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[CAS NO. 918348-67-1] BMS-779788
| Ships within | Stock | Price | Qty | Total |
Please click "REQUEST A QUOTE" button if there is no stock, or you need other sizes or custom synthesis.
| Catalog: | HY-19919 |
| Brand: | MCE |
| CAS: | 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 |
1 Publications Citing Use of MCE
Summary
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
DMSO : 100 mg/mL ( 196.44 mM ; Need ultrasonic)
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 |
-
1.
-
2.
Add each solvent one by one: 10% DMSO >> 90% corn oil
Solubility: ≥ 2.5 mg/mL (4.91 mM); Clear solution
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.
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