ASP-4058 |
Catalog No.GC31870
One-Click Copy Product Info
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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.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 952565-91-2
Sample solution is provided at 25 µL, 10mM.
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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[1].
ASP4058 (p.o., daily for 21 days) reduces the clinical score in a dose-dependent manner and the cumulative clinical score from day 0 to 21 dpi at 0.03, 0.1 and 0.3 mg/kg are 15.5±1.48, 9.50±2.17 and 1.17±1.17, respectively, while that of vehicle-treated group is 15.5±0.619 in rats. ASP4058 prevents decreases in body weight of EAE rats[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].|| Animal Model:|Male Lewis rats with an induction of EAE[1].|Dosage:|0.03, 0.1 or 0.3 mg/kg.|Administration:|Oral administration once daily for 21 days.|Result:|Reduced the clinical score in a dose-dependent manner and the cumulative clinical score.|| Animal Model:|SJL mice immunized with PLP139-151 and boosted with pertussis toxin developed relapsing-remitting EAE[1].|Dosage:|0.1 and 0.3 mg/kg|Administration:|Oral administration once daily from day 12 to day 45.|Result:|Maintained the clinical score at a relatively low level and the cumulative clinical scores (18-45 dpi).
[1]. Rie Yamamoto, et al. ASP4058, a Novel Agonist for Sphingosine 1-Phosphate Receptors 1 and 5, Ameliorates Rodent Experimental Autoimmune Encephalomyelitis with a Favorable Safety Profile. PLoS One. 2014 Oct 27;9(10):e110819.
| Cas No. | 952565-91-2 | SDF | |
| Canonical SMILES | C[C@H](OC1=CC=C(C2=NC(C3=CC=C4N=CNC4=C3)=NO2)C=C1C(F)(F)F)C(F)(F)F | ||
| Formula | C19H12F6N4O2 | M.Wt | 442.31 |
| Solubility | DMSO : ≥ 50 mg/mL (113.04 mM) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.2609 mL | 11.3043 mL | 22.6086 mL |
| 5 mM | 452.2 μL | 2.2609 mL | 4.5217 mL |
| 10 mM | 226.1 μL | 1.1304 mL | 2.2609 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)