ML278
Based on 1 Customer Validation
ML278 is a scavenger receptor-BI (SR-BI) inhibitor with an IC50 of 0.93 nM in mice. ML278 inhibits SR-BI-mediated lipid uptake, enhances the binding of high-density lipoprotein (HDL) to SR-BI, blocks the uptake of oleoylcholesteryl ester from HDL, and reversibly inhibits the efflux of free cholesterol to HDL particles. ML278 can be used in studies related to atherosclerotic coronary artery disease.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza : 97.95%
- No. CAS: 1604821-43-3
- Fòrmula: C23H23N3O5S
- Peso molecular:453.51
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Almacenamiento:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
Actividad biológica
Descripciòn
IC50 & Target
[1]|
SR-BI 0.93 nM (IC50) |
In Vitro
ML278 (dose range) inhibits [3H]CE-HDL uptake in ldlA[mSR-BI] cells with an IC50 of 7 nM, which is more potent than ITX-5061[1].
ML278 (dose range) increases Alexa488-HDL binding to SR-BI in ldlA[mSR-BI] cells with an EC50 of 0.035 μM[1].
ML278 (Up to 35 μM; 3 h) potently inhibits murine SR-BI-mediated DiI-HDL uptake in ldlA[mSR-BI] CHO cells with an IC50 of 0.93 nM, and shows no SR-BI-independent activity in ldlA7 CHO cells at concentrations up to 35 μM[2].
ML278 (Up to 35 μM) increases human HDL binding to murine SR-BI in ldlA[mSR-BI] CHO cells with an AC50 of 0.035 μM[2].
ML278 (1 h pretreatment, then 2 h incubation) reduces SR-BI-mediated free cholesterol efflux to HDL in both wild-type and SR-BIC384S mutant SR-BI-expressing ldlA CHO cells, indicating it acts independently of the BLT-1 binding site at cysteine 384[2].
ML278 (3 h pre-treatment, followed by 3 h DiI-HDL incubation without ML278; 3 h pre-treatment, 4 h washout, followed by 3 h DiI-HDL incubation without ML278) acts as a reversible inhibitor of SR-BI-mediated DiI-HDL uptake in ldlA[mSR-BI] CHO cells, as its inhibitory activity is lost or reduced after compound washout[2].
ML278 (0.1-1 μM; 60 min preincubation, followed by 4 h incubation with [3H]CE-HDL) directly interacts with purified murine SR-BI to inhibit selective [3H]CE-HDL uptake into SR-BI-reconstituted liposomes, confirming its direct target activity[2].
ML278 (1 h) has moderate metabolic stability, with 75% remaining after 1 h in CD-1 mouse liver microsomes and 48% remaining in human liver microsomes[1].
ML278 (24 h) is noncytotoxic to ldlA[mSR-BI] cells after 24 h incubation[1].
ML278 (10 μM) inhibits 11 off-target receptors by ≥20%, with the greatest inhibition (43%) against the Adenosine A3 receptor[1].
ML278 has a measurable aqueous solubility of 0.57 μM in PBS[1].
ML278 (Up to 35 μM; 3 h, 24 h) shows no cytotoxicity in ldlA[mSR-BI] CHO cells after 3-hour or 24-hour incubation, with a cytotoxicity IC50 >35 μM[2].
ML278 (35 μM; 3 h pre-treatment, followed by 30 min transferrin incubation) does not inhibit clathrin-mediated transferrin endocytosis in ldlA[mSR-BI] CHO cells at concentrations up to 35 μM, demonstrating selective activity against SR-BI[2].
ML278 (48 h (PBS stability), 5 h (human plasma stability)) has a solubility of 0.57 µM in PBS with 1% DMSO, is stable in PBS over 48 hours and in human plasma over 5 hours, and is 93.5% bound to human plasma proteins[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:ldlA[mSR-BI] Chinese hamster ovary (CHO) cells overexpressing murine SR-BI
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Concentration:Up to 35 μM
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Incubation Time:3 h; 24 h
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Result:Showed no cytotoxicity at either 3-hour or 24-hour time point.
Had an IC50 for cytotoxicity greater than 35 μM for both treatments.
Chemical Information
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No. CAS 1604821-43-3
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Appearance Solid
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Peso molecular 453.51
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Fòrmula C23H23N3O5S
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Color White to off-white
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SMILES
O=C(NC1=NC(C2=CC3=C(N(C(COC)=O)CC3)C=C2)=CS1)C4=CC(OC)=CC(OC)=C4
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
In Vitro:
DMSO : 2.5 mg/mL (5.51 mM; ultrasonic and warming and heat to 60°C; 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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 90% (20% SBE-β-CD in Saline)
Solubility: 1 mg/mL (2.21 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 1 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 (10.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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.
Pureza y Documentación
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Ficha de datos (277 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Dockendorff C, et al. Indolinyl-Thiazole Based Inhibitors of Scavenger Receptor-BI (SR-BI)-Mediated Lipid Transport. ACS Med Chem Lett. 2015 Feb 2;6(4):375-380. [Content Brief]
[2]. Faloon PW, et al. A Small Molecule Inhibitor of Scavenger Receptor BI-mediated Lipid Uptake—Probe 1. 2011 Dec 15 [updated 2014 Sep 18]. In: Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010–. [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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.2050 mL | 11.0251 mL | 22.0502 mL | 55.1256 mL |
| 5 mM | 0.4410 mL | 2.2050 mL | 4.4100 mL | 11.0251 mL |
ML278 Related Classifications
HY-19616 Related Classifications
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Keywords
- ML278
- 1604821-43-3
- ML 278
- ML-278
- Scavenger Receptor Class B type I (SR-BI）
- ldlA7 CHO cells
- Scavenger Receptor-BI
- Adenosine A3 receptor
- ldlA[mSR-BI] CHO cells
- CD-1 mouse liver microsomes
- ldlA[mSR-BI] cells
- human liver microsomes
- atherosclerotic coronary artery disease
- SR-BI
- C384S mutant SR-BI
- Inhibitor
- inhibitor
- inhibit