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

Name: BMS-779788
Brand: MedChemExpress
SKU: HY-19919
Rating: 5.0 (1 reviews)

Cat. No.: HY-19919 Purity: 99.86%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

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

CAS No. : 918348-67-1

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 73	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 73	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 65	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 95	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 195	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 320	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 500	In-stock	Estimated Time of Arrival: December 31
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Customer Review

Based on 1 publication(s) in Google Scholar

1 Publications Citing Use of MCE BMS-779788

•Radboud University Nijmegen. 2021 Mar.

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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]

Cellular Effect

Cell Line	Type	Value	Description	References
CV-1	EC₅₀	220 nM Compound: 5; BMS-779788	Agonist activity at human LXR-alpha expressed in African green monkey CV1 cells measured after 18 to 20 hrs by luciferase reporter gene assay Agonist activity at human LXR-alpha expressed in African green monkey CV1 cells measured after 18 to 20 hrs by luciferase reporter gene assay	[PMID: 27994765]
CV-1	EC₅₀	230 nM Compound: 18	Transactivation of LXRalpha (unknown origin) expressed in CV1 cells by luciferase reporter gene assay Transactivation of LXRalpha (unknown origin) expressed in CV1 cells by luciferase reporter gene assay	[PMID: 25435151]
CV-1	EC₅₀	250 nM Compound: 5; BMS-779788	Agonist activity at human LXR-beta expressed in African green monkey CV1 cells measured after 18 to 20 hrs by luciferase reporter gene assay Agonist activity at human LXR-beta expressed in African green monkey CV1 cells measured after 18 to 20 hrs by luciferase reporter gene assay	[PMID: 27994765]
CV-1	EC₅₀	250 nM Compound: 18	Transactivation of LXRbeta (unknown origin) expressed in CV1 cells by luciferase reporter gene assay Transactivation of LXRbeta (unknown origin) expressed in CV1 cells by luciferase reporter gene assay	[PMID: 25435151]
HeLa	EC₅₀	33 nM Compound: 5; BMS-779788	Agonist activity at LXR-beta in human HeLa cells assessed as induction of ABCA1 by beta-galactosidase/luciferase reporter gene assay Agonist activity at LXR-beta in human HeLa cells assessed as induction of ABCA1 by beta-galactosidase/luciferase reporter gene assay	[PMID: 27994765]
HeLa	EC₅₀	33 nM Compound: 18	Transactivation of LXR (unknown origin) expressed in human HeLa cells by ABCA1 LXREx3 reporter assay Transactivation of LXR (unknown origin) expressed in human HeLa cells by ABCA1 LXREx3 reporter assay	[PMID: 25435151]

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.

918348-67-1

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
10 mM	0.1964 mL	0.9822 mL	1.9644 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)

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

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)

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

Purity: 99.86%

Select Batch:

Data Sheet (280 KB) SDS (252 KB)

COA (256 KB) HNMR (236 KB) RP-HPLC (262 KB) LCMS (97 KB)

Handling Instructions (2659 KB)

References

[1]. Kirchgessner TG, et al. Pharmacological characterization of a novel liver X receptor agonist with partial LXRα activity and a favorable window in nonhuman primates. J Pharmacol Exp Ther. 2015 Feb;352(2):305-14. [Content Brief]

[2]. Kick E, et al. Liver X receptor (LXR) partial agonists: biaryl pyrazoles and imidazoles displaying a preference for LXRβ. Bioorg Med Chem Lett. 2015 Jan 15;25(2):372-7. [Content Brief]

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

[1]. Kirchgessner TG, et al. Pharmacological characterization of a novel liver X receptor agonist with partial LXRα activity and a favorable window in nonhuman primates. J Pharmacol Exp Ther. 2015 Feb;352(2):305-14. [Content Brief]

[2]. Kick E, et al. Liver X receptor (LXR) partial agonists: biaryl pyrazoles and imidazoles displaying a preference for LXRβ. Bioorg Med Chem Lett. 2015 Jan 15;25(2):372-7. [Content Brief]

Complete Stock Solution Preparation Table

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

BMS-779788 Related Classifications

Metabolic Disease

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

Customer Review

BMS-779788 Related Antibodies

1 Publications Citing Use of MCE BMS-779788

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Purity & Documentation

References

Customer Review

BMS-779788 Related Antibodies

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Complete Stock Solution Preparation Table

BMS-779788 Related Classifications

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