1. Membrane Transporter/Ion Channel Neuronal Signaling Metabolic Enzyme/Protease
  2. iGluR Lipoxygenase
  3. Osavampator

Osavampator  (Synonyms: TAK-653; NBI-1065845)

Cat. No.: HY-115864 Pureza: 99.74%
Instrucciones de manejo Technical Support

Osavampator (TAK-653) is a AMPA receptor positive allosteric modulator. Osavampator selectively binds to AMPA-R in a glutamate-dependent manner and induces Ca2+ influx in hGluA1i CHO cells (EC50 = 3.3 μM). Osavampator improves learning and memory in many models. Osavampator is can be used for the research of depressive disorders.

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Osavampator

Osavampator Estructura química

No. CAS : 1358751-06-0

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Muestra gratis (0.1 - 0.2 mg)   Solicite ahora  
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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Descripciòn

Osavampator (TAK-653) is a AMPA receptor positive allosteric modulator. Osavampator selectively binds to AMPA-R in a glutamate-dependent manner and induces Ca2+ influx in hGluA1i CHO cells (EC50 = 3.3 μM). Osavampator improves learning and memory in many models. Osavampator is can be used for the research of depressive disorders[1][2].

IC50 & Target

AMPA Receptor

 

5-LO

 

In Vivo

Osavampator (0.03-0.3 mg/kg, p.o., single dose) enhances visual learning and memory in normal rats[2].
Osavampator (0.3 mg/kg, p.o., single dose) enhances sustained attention in the poor performing rats[2].
Osavampator (0.06 mg/kg, p.o., single dose) improves working memory in monkeys[2].
Osavampator (1 mg/kg, p.o., single dose) produces antidepressant-like effects in the rat RSBM (reduction of submissive behavior model)[1].

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

Animal Model: Normal rats[2]
Dosage: 0.03 mg/kg, 0.1 mg/kg, 0.3 mg/kg
Administration: Oral gavage (p.o.)
Result: Improved the novelty discrimination index (NDI).
Animal Model: Poor performing rats[2]
Dosage: 0.3 mg/kg
Administration: Oral gavage (p.o.)
Result: Increased correct responses and decreased omissions in the poor performing rats.
Animal Model: Fasted monkey[2]
Dosage: 0.06 mg/kg
Administration: Oral gavage (p.o.)
Result: Significantly increased delayed match-to-sample (DMTS) accuracy at a 16-s delay interval.
Maintained the beneficial effect 24 h after administration.
Animal Model: submissive behavior model [1]
Dosage: 0.1 mg/kg, 1 mg/kg
Administration: Oral gavage (p.o.)
Result: Led to a significant reduction in dominance levels compared with vehicle treatment starting from the seventh day of treatment and maintained throughout the study period.
Had a significant effect in reducing dominance levels at 0.1 and 1 mg/kg.
Ensayo clínico
Peso molecular

373.47

Fòrmula

C19H23N3O3S

No. CAS
Appearance

Solid

Color

White to yellow

SMILES

O=S1(N=C2C(C3=CC=C(C=C3)OC4CCCCC4)=NC(C)=CN2CC1)=O

Envío

Room temperature in continental US; may vary elsewhere.

Almacenamiento

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)

Solvente y solubilidad
In Vitro: 

DMSO : ≥ 12.5 mg/mL (33.47 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 2.6776 mL 13.3880 mL 26.7759 mL
5 mM 0.5355 mL 2.6776 mL 5.3552 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.

  • 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:

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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:  50% PEG300    50% Saline

    Solubility: 0.83 mg/mL (2.22 mM); Suspended solution; Need ultrasonic

  • Protocol 2

    Add each solvent one by one:  15% Cremophor EL    85% Saline

    Solubility: 1 mg/mL (2.68 mM); Suspended solution; Need ultrasonic

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: 99.74%

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 (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 2.6776 mL 13.3880 mL 26.7759 mL 66.9398 mL
5 mM 0.5355 mL 2.6776 mL 5.3552 mL 13.3880 mL
10 mM 0.2678 mL 1.3388 mL 2.6776 mL 6.6940 mL
15 mM 0.1785 mL 0.8925 mL 1.7851 mL 4.4627 mL
20 mM 0.1339 mL 0.6694 mL 1.3388 mL 3.3470 mL
25 mM 0.1071 mL 0.5355 mL 1.0710 mL 2.6776 mL
30 mM 0.0893 mL 0.4463 mL 0.8925 mL 2.2313 mL
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  • 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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Nombre del producto:
Osavampator
Cat. No.:
HY-115864
Cantidad:
MCE Japan Authorized Agent: