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

SCH442416 

Cat. No.: HY-103169 Purity: 98.19%
Handling Instructions

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.

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

SCH442416 Chemical Structure

SCH442416 Chemical Structure

CAS No. : 316173-57-6

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 110 In-stock
Estimated Time of Arrival: December 31
5 mg USD 100 In-stock
Estimated Time of Arrival: December 31
10 mg USD 170 In-stock
Estimated Time of Arrival: December 31
25 mg USD 360 In-stock
Estimated Time of Arrival: December 31
50 mg USD 580 In-stock
Estimated Time of Arrival: December 31
100 mg USD 900 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

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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].

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

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].

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

Molecular Weight

389.41

Formula

C₂₀H₁₉N₇O₂

CAS No.

316173-57-6

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 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 62.5 mg/mL (160.50 mM; Need ultrasonic)

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
10 mM 0.2568 mL 1.2840 mL 2.5680 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 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

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

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

*All of the co-solvents are provided by MCE.
References
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Keywords:

SCH442416SCH 442416SCH-442416Adenosine ReceptorP1 receptoradenosineA2AimagingInhibitorinhibitorinhibit

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Product Name:
SCH442416
Cat. No.:
HY-103169
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