1. Vitamin D Related/Nuclear Receptor
  2. Thyroid Hormone Receptor
  3. MB-07811

MB-07811  (Synonyms: VK-2809)

Cat. No.: HY-111288 Pureza: 99.75% ee.: 100.00%
Instrucciones de manejo Technical Support

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.

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MB-07811

MB-07811 Estructura química

No. CAS : 852948-13-1

Tamaño Precio Stock Cantidad
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
En stock
Solution
10 mM * 1 mL in DMSO En stock
Solid
1 mg En stock
5 mg En stock
10 mg En stock
25 mg En stock
50 mg   Obtener un presupuesto  
100 mg   Obtener un presupuesto  

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Descripciòn

MB-07811 (VK-2809) is an orally active HepDirect prodrug of MB07344, a liver-targeted thyroid hormone receptor-β agonist[1]. MB-07811 has cholesterol and triglycerides lowering activity[2].

IC50 & Target

Thyroid hormone receptor-β[2]

In Vitro

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.

In Vivo

MB-07811 (VK-2809) (0.3-30 mg/kg; orally once daily for 14 days) reduces cholesterol and triglycerides in diet-induced obese mice[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: 4-week-old male C57BL/6 mice (diet-induced obese (DIO) mice)[2]
Dosage: 0.3 mg/kg, 1 mg/kg, 3 mg/kg, 10 mg/kg, 30 mg/kg
Administration: Orally once daily; 14 days
Result: Reduced total plasma cholesterol, and reduced plasma triglycerides (40%) at the highest doses.
Ensayo clínico
Peso molecular

514.98

Fòrmula

C28H32ClO5P

No. CAS
Appearance

Solid

Color

White to off-white

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

Envío

Room temperature in continental US; may vary elsewhere.

Almacenamiento
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvente y solubilidad
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.9418 mL 9.7091 mL 19.4182 mL
5 mM 0.3884 mL 1.9418 mL 3.8836 mL
View the 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.

  • Calculadora de molaridad

  • Calculadora de dilución

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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.

  • Protocol 1

    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.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.08 mg/mL (4.04 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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

Purity: 99.75% ee.: 100.00%

Referencias

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 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
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Inquiry Information

Nombre del producto:
MB-07811
Cat. No.:
HY-111288
Cantidad:
MCE Japan Authorized Agent: