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Rodatristat (Synonyms: KAR5417)

Katalog-Nr.GC63842

Rodatristat (KAR5417) ist ein potenter Tryptophan-Hydroxylase-1 (TPH1)- und TPH2-Inhibitor mit einem IC50s-Wert von 33 nM bzw. 7 nM und zeigt eine robuste Reduktion des intestinalen Serotoninspiegels (5-HT) bei MÄusen.

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Rodatristat Chemische Struktur

Cas No.: 1673568-73-4

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5 mg
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10 mg
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Sample solution is provided at 25 µL, 10mM.

Description of Rodatristat

Rodatristat (KAR5417) is a potent tryptophan hydroxylase 1 (TPH1) and TPH2 inhibitor with IC50s value of 33 nM and 7 nM, respectively, and shows robust reduction of intestinal serotonin (5-HT) levels in mice[1].

Rodatristat (10-50 mg/kg; oral administration; mice) treatment decreases intestinal 5-HT concentrations at 50 mg/kg, their efficacy drop off significantly at the lower 10 mg/kg dose[1].

[1]. Goldberg DR, et al. Optimization of spirocyclic proline tryptophan hydroxylase-1 inhibitors. Bioorg Med Chem Lett. 2017 Feb 1;27(3):413-419.

Chemical Properties of Rodatristat

Cas No. 1673568-73-4 SDF
Überlieferungen KAR5417
Formula C27H27ClF3N5O3 M.Wt 561.98
Löslichkeit DMSO : 20 mg/mL (35.59 mM; ultrasonic and warming and heat to 80°C) 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.

Complete Stock Solution Preparation Table of Rodatristat

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1 mg 5 mg 10 mg
1 mM 1.7794 mL 8.8971 mL 17.7942 mL
5 mM 0.3559 mL 1.7794 mL 3.5588 mL
10 mM 0.1779 mL 0.8897 mL 1.7794 mL
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In vivo Formulation Calculator (Clear solution) of Rodatristat

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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.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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3. All of the above co-solvents are available for purchase on the GlpBio website.

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Average Rating: 5 ★★★★★ (Based on Reviews and 37 reference(s) in Google Scholar.)

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