ASP-4058
Based on 1 publication(s) in Google Scholar
ASP-4058 is a next-generation, selective and oral bioactive agonist for Sphingosine 1-Phosphate receptors 1 and 5 (S1P1 and S1P5), ameliorates rodent experimental autoimmune encephalomyelitis with a favorable safety profile.
For research use only. We do not sell to patients.
- Purity: 99.54%
- CAS No.: 952565-91-2
- Formula: C19H12F6N4O2
- Molecular Weight:442.31
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Storage:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) ASP-4058
More
Biological Activity
S1P1 and S1P5[1].
ASP4058 (p.o., daily for day 12 to day 45) maintains the clinical score at a relatively low level and the cumulative clinical scores (18-45 dpi) among the groups treated with 0.1 and 0.3 mg/kg dosages are 6.90±2.85 and 5.60±2.21, respectively in mice. The ED50 values for ASP4058 is 0.063 mg/kg[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male Lewis rats with an induction of EAE[1].
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Dosage:0.03, 0.1 or 0.3 mg/kg.
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Administration:Oral administration once daily for 21 days.
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Result:Reduced the clinical score in a dose-dependent manner and the cumulative clinical score.
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Animal Model:SJL mice immunized with PLP139-151 and boosted with pertussis toxin developed relapsing-remitting EAE[1].
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Dosage:0.1 and 0.3 mg/kg
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Administration:Oral administration once daily from day 12 to day 45.
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Result:Maintained the clinical score at a relatively low level and the cumulative clinical scores (18-45 dpi).
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 952565-91-2
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Appearance Solid
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Molecular Weight 442.31
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Formula C19H12F6N4O2
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Color White to off-white
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SMILES
C[C@H](OC1=CC=C(C2=NC(C3=CC=C4N=CNC4=C3)=NO2)C=C1C(F)(F)F)C(F)(F)F
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Publications (1)
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Journal Impact Factor
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Most Recent
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Sci Adv
Mfsd2a and Spns2 are essential for sphingosine-1-phosphate transport in the formation and maintenance of the blood-brain barrier. [Abstract]2020 May 29;6(22):eaay8627. PMID: 32523984
Solvent & Solubility
DMSO : ≥ 50 mg/mL (113.04 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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 (protect from light). 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 (protect from light). 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: ≥ 1.25 mg/mL (2.83 mM); Clear solution
This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 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: 1.25 mg/mL (2.83 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 1.25 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 (12.5 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. * In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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
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 (protect from light). 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 | 2.2609 mL | 11.3043 mL | 22.6086 mL | 56.5214 mL |
| 5 mM | 0.4522 mL | 2.2609 mL | 4.5217 mL | 11.3043 mL | |
| 10 mM | 0.2261 mL | 1.1304 mL | 2.2609 mL | 5.6521 mL | |
| 15 mM | 0.1507 mL | 0.7536 mL | 1.5072 mL | 3.7681 mL | |
| 20 mM | 0.1130 mL | 0.5652 mL | 1.1304 mL | 2.8261 mL | |
| 25 mM | 0.0904 mL | 0.4522 mL | 0.9043 mL | 2.2609 mL | |
| 30 mM | 0.0754 mL | 0.3768 mL | 0.7536 mL | 1.8840 mL | |
| 40 mM | 0.0565 mL | 0.2826 mL | 0.5652 mL | 1.4130 mL | |
| 50 mM | 0.0452 mL | 0.2261 mL | 0.4522 mL | 1.1304 mL | |
| 60 mM | 0.0377 mL | 0.1884 mL | 0.3768 mL | 0.9420 mL | |
| 80 mM | 0.0283 mL | 0.1413 mL | 0.2826 mL | 0.7065 mL | |
| 100 mM | 0.0226 mL | 0.1130 mL | 0.2261 mL | 0.5652 mL |
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