1. Metabolic Enzyme/Protease
  2. Tryptophan Hydroxylase
  3. ACT-678689

ACT-678689 (Compound Example 1.53.4) is a tryptophan hydroxylase (TPH) inhibitor with an IC50 of 8 nM.

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

ACT-678689 Chemical Structure

ACT-678689 Chemical Structure

CAS No. : 1783256-96-1

Size Price Stock Quantity
5 mg USD 330 In-stock
10 mg USD 500 In-stock
25 mg USD 850 In-stock
50 mg USD 1150 In-stock
100 mg USD 1550 In-stock
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Based on 1 publication(s) in Google Scholar

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Description

ACT-678689 (Compound Example 1.53.4) is a tryptophan hydroxylase (TPH) inhibitor with an IC50 of 8 nM[1].

IC50 & Target

IC50: 8 nM (TPH)[1]

In Vitro

TPH comprises two isoforms: TPH2 is mainly expressed in neuronal cell types in the central nervous system (CNS), while TPH1 is mainly expressed in peripheral tissues, including the entrochromaffin cells (EC) in the gut, where it is responsible for synthesizing 5HT that is stored in circulating blood platelets[1].

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

Molecular Weight

565.04

Formula

C23H22ClFN6O4S2

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

CS(=O)(NC1=NC(Cl)=C(OCC(N2CCC3=C(N4C(SC(C)=N4)=N3)[C@@H]2C5=CC=C(C)C=C5F)=O)C=C1)=O

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 (176.98 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.7698 mL 8.8489 mL 17.6979 mL
5 mM 0.3540 mL 1.7698 mL 3.5396 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.

  • Molarity Calculator

  • Dilution Calculator

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    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (4.42 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

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

    Solubility: ≥ 2.08 mg/mL (3.68 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
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 1.7698 mL 8.8489 mL 17.6979 mL 44.2447 mL
5 mM 0.3540 mL 1.7698 mL 3.5396 mL 8.8489 mL
10 mM 0.1770 mL 0.8849 mL 1.7698 mL 4.4245 mL
15 mM 0.1180 mL 0.5899 mL 1.1799 mL 2.9496 mL
20 mM 0.0885 mL 0.4424 mL 0.8849 mL 2.2122 mL
25 mM 0.0708 mL 0.3540 mL 0.7079 mL 1.7698 mL
30 mM 0.0590 mL 0.2950 mL 0.5899 mL 1.4748 mL
40 mM 0.0442 mL 0.2212 mL 0.4424 mL 1.1061 mL
50 mM 0.0354 mL 0.1770 mL 0.3540 mL 0.8849 mL
60 mM 0.0295 mL 0.1475 mL 0.2950 mL 0.7374 mL
80 mM 0.0221 mL 0.1106 mL 0.2212 mL 0.5531 mL
100 mM 0.0177 mL 0.0885 mL 0.1770 mL 0.4424 mL
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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.

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Product Name:
ACT-678689
Cat. No.:
HY-19572
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