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ASP-4058 hydrochloride

Katalog-Nr.GC62851

ASP-4058-Hydrochlorid ist ein selektiver und oral aktiver Agonist der nÄchsten Generation fÜr die Sphingosin-1-Phosphat-Rezeptoren 1 und 5 (S1P1 und S1P5), der die experimentelle Autoimmunenzephalomyelitis bei Nagetieren mit einem gÜnstigen Sicherheitsprofil lindert.

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ASP-4058 hydrochloride Chemische Struktur

Cas No.: 952510-14-4

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5 mg
277,00 $
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10 mg
441,00 $
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25 mg
882,00 $
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Sample solution is provided at 25 µL, 10mM.

Description of ASP-4058 hydrochloride

ASP-4058 hydrochloride is a next-generation, selective and orally active 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) hydrochloride 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) hydrochloride 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].

[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.

Chemical Properties of ASP-4058 hydrochloride

Cas No. 952510-14-4 SDF
Formula C19H13ClF6N4O2 M.Wt 478.78
Löslichkeit DMSO : 200 mg/mL (417.73 mM; Need ultrasonic) Storage 4°C, protect from light
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.

Complete Stock Solution Preparation Table of ASP-4058 hydrochloride

Prepare stock solution
1 mg 5 mg 10 mg
1 mM 2.0886 mL 10.4432 mL 20.8864 mL
5 mM 0.4177 mL 2.0886 mL 4.1773 mL
10 mM 0.2089 mL 1.0443 mL 2.0886 mL
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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 ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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