2. Membrane Transporter/Ion Channel Neuronal Signaling
  3. GlyT
  4. Iclepertin

Iclepertin (BI-425809) is a potent, selective and orally active glycine transporter 1 (GlyT1) inhibitor. Iclepertin is inactive against GlyT2. Iclepertin can be used for Alzheimer disease and schizophrenia research.

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Iclepertin

Iclepertin Estructura química

No. CAS : 1421936-85-7

Tamaño Precio Stock Cantidad
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 En stock
Solution
10 mM * 1 mL in DMSO En stock
Solid
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Revisión del cliente

Based on 3 publication(s) in Google Scholar

Iclepertin Related Antibodies

Top Publications Citing Use of Products

Ver todos los productos específicos de isoformas GlyT:

Ver todas las isoformas
GlyT1 GlyT2

  • Actividad biológica

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Descripciòn

Iclepertin (BI-425809) is a potent, selective and orally active glycine transporter 1 (GlyT1) inhibitor. Iclepertin is inactive against GlyT2. Iclepertin can be used for Alzheimer disease and schizophrenia research[1].

IC50 & Target[1]

GLT1

5.2 mM (IC50, In rat primary neurons )

GLT1

5 nM (IC50, In human SK-N-MC cells)

In Vitro

Iclepertin inhibits GlyT1 with the IC50 values of 5.2 nM in rat primary neurons and 5.0 nM in human SK-N-MC cells[1].

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

Iclepertin Related Antibodies
In Vivo

Single oral administration of Iclepertin induced a dose-dependent increase of glycine cerebrospinal fluid (CSF) levels. Oral administration of Iclepertin in rats induced a dose‐dependent increase of glycine CSF levels from 30% (0.2 mg/kg, not significant) to 78% (2 mg/kg), relative to vehicle[1].

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

512.42

Fòrmula

C20H18F6N2O5S
No. CAS
Appearance

Solid

Color

White to off-white

SMILES

O=C(C1=C(C=CC(S(C)(=O)=O)=C1)O[C@H](C)C(F)(F)F)N2C[C@]3(C4=NOC(C(F)(F)F)=C4)[C@@](C2)([H])C3
Envío

Room temperature in continental US; may vary elsewhere.
Almacenamiento
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvente y solubilidad
In Vitro: 

DMSO : 11.36 mg/mL (22.17 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 1.9515 mL 9.7576 mL 19.5152 mL
5 mM 0.3903 mL 1.9515 mL 3.9030 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.

  • Calculadora de molaridad

  • Calculadora de dilución

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 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.
Calculation results:
Working solution concentration: mg/mL
Pureza y Documentación

Purity: 99.97%

SDS (393 KB)

COA (254 KB) LCMS (94 KB)

Instrucciones de manejo (2659 KB)
Referencias

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 1.9515 mL 9.7576 mL 19.5152 mL 48.7881 mL
5 mM 0.3903 mL 1.9515 mL 3.9030 mL 9.7576 mL
10 mM 0.1952 mL 0.9758 mL 1.9515 mL 4.8788 mL
15 mM 0.1301 mL 0.6505 mL 1.3010 mL 3.2525 mL
20 mM 0.0976 mL 0.4879 mL 0.9758 mL 2.4394 mL
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Iclepertin 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:

Iclepertin1421936-85-7BI-425809BI425809BI 425809GlyTGlycine transportersGlyT1AlzheimerdiseaseschizophreniaInhibitorinhibitorinhibit

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Inquiry Information

Nombre del producto:
Iclepertin
Cat. No.:
HY-138935
Cantidad:
MCE Japan Authorized Agent:

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SAFETY DATA SHEET (SDS)

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