ASP-4058 |
| رقم الكتالوجGC31870 |
ASP-4058 هو ناهض حيوي من الجيل التالي انتقائي وشفوي لمستقبلات Sphingosine 1-Phosphate 1 و 5 (S1P1 و S1P5) ، يخفف التهاب الدماغ والنخاع التجريبي الذاتي للقوارض مع ملف تعريف أمان مناسب
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 |
| الذوبان | 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. |
||
| 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 | 0.4522 mL | 2.2609 mL | 4.5217 mL |
| 10 mM | 0.2261 mL | 1.1304 mL | 2.2609 mL |
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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.
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Quality Control & SDS
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- Purity: >99.00%
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- SDS (Safety Data Sheet)
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Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)
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