone receptor-β agonist. MB-07811 has cholesterol and triglycerides lowering activity.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 99.75%
- CAS. Nr.: 852948-13-1
- Formel: C28H32ClO5P
- Molecular Weight:514.98
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Speicherung: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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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
Biologische Aktivität
Thyroid hormone receptor-β[2]
MB-07811 (VK-2809) is potential for liver targeting with a low affinity for thyroid hormone receptors (TRβ Ki=14.6 ± 0.5 μM; TRα Ki=12.5 ± 0.6 μM)[2].
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.
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Animal Model:4-week-old male C57BL/6 mice (diet-induced obese (DIO) mice)[2]
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Dosage:0.3 mg/kg, 1 mg/kg, 3 mg/kg, 10 mg/kg, 30 mg/kg
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Administration:Orally once daily; 14 days
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Result:Reduced total plasma cholesterol, and reduced plasma triglycerides (40%) at the highest doses.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS. Nr. 852948-13-1
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Appearance Solid
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Molecular Weight 514.98
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Formel C28H32ClO5P
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Color White to off-white
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SMILES
OC1=CC=C(CC2=C(C)C=C(OC[P@]3(OCC[C@@H](C4=CC=CC(Cl)=C4)O3)=O)C=C2C)C=C1C(C)C
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Synonyms
VK-2809
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Lösungsmittel & Löslichkeit
DMSO : 250 mg/mL (485.46 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.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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: ≥ 2.08 mg/mL (4.04 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
Reinheit & Dokumentation
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Data Sheet (271 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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Handling Instructions (2659 KB)
Verweise
[1]. Cable EE, et al. Reduction of hepatic steatosis in rats and mice after treatment with aliver-targeted thyroidhormone receptor agonist. Hepatology. 2009 Feb;49(2):407-17. [Content Brief]
[2]. Erion MD, et al. Targeting thyroid hormone receptor-beta agonists to the liver reduces cholesterol and triglycerides and improves the therapeutic index. Proc Natl Acad Sci U S A. 2007 Sep 25;104(39):15490-5. [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. 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 |
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| DMSO | 1 mM | 1.9418 mL | 9.7091 mL | 19.4182 mL | 48.5456 mL |
| 5 mM | 0.3884 mL | 1.9418 mL | 3.8836 mL | 9.7091 mL | |
| 10 mM | 0.1942 mL | 0.9709 mL | 1.9418 mL | 4.8546 mL | |
| 15 mM | 0.1295 mL | 0.6473 mL | 1.2945 mL | 3.2364 mL | |
| 20 mM | 0.0971 mL | 0.4855 mL | 0.9709 mL | 2.4273 mL | |
| 25 mM | 0.0777 mL | 0.3884 mL | 0.7767 mL | 1.9418 mL | |
| 30 mM | 0.0647 mL | 0.3236 mL | 0.6473 mL | 1.6182 mL | |
| 40 mM | 0.0485 mL | 0.2427 mL | 0.4855 mL | 1.2136 mL | |
| 50 mM | 0.0388 mL | 0.1942 mL | 0.3884 mL | 0.9709 mL | |
| 60 mM | 0.0324 mL | 0.1618 mL | 0.3236 mL | 0.8091 mL | |
| 80 mM | 0.0243 mL | 0.1214 mL | 0.2427 mL | 0.6068 mL | |
| 100 mM | 0.0194 mL | 0.0971 mL | 0.1942 mL | 0.4855 mL |
MB-07811 Related Classifications
HY-111288 Related Classifications
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