Rodatristat ethyl
Based on 1 Customer Validation
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).
For research use only. We do not sell to patients.
- Purity: 99.82%
- CAS No.: 1673571-51-1
- Formula: C29H31ClF3N5O3
- Molecular Weight:590.04
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
All 5-HT Receptor Isoforms
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Biological Activity
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5-HT1 Receptor |
TPH1 |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male Sprague-Dawley rats (175-200 g)[1]
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Dosage:100 mg/kg or 200 mg/kg
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Administration:Oral administration; once daily; for 28 days
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Result:Decreased serum, gut and lung 5-HT levels in a dose-dependent manner and significantly reduced pulmonary arterial pressure, and pulmonary vessel wall thickness and occlusion in male rats.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1673571-51-1
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Appearance Solid
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Molecular Weight 590.04
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Formula C29H31ClF3N5O3
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Color White to off-white
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SMILES
ClC1=CC(C2=CC=CC=C2)=C([C@@H](OC3=NC(N)=NC(N4CCC5(CN[C@H](C(OCC)=O)C5)CC4)=C3)C(F)(F)F)C=C1
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Synonyms
KAR5585
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 100 mg/mL (169.48 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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Data Sheet (273 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 1.6948 mL | 8.4740 mL | 16.9480 mL | 42.3700 mL |
| 5 mM | 0.3390 mL | 1.6948 mL | 3.3896 mL | 8.4740 mL | |
| 10 mM | 0.1695 mL | 0.8474 mL | 1.6948 mL | 4.2370 mL | |
| 15 mM | 0.1130 mL | 0.5649 mL | 1.1299 mL | 2.8247 mL | |
| 20 mM | 0.0847 mL | 0.4237 mL | 0.8474 mL | 2.1185 mL | |
| 25 mM | 0.0678 mL | 0.3390 mL | 0.6779 mL | 1.6948 mL | |
| 30 mM | 0.0565 mL | 0.2825 mL | 0.5649 mL | 1.4123 mL | |
| 40 mM | 0.0424 mL | 0.2119 mL | 0.4237 mL | 1.0593 mL | |
| 50 mM | 0.0339 mL | 0.1695 mL | 0.3390 mL | 0.8474 mL | |
| 60 mM | 0.0282 mL | 0.1412 mL | 0.2825 mL | 0.7062 mL | |
| 80 mM | 0.0212 mL | 0.1059 mL | 0.2119 mL | 0.5296 mL | |
| 100 mM | 0.0169 mL | 0.0847 mL | 0.1695 mL | 0.4237 mL |
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