2. GPCR/G Protein
  3. Adenosine Receptor
  4. SCH442416

SCH442416 is a potent, selective and brain-penetrant antagonist of adenosine A2A receptor (A2AR), with Kis of 0.048 and 0.5 nM for human and rat A2AR respectively. SCH442416 displays more than 23000-fold selectivity over A1R, A2BR, and A3R (Ki=1111, 10000, and 10000 nM, respectively). SCH442416 can be used for imaging of adenosine A2A receptors in rat and primate brain.

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SCH442416 Chemical Structure

SCH442416 Chemical Structure

CAS No. : 316173-57-6

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 121 In-stock
Solution
10 mM * 1 mL in DMSO USD 121 In-stock
Solid
1 mg USD 52 In-stock
5 mg USD 110 In-stock
10 mg USD 187 In-stock
25 mg USD 396 In-stock
50 mg USD 638 In-stock
100 mg USD 990 In-stock
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Customer Review

Based on 2 publication(s) in Google Scholar

SCH442416 Related Antibodies

Top Publications Citing Use of Products

View All Adenosine Receptor Isoform Specific Products:

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

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

SCH442416 is a potent, selective and brain-penetrant antagonist of adenosine A2A receptor (A2AR), with Kis of 0.048 and 0.5 nM for human and rat A2AR respectively. SCH442416 displays more than 23000-fold selectivity over A1R, A2BR, and A3R (Ki=1111, 10000, and 10000 nM, respectively). SCH442416 can be used for imaging of adenosine A2A receptors in rat and primate brain[1][2].

IC50 & Target

IC50: 0.048 nM (hA2AR), 0.5 nM (rA2AR)[1]
In Vitro

SCH442416 is selective for A2AR (Ki=0.50 nM) in rat striatal membranes over A1R and A3R (Ki=1815 and >10000, respectively)[1].
SCH442416 (0.1-10?μM) increases the glutamine synthetase (GS) and glutamate aspartate transporter (GLAST) proteins expression of Müller cells in Group 1?μM[5].

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

SCH442416 Related Antibodies
In Vivo

SCH-442416 (0.017 mg/kg; i.p.) completely abrogates the CGS-21680-induced decrease in skeletal muscle injury[3].
SCH-442416 (1 μM?2μL; i.v.) increases the GS and GLAST protein expression in rats[5].
SCH442416 (1 μM) significantly attenuates the adenosine-induced dilation (from 15.3 to 5.6 μm)[4].

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

389.41

Formula

C20H19N7O2
CAS No.
Appearance

Solid

Color

Off-white to light brown

SMILES

NC1=NC(N(CCCC2=CC=C(OC)C=C2)N=C3)=C3C4=NC(C5=CC=CO5)=NN14
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 62.5 mg/mL (160.50 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 2.5680 mL 12.8399 mL 25.6799 mL
5 mM 0.5136 mL 2.5680 mL 5.1360 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

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: 0.2 mg/mL (0.51 mM); Clear solution; Need ultrasonic

    This protocol yields a clear solution of 0.2 mg/mL.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (2.0 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% Corn Oil

    Solubility: ≥ 0.2 mg/mL (0.51 mM); Clear solution

    This protocol yields a clear solution of ≥ 0.2 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (2.0 mg/mL) to 900 μL Corn oil, and mix evenly.

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).
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.5680 mL 12.8399 mL 25.6799 mL 64.1997 mL
5 mM 0.5136 mL 2.5680 mL 5.1360 mL 12.8399 mL
10 mM 0.2568 mL 1.2840 mL 2.5680 mL 6.4200 mL
15 mM 0.1712 mL 0.8560 mL 1.7120 mL 4.2800 mL
20 mM 0.1284 mL 0.6420 mL 1.2840 mL 3.2100 mL
25 mM 0.1027 mL 0.5136 mL 1.0272 mL 2.5680 mL
30 mM 0.0856 mL 0.4280 mL 0.8560 mL 2.1400 mL
40 mM 0.0642 mL 0.3210 mL 0.6420 mL 1.6050 mL
50 mM 0.0514 mL 0.2568 mL 0.5136 mL 1.2840 mL
60 mM 0.0428 mL 0.2140 mL 0.4280 mL 1.0700 mL
80 mM 0.0321 mL 0.1605 mL 0.3210 mL 0.8025 mL
100 mM 0.0257 mL 0.1284 mL 0.2568 mL 0.6420 mL
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SCH442416 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:

SCH442416316173-57-6SCH 442416SCH-442416Adenosine ReceptorP1 receptoradenosineA2AimagingInhibitorinhibitorinhibit

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