2. Metabolic Enzyme/Protease
  3. FXR
  4. NDB

NDB is a selective human FXRα (hFXRα) antagonist that is effective in modulating transcription of FXRα downstream genes. NDB can be used in anti-diabetes research.

For research use only. We do not sell to patients.

NDB Chemical Structure

NDB Chemical Structure

CAS No. : 1660153-08-1

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Based on 1 publication(s) in Google Scholar

NDB Related Antibodies

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  • Biological Activity

  • Purity & Documentation

  • References

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Description

NDB is a selective human FXRα (hFXRα) antagonist that is effective in modulating transcription of FXRα downstream genes. NDB can be used in anti-diabetes research[1].

IC50 & Target

Human FXRα (hFXRα)[1]
In Vitro

NDB induces rearrangements of helix 11 (H11) and helix 12 (H12, AF-2) by forming a homodimer of hFXRα-LBD, totally different from the active conformation in monomer state[1].
NDB (25 μM) effectively antagonizes the GW4064-stimulated FXR/RXR interaction and FXRα target gene expression in primary mouse hepatocytes, including the small heterodimer partner (SHP) and bile-salt export pump (BSEP)[1].

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

NDB Related Antibodies
In Vivo

NDB (24 mg/kg; intraperitoneal injection; once a day; for 4 weeks) efficiently decreases the gene expressions of phosphoenolpyruvate carboxykinase (PEPCK), glucose 6-phosphatase (G6-pase), small heterodimer partner, and BSEP in db/db mice[1].

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

Animal Model: Male C57BL/6J db/db mice (8 weeks of age)[1]
Dosage: 24 mg/kg
Administration: Intraperitoneal injection; once a day; for 4 weeks
Result: Decreased the gene expressions of PEPCK, G6-pase, small heterodimer partner, and BSEP.
Molecular Weight

471.42

Formula

C26H28Cl2N2O2
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(N(C1=CC=C(O)C(C(C)(C)C)=C1)CC2=CC=CC=C2)C3=C(Cl)C=C(N(C)C)C=C3Cl
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (212.13 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 2.1213 mL 10.6063 mL 21.2125 mL
5 mM 0.4243 mL 2.1213 mL 4.2425 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.

  • Molarity Calculator

  • Dilution Calculator

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

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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

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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    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (5.30 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 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 (25.0 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.
Purity & Documentation
References

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 2.1213 mL 10.6063 mL 21.2125 mL 53.0313 mL
5 mM 0.4243 mL 2.1213 mL 4.2425 mL 10.6063 mL
10 mM 0.2121 mL 1.0606 mL 2.1213 mL 5.3031 mL
15 mM 0.1414 mL 0.7071 mL 1.4142 mL 3.5354 mL
20 mM 0.1061 mL 0.5303 mL 1.0606 mL 2.6516 mL
25 mM 0.0849 mL 0.4243 mL 0.8485 mL 2.1213 mL
30 mM 0.0707 mL 0.3535 mL 0.7071 mL 1.7677 mL
40 mM 0.0530 mL 0.2652 mL 0.5303 mL 1.3258 mL
50 mM 0.0424 mL 0.2121 mL 0.4243 mL 1.0606 mL
60 mM 0.0354 mL 0.1768 mL 0.3535 mL 0.8839 mL
80 mM 0.0265 mL 0.1326 mL 0.2652 mL 0.6629 mL
100 mM 0.0212 mL 0.1061 mL 0.2121 mL 0.5303 mL
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NDB Related Classifications

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.

Keywords:

NDB1660153-08-1FXRNR1H4anti-diabetes effectFXRαFXRα downstream genesInhibitorinhibitorinhibit

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