[CAS NO. 918348-67-1] BMS-779788

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PRODUCTS SPECIFICATIONS [918348-67-1]

Catalog

HY-19919

Brand

MCE

CAS

918348-67-1

DESCRIPTION [918348-67-1]

Overview

MDL	-
Molecular Weight	509.06
Molecular Formula	C28H29ClN2O3S
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

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

1 Publications Citing Use of MCE

[1]Radboud University Nijmegen. 2021 Mar.

Summary

BMS-779788 is a LXR partial agonist with IC ₅₀ values of 68 nM for LXR α and 14 nM for LXR β .

IC50 & Target

IC50: 68 nM (LXR α ); 14 nM (LXR β ) ^[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 (EC ₅₀ =1.2 μM, 55% efficacy) ^[2] .

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 EC ₅₀ =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] .

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

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase
NCT00836602	Bristol-Myers Squibb	Atherosclerosis	February 2009	Phase 1

Appearance

Solid

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL ( 196.44 mM ; Need ultrasonic)

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

* Please refer to the solubility information to select the appropriate solvent.

In Vivo:

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
2.

Add each solvent one by one: 10% DMSO >> 90% corn oil

Solubility: ≥ 2.5 mg/mL (4.91 mM); Clear solution

* All of the co-solvents are available by MCE.