| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
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| ln Vivo |
ASP4058 (oral, once daily for 21 days) lowered clinical ratings in a dose-dependent manner, with cumulative clinical scores of 15.5±1.48, 9.50±2.17 and 0.3 mg/kg from day 0 to 21 dpi, respectively. 1.17±0.619 in rats, respectively, and 15.5±0.619 in the vehicle-treated group. ASP4058 reduces weight loss in EAE rats [1]. ASP4058 (oral, daily from days 12 to 45) maintained clinical ratings at relatively low levels, with cumulative clinical scores (18-45 dpi) of 6.90 ± 2.85 and 5.60 for the 0.1 and 0.3 mg/kg dosage treatment groups, respectively. ±2.21, respectively, in mice. The ED50 value of ASP4058 is 0.063 mg/kg[1].
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| Animal Protocol |
Animal/Disease Models: Male Lewis rats with induced EAE [1].
Doses: 0.03, 0.1 or 0.3 mg/kg. Route of Administration: po (po (oral gavage)) one time/day for 21 days. Experimental Results: Clinical scores and cumulative clinical scores were diminished in a dose-dependent manner. Animal/Disease Models: SJL mice immunized with PLP139-151 and boosted with pertussis toxin developed relapsing-remitting EAE[1]. Doses: 0.1 and 0.3 mg/kg Route of Administration: Orally one time/day from days 12 to 45. Experimental Results: Clinical scores and cumulative clinical scores (18-45 dpi) were maintained at relatively low levels. |
| References | |
| Additional Infomation |
ASP4058 has been used in trials studying Food Effect of ASP4058 and Pharmacokinetics of ASP4058.
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| Molecular Formula |
C19H12F6N4O2
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|---|---|
| Molecular Weight |
442.314604759216
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| Exact Mass |
442.086
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| CAS # |
952565-91-2
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| Related CAS # |
952510-14-4 (HCl);
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| PubChem CID |
16755143
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| Appearance |
White to off-white solid powder
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| LogP |
5.4
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
11
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
31
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| Complexity |
621
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| Defined Atom Stereocenter Count |
1
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| SMILES |
FC([C@H](C)OC1C=CC(C2=NC(C3C=CC4=C(C=3)NC=N4)=NO2)=CC=1C(F)(F)F)(F)F
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| InChi Key |
NJNXCJPSMWKXHO-VIFPVBQESA-N
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| InChi Code |
InChI=1S/C19H12F6N4O2/c1-9(18(20,21)22)30-15-5-3-11(6-12(15)19(23,24)25)17-28-16(29-31-17)10-2-4-13-14(7-10)27-8-26-13/h2-9H,1H3,(H,26,27)/t9-/m0/s1
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| Chemical Name |
3-(3H-benzimidazol-5-yl)-5-[3-(trifluoromethyl)-4-[(2S)-1,1,1-trifluoropropan-2-yl]oxyphenyl]-1,2,4-oxadiazole
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ≥ 50 mg/mL (~113.04 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1.25 mg/mL (2.83 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 12.5 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 1.25 mg/mL (2.83 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 12.5 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 1.25 mg/mL (2.83 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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