2. GPCR/G Protein
  3. Adenosine Receptor
  4. Sipagladenant

Sipagladenant (Compound I) is an orally active adenosine receptor A2A inverse agonist. Sipagladenant can be used in frontal lobe dysfunction research.

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Sipagladenant

Sipagladenant Estructura química

No. CAS : 858979-50-7

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
5 mg En stock
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Sipagladenant Related Antibodies

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Adenosine A1 receptor (A1R) Adenosine A2A receptor (A2AR) Adenosine A2B receptor (A2BR) Adenosine A3 receptor (A3R)

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Descripciòn

Sipagladenant (Compound I) is an orally active adenosine receptor A2A inverse agonist[1]. Sipagladenant can be used in frontal lobe dysfunction research[2].

In Vivo

Sipagladenant (oral administration; 0.3 mg/kg; once) treatment improves cognitive impairment due to a decline in dopamine function in the medial prefrontal cortex[2].
Sipagladenant (oral administration; 0.1 mg/kg; once) treatment can improve alternation behavior[2].
Sipagladenant (oral administration; 0.1 mg/kg; once) treatment can improve gait parameters[2].

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

Animal Model: Medial prefrontal dopaminerjic terminal-lesioned CD(SD) IGS male rat[2]
Dosage: 0.3 mg/kg
Administration: Oral administration; 0.3 mg/kg; once
Result: Showed longer exploration time of the novel object (65.03%) than that of the familiar object (34.97%) (p<0.001).
Animal Model: ICR mice with cognitive impairment and/or movement disoder[2]
Dosage: 0.1 mg/kg
Administration: Oral administration; 0.1 mg/kg; once
Result: Showed a significantly high alternation behavior (69.5%) as compared to the vehicle administration group (59.6%) (p<0.01).
Animal Model: ICR mice with cognitive impairment and/or movement disoder[2]
Dosage: 0.1 mg/kg
Administration: Oral administration; 0.1 mg/kg; once
Result: Showed a significantly large maximum contact area and gait area of the left hindpaw as compared to the vehicle administration group (p<0.05), tendency of the maximum contact area and gait area of the right forepaw being large (p<0.1).
Ensayo clínico
Peso molecular

397.45

Fòrmula

C20H19N3O4S
No. CAS
Appearance

Solid

Color

Off-white to light yellow

SMILES

O=C(C1=CN=C(C)C=C1)NC2=NC(C3=CC=CO3)=C(C(C4CCOCC4)=O)S2
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 : 50 mg/mL (125.80 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 2.5160 mL 12.5802 mL 25.1604 mL
5 mM 0.5032 mL 2.5160 mL 5.0321 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:

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    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (6.29 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.
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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 2.5160 mL 12.5802 mL 25.1604 mL 62.9010 mL
5 mM 0.5032 mL 2.5160 mL 5.0321 mL 12.5802 mL
10 mM 0.2516 mL 1.2580 mL 2.5160 mL 6.2901 mL
15 mM 0.1677 mL 0.8387 mL 1.6774 mL 4.1934 mL
20 mM 0.1258 mL 0.6290 mL 1.2580 mL 3.1450 mL
25 mM 0.1006 mL 0.5032 mL 1.0064 mL 2.5160 mL
30 mM 0.0839 mL 0.4193 mL 0.8387 mL 2.0967 mL
40 mM 0.0629 mL 0.3145 mL 0.6290 mL 1.5725 mL
50 mM 0.0503 mL 0.2516 mL 0.5032 mL 1.2580 mL
60 mM 0.0419 mL 0.2097 mL 0.4193 mL 1.0483 mL
80 mM 0.0315 mL 0.1573 mL 0.3145 mL 0.7863 mL
100 mM 0.0252 mL 0.1258 mL 0.2516 mL 0.6290 mL
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Sipagladenant Related Classifications

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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.

Keywords:

Sipagladenant858979-50-7KW-6356KW6356KW 6356Adenosine ReceptorP1 receptorfrontal lobe dysfunctionInhibitorinhibitorinhibit

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