BMS-466442
Based on 1 publication(s) in Google Scholar
BMS-466442 is a potent and selective inhibitor of asc-1 (alanine serine cysteine transporter-1), with an IC50 of 11 nM. BMS-466442 inhibits [3H] D-serine uptake into rat brain synaptosomes, with an IC50 of 400 nM. BMS-466442 can be used for schizophrenia research.
For research use only. We do not sell to patients.
- Purity: 98.24%
- CAS No.: 1598424-76-0
- Formula: C31H30N4O5
- Molecular Weight:538.59
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Storage:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
Publications Citing Use of MedChemExpress (MCE) BMS-466442
MoreAll Adrenergic Receptor Isoforms
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Biological Activity
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α adrenergic receptor ≥10 μM (IC50) |
ASCT1 1 nM (IC50) |
BMS-466442 dose-dependently inhibits asc-1 activity in human asc-1 expressing cells and primary cultures with IC50 values of 36.8 ± 11.6 nM and 19.7 ± 6.7 nM, respectively[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 1598424-76-0
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Appearance Solid
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Molecular Weight 538.59
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Formula C31H30N4O5
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Color Off-white to yellow
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SMILES
O=C([C@H](CC1=CN(C=N1)CC2=CC=CC=C2)NC(C3=CC4=C(C=C(C(OC)=C4)OCC5=CC=CC=C5)N3)=O)OC
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Publications (1)
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Journal Impact Factor
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Most Recent
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Nat Chem Biol
2025 Jun 2. PMID: 40456963
Solvent & Solubility
DMSO : 100 mg/mL (185.67 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, 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)
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 (4.64 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (4.64 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
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.
Purity & Documentation
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Data Sheet (274 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)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
[1]. Brown JM, et al. In vitro Characterization of a small molecule inhibitor of the alanine serine cysteine transporter -1 (SLC7A10). J Neurochem. 2014 Apr;129(2):275-83. [Content Brief]
[2]. Torrecillas IR, et al. Inhibition of the Alanine-Serine-Cysteine-1 Transporter by BMS-466442. ACS Chem Neurosci. 2019 May 15;10(5):2510-2517. [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 | 1.8567 mL | 9.2835 mL | 18.5670 mL | 46.4175 mL |
| 5 mM | 0.3713 mL | 1.8567 mL | 3.7134 mL | 9.2835 mL | |
| 10 mM | 0.1857 mL | 0.9283 mL | 1.8567 mL | 4.6417 mL | |
| 15 mM | 0.1238 mL | 0.6189 mL | 1.2378 mL | 3.0945 mL | |
| 20 mM | 0.0928 mL | 0.4642 mL | 0.9283 mL | 2.3209 mL | |
| 25 mM | 0.0743 mL | 0.3713 mL | 0.7427 mL | 1.8567 mL | |
| 30 mM | 0.0619 mL | 0.3094 mL | 0.6189 mL | 1.5472 mL | |
| 40 mM | 0.0464 mL | 0.2321 mL | 0.4642 mL | 1.1604 mL | |
| 50 mM | 0.0371 mL | 0.1857 mL | 0.3713 mL | 0.9283 mL | |
| 60 mM | 0.0309 mL | 0.1547 mL | 0.3094 mL | 0.7736 mL | |
| 80 mM | 0.0232 mL | 0.1160 mL | 0.2321 mL | 0.5802 mL | |
| 100 mM | 0.0186 mL | 0.0928 mL | 0.1857 mL | 0.4642 mL |