2. Neuronal Signaling
  3. Glucosylceramide Synthase (GCS)
  4. Glucosylceramide synthase-IN-2

Glucosylceramide synthase-IN-2 

Cat. No.: HY-144267 Purity: 98.45%
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Glucosylceramide synthase-IN-2 (compound T-690) is a potent, brain-penetrant and orally active glucosylceramide synthase (GCS) inhibitor with IC50s of 15 nM and 190 nM for human GCS and mouse GCS, respectively.Glucosylceramide synthase-IN-2 exhibits noncompetitive type inhibition with C8-ceramide and UDP-glucose.Glucosylceramide synthase-IN-2 can be used for Gaucher's disease research.

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

Glucosylceramide synthase-IN-2 Chemical Structure

Glucosylceramide synthase-IN-2 Chemical Structure

CAS No. : 2597958-02-4

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5 mg USD 450 In-stock
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25 mg USD 1650 In-stock
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Based on 1 publication(s) in Google Scholar

Glucosylceramide synthase-IN-2 Related Antibodies

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Description

Glucosylceramide synthase-IN-2 (compound T-690) is a potent, brain-penetrant and orally active glucosylceramide synthase (GCS) inhibitor with IC50s of 15 nM and 190 nM for human GCS and mouse GCS, respectively.Glucosylceramide synthase-IN-2 exhibits noncompetitive type inhibition with C8-ceramide and UDP-glucose.Glucosylceramide synthase-IN-2 can be used for Gaucher's disease research[1].

In Vitro

Glucosylceramide synthase-IN-2 (compound T-690) has no SERT inhibitory activity (IC50>10 μM). Glucosylceramide synthase-IN-2 does not affect GCase activity (EC50>300 μM)[1].
Glucosylceramide synthase-IN-2 (30 μM) does not potently inhibit hERG, CaV1.2, and NaV1.5 channels[1].

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

Glucosylceramide synthase-IN-2 Related Antibodies
In Vivo

Glucosylceramide synthase-IN-2 (compound T-690; po; 30, 100, 300 mg/kg) reduces GlcCer concentrations in the plasma and cerebral cortex in a dose-dependent manner in C57BL/6J mice[1].
Glucosylceramide synthase-IN-2 (po; 5 mg/kg) has a Cmax of 416 ng/mL. Glucosylceramide synthase-IN-2 shows good oral exposure (BA = 31%)[1].
Glucosylceramide synthase-IN-2 reveals good brain exposure (Cu,brain = 0.21 μM at 30 mg/kg dosing, 1 h)[1].

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

447.41

Formula

C22H20F3N3O4
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C(C1=CC=NN(C1=O)C2=C(OCC(F)(F)F)C=CC=C2)NC3=CC=C(C(C)(O)C)C=C3
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 (223.51 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 2.2351 mL 11.1754 mL 22.3509 mL
5 mM 0.4470 mL 2.2351 mL 4.4702 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
×
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 (5.59 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% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (5.59 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 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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 2.2351 mL 11.1754 mL 22.3509 mL 55.8772 mL
5 mM 0.4470 mL 2.2351 mL 4.4702 mL 11.1754 mL
10 mM 0.2235 mL 1.1175 mL 2.2351 mL 5.5877 mL
15 mM 0.1490 mL 0.7450 mL 1.4901 mL 3.7251 mL
20 mM 0.1118 mL 0.5588 mL 1.1175 mL 2.7939 mL
25 mM 0.0894 mL 0.4470 mL 0.8940 mL 2.2351 mL
30 mM 0.0745 mL 0.3725 mL 0.7450 mL 1.8626 mL
40 mM 0.0559 mL 0.2794 mL 0.5588 mL 1.3969 mL
50 mM 0.0447 mL 0.2235 mL 0.4470 mL 1.1175 mL
60 mM 0.0373 mL 0.1863 mL 0.3725 mL 0.9313 mL
80 mM 0.0279 mL 0.1397 mL 0.2794 mL 0.6985 mL
100 mM 0.0224 mL 0.1118 mL 0.2235 mL 0.5588 mL
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Glucosylceramide synthase-IN-2 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:

Glucosylceramide synthase-IN-22597958-02-4Glucosylceramide Synthase (GCS)glucosylceramide synthase inhibitor brain-penetrantorally activeGaucher’s diseaseC8-ceramideUDP-glucoseInhibitorinhibitorinhibit

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