Rodatristat ethyl (Synonyms: KAR5585) |
| Katalog-Nr.GC62458 |
Rodatristat Ethyl (KAR5585) ist ein erstklassiger oraler Tryptophan-Hydroxylase-1 (TPH1)-Inhibitor mit nanomolarer In-vitro-Wirksamkeit.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1673571-51-1
Sample solution is provided at 25 µL, 10mM.
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Rodatristat ethyl (KAR5585) is a first-in-class oral tryptophan hydroxylase 1 (TPH1) Inhibitor with nanomolar in vitro potency. Rodatristat ethyl reduces the level of 5-HT and significantly reduces pulmonary arterial hypertension (PAH)[1][2].
Rodatristat ethyl (100 or 200 mg/kg; oral administration; once daily; for 28 days; male Sprague-Dawley rats) treatment decreases erum, gut and lung 5-HT levels in a dose-dependent manner and significantly reduces pulmonary arterial pressure, and pulmonary vessel wall thickness and occlusion in male rats with monocrotaline (MCT)[1].
[1]. Aiello RJ, et al. Tryptophan hydroxylase 1 Inhibition Impacts Pulmonary Vascular Remodeling in Two Rat Modelsof Pulmonary Hypertension. J Pharmacol Exp Ther. 2017 Feb;360(2):267-279.
[2]. Alice MelÃo, MSc. Early Results on Rodatristat Ethyl Support Launch of Phase 2 Trial in PAH Patients. FEBRUARY 4, 2019.
| Cas No. | 1673571-51-1 | SDF | |
| Überlieferungen | KAR5585 | ||
| Formula | C29H31ClF3N5O3 | M.Wt | 590.04 |
| Löslichkeit | DMSO : 100 mg/mL (169.48 mM; ultrasonic and warming and heat to 60°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. |
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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 | 1.6948 mL | 8.474 mL | 16.948 mL |
| 5 mM | 0.339 mL | 1.6948 mL | 3.3896 mL |
| 10 mM | 0.1695 mL | 0.8474 mL | 1.6948 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 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.
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: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 38 reference(s) in Google Scholar.)
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