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

Catalog No.GC31372

BMS-779788 (EXEL04286652) is a LXR partial agonist with IC50 values of 68 nM for LXRα and 14 nM for LXRβ.

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BMS-779788 (EXEL04286652) Chemical Structure

Cas No.: 918348-67-1

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10mM (in 1mL DMSO)
$87.00
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5mg
$78.00
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10mg
$117.00
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50mg
$360.00
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100mg
$603.00
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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Protocol

Animal experiment:

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].

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.
[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.

Background

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

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].

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].

[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. [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.

Chemical Properties

Cas No. 918348-67-1 SDF
Synonyms EXEL04286652; XL-652; BMS-788
Canonical 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
Formula C28H29ClN2O3S M.Wt 509.06
Solubility DMSO : ≥ 31 mg/mL (60.90 mM) Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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1 mg 5 mg 10 mg
1 mM 1.9644 mL 9.822 mL 19.644 mL
5 mM 0.3929 mL 1.9644 mL 3.9288 mL
10 mM 0.1964 mL 0.9822 mL 1.9644 mL
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Average Rating: 5 ★★★★★ (Based on Reviews and 25 reference(s) in Google Scholar.)

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