1. Metabolic Enzyme/Protease Vitamin D Related/Nuclear Receptor
  2. LXR
  3. BMS-779788

BMS-779788  (Synonyms: EXEL04286652; XL-652; BMS-788)

Cat. No.: HY-19919 Purity: 99.86%
COA Handling Instructions

BMS-779788 is a LXR partial agonist with IC50 values of 68 nM for LXRα and 14 nM for LXRβ.

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

BMS-779788 Chemical Structure

BMS-779788 Chemical Structure

CAS No. : 918348-67-1

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 73 In-stock
Solution
10 mM * 1 mL in DMSO USD 73 In-stock
Solid
5 mg USD 65 In-stock
10 mg USD 95 In-stock
25 mg USD 195 In-stock
50 mg USD 320 In-stock
100 mg USD 500 In-stock
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 1 publication(s) in Google Scholar

Top Publications Citing Use of Products

1 Publications Citing Use of MCE BMS-779788

  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

BMS-779788 is a LXR partial agonist with IC50 values of 68 nM for LXRα and 14 nM for LXRβ.

IC50 & Target

IC50: 68 nM (LXRα); 14 nM (LXRβ)[1]

In Vitro

The LXR selective partial agonist BMS-779788 is identified with potent induction of ATP binding transporters ABCA1 and ABCG1 in human whole blood (EC50=1.2 μM, 55% efficacy)[2].

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

In Vivo

BMS-779788 induces LXR target genes in blood in vivo with an EC50=610 nM, a value similar to its in vitro blood gene induction potency. BMS-779788 is 29- and 12-fold less potent than the full agonist T0901317 in elevating plasma triglyceride and LDL cholesterol, respectively, with similar results for plasma cholesteryl ester transfer protein and apolipoprotein B[1]. In mice BMS-779788 displays peripheral induction of ABCA1 at 3 and 10 mpk doses with no significant elevation of plasma or hepatic triglycerides at these doses, showing an improved profile compared to a full pan-agonist[2].

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

Clinical Trial
Molecular Weight

509.06

Formula

C28H29ClN2O3S

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

OC(C)(C)C1=CN(C2=CC=C(C3=CC=CC(S(=O)(C)=O)=C3)C=C2)C(C(C)(C4=CC=CC=C4Cl)C)=N1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (196.44 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 1.9644 mL 9.8220 mL 19.6440 mL
5 mM 0.3929 mL 1.9644 mL 3.9288 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

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: 2.5 mg/mL (4.91 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    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.
  • Protocol 2

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

    Solubility: ≥ 2.5 mg/mL (4.91 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
Animal Administration
[1]

Monkeys: Male cynomolgus monkeys are used in the study. For a single-dose pharmacokinetic (PK)-pharmacodynamic (PD) study, 2 animals each are treated either with vehicle [0.5% carboxymethyl cellulose and 2% Tween 80 in purified water) or 1 mg/kg BMS-779788. For the 7 day PD study, 18 animals are randomized into 6 treatment groups (N=3/group; 3-6 kg) and received the following treatments at 7 AM daily for 7 days by oral gavage: vehicle, 10 mg/kg per day T0901317 and 0.3, 1, 3, or 10 mg/kg per day BMS-779788[1].

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

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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.9644 mL 9.8220 mL 19.6440 mL 49.1101 mL
5 mM 0.3929 mL 1.9644 mL 3.9288 mL 9.8220 mL
10 mM 0.1964 mL 0.9822 mL 1.9644 mL 4.9110 mL
15 mM 0.1310 mL 0.6548 mL 1.3096 mL 3.2740 mL
20 mM 0.0982 mL 0.4911 mL 0.9822 mL 2.4555 mL
25 mM 0.0786 mL 0.3929 mL 0.7858 mL 1.9644 mL
30 mM 0.0655 mL 0.3274 mL 0.6548 mL 1.6370 mL
40 mM 0.0491 mL 0.2456 mL 0.4911 mL 1.2278 mL
50 mM 0.0393 mL 0.1964 mL 0.3929 mL 0.9822 mL
60 mM 0.0327 mL 0.1637 mL 0.3274 mL 0.8185 mL
80 mM 0.0246 mL 0.1228 mL 0.2456 mL 0.6139 mL
100 mM 0.0196 mL 0.0982 mL 0.1964 mL 0.4911 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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Product Name:
BMS-779788
Cat. No.:
HY-19919
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