2. Metabolic Enzyme/Protease GPCR/G Protein Neuronal Signaling
  3. Tryptophan Hydroxylase 5-HT Receptor
  4. Rodatristat ethyl

Rodatristat ethyl  (Synonyms: KAR5585)

Cat. No.: HY-101124 Purity: 97.25%
COA Handling Instructions

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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).

For research use only. We do not sell to patients.

Rodatristat ethyl Chemical Structure

Rodatristat ethyl Chemical Structure

CAS No. : 1673571-51-1

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5 mg USD 920 In-stock
10 mg USD 1450 In-stock
25 mg USD 2900 In-stock
50 mg USD 4650 In-stock
100 mg USD 7500 In-stock
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Based on 1 publication(s) in Google Scholar

Rodatristat ethyl Related Antibodies

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5-HT1 Receptor 5-HT2 Receptor 5-HT3 Receptor 5-HT4 Receptor 5-HT5 Receptor 5-HT6 Receptor 5-HT7 Receptor 5-HT Receptor

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  • Purity & Documentation

  • References

  • Customer Review

Description

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].

IC50 & Target

5-HT1 Receptor

 

TPH1

 

In Vivo

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male Sprague-Dawley rats (175-200 g)[1]
Dosage: 100 mg/kg or 200 mg/kg
Administration: Oral administration; once daily; for 28 days
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.
Clinical Trial
Molecular Weight

590.04

Formula

C29H31ClF3N5O3
CAS No.
Appearance

Solid

Color

White to off-white

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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.6948 mL 8.4740 mL 16.9480 mL
5 mM 0.3390 mL 1.6948 mL 3.3896 mL
View the 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.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

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.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.08 mg/mL (3.53 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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

Purity: ≥98.0%

COA (250 KB) HNMR (120 KB) LCMS (382 KB)

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
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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Rodatristat ethyl Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Rodatristat ethyl1673571-51-1KAR5585KAR 5585KAR-5585Tryptophan Hydroxylase5-HT ReceptorSerotonin Receptor5-hydroxytryptamine ReceptorInhibitorinhibitorinhibit

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