BMS-779788
Based on 1 publication(s) in Google Scholar
BMS-779788 is a LXR partial agonist with IC50 values of 68 nM for LXRα and 14 nM for LXRβ.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.57%
- No. CAS: 918348-67-1
- Fòrmula: C28H29ClN2O3S
- Peso molecular:509.06
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Protocolo
- Pureza y Documentación
- Referencias
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) BMS-779788
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Actividad biológica
Descripciòn
IC50 & Target
IC50: 68 nM (LXRα); 14 nM (LXRβ)[1]
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CV-1 | EC50 |
220 nM
Compound: 5; BMS-779788
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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
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[PMID: 27994765] |
| CV-1 | EC50 |
230 nM
Compound: 18
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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
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[PMID: 25435151] |
| CV-1 | EC50 |
250 nM
Compound: 18
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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
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[PMID: 25435151] |
| CV-1 | EC50 |
250 nM
Compound: 5; BMS-779788
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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
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[PMID: 27994765] |
| HeLa | EC50 |
33 nM
Compound: 18
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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
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[PMID: 25435151] |
| HeLa | EC50 |
33 nM
Compound: 5; BMS-779788
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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
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[PMID: 27994765] |
In Vitro
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Ensayo clínico
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 918348-67-1
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Appearance Solid
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Peso molecular 509.06
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Fòrmula C28H29ClN2O3S
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Color White to off-white
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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
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Synonyms
EXEL04286652; XL-652; BMS-788
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (1)
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Journal Impact Factor
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Most Recent
Solvente y solubilidad
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)
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.
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.
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.
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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Protocolo
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureza y Documentación
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Ficha de datos (280 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[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
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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