2. Neuronal Signaling
  3. Glucosylceramide Synthase (GCS)
  4. TP-060

TP-060  (Synonyms: Glucosylceramide synthase-IN-1)

Cat. No.: HY-144266 Purity: 99.83%
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Glucosylceramide synthase-IN-1 (T-036) a potent, brain-penetrant and orally active glucosylceramide synthase (GCS) inhibitor with IC50s of 31 nM and 51 nM for human GCS and mouse GCS, respectively. Glucosylceramide synthase-IN-1 can be used for Gaucher's disease research.

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

TP-060 Chemical Structure

TP-060 Chemical Structure

CAS No. : 2601393-20-6

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Based on 1 publication(s) in Google Scholar

TP-060 Related Antibodies

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Description

Glucosylceramide synthase-IN-1 (T-036) a potent, brain-penetrant and orally active glucosylceramide synthase (GCS) inhibitor with IC50s of 31 nM and 51 nM for human GCS and mouse GCS, respectively. Glucosylceramide synthase-IN-1 can be used for Gaucher's disease research[1].

IC50 & Target

IC50: 31 nM (human GCS) and 51 nM (mouse GCS)[1]
In Vitro

Glucosylceramide synthase-IN-1 (T-036) potently reduces the GCS product, catalyze glucosylceramide (GlcCer), in the fibroblasts with Gaucher’s disease (EC50 of 7.6 nM)[1].

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

TP-060 Related Antibodies
In Vivo

Glucosylceramide synthase-IN-1 (T-036) has good oral exposure (BA = 67%) and moderate brain penetration (Kpuu,brain = 0.11). Administration of a single dose of Glucosylceramide synthase-IN-1 (T-036) reduces GlcCer in the plasma and cerebral cortex of wild-type mice, and administration of Glucosylceramide synthase-IN-1 (T-036) for 2 months significantly reduces glucosylsphingosine (GlcSph) in the cerebral cortex of the Gaucher’s disease mouse model[1].

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

460.42

Formula

C24H20F4N2O3
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

FC1=CC(OCC(F)(F)F)=C(C2=NC=CC3=C2CN(C4=CC=C(C(C)(O)C)C=C4)C3=O)C=C1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (217.19 mM; Need ultrasonic; 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 2.1719 mL 10.8596 mL 21.7193 mL
5 mM 0.4344 mL 2.1719 mL 4.3439 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 (sealed storage, away from moisture and light). 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
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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 (5.43 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.
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).

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

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 (sealed storage, away from moisture and light). 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 2.1719 mL 10.8596 mL 21.7193 mL 54.2982 mL
5 mM 0.4344 mL 2.1719 mL 4.3439 mL 10.8596 mL
10 mM 0.2172 mL 1.0860 mL 2.1719 mL 5.4298 mL
15 mM 0.1448 mL 0.7240 mL 1.4480 mL 3.6199 mL
20 mM 0.1086 mL 0.5430 mL 1.0860 mL 2.7149 mL
25 mM 0.0869 mL 0.4344 mL 0.8688 mL 2.1719 mL
30 mM 0.0724 mL 0.3620 mL 0.7240 mL 1.8099 mL
40 mM 0.0543 mL 0.2715 mL 0.5430 mL 1.3575 mL
50 mM 0.0434 mL 0.2172 mL 0.4344 mL 1.0860 mL
60 mM 0.0362 mL 0.1810 mL 0.3620 mL 0.9050 mL
80 mM 0.0271 mL 0.1357 mL 0.2715 mL 0.6787 mL
100 mM 0.0217 mL 0.1086 mL 0.2172 mL 0.5430 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.

Keywords:

TP-0602601393-20-6Glucosylceramide synthase-IN-1TP060TP 060Glucosylceramide Synthase (GCS)glucosylceramide synthase inhibitor brain-penetrantorally activeGaucher’s diseaseInhibitorinhibitorinhibit

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