Adenosine Receptor Antagonist

Adenosine Receptor Antagonists (101):

Cat. No.	Product Name	Effect	Purity

HY-19532

ZM241385	Antagonist	99.26%
ZM241385 is a potent, high affinity and selective adenosine A_2a receptor (A_2AR) antagonist with a K_i value of 1.4 nM.

HY-148088A

M1069 free base	Antagonist	98.92%
M1069 (free base) is a selective and orall active, dual A2A/A2B adenosine receptor antagonist with a selectivity of >100 fold against the A1 and A3 receptors. M1069 (free base) counteracts immune-suppressive mechanisms of adenosine, and exhibits anti-tumor activity.

HY-19533

SCH 58261	Antagonist	99.78%
SCH 58261 is a potent, selective and competitive antagonist of adenosine A2A receptor with an IC₅₀ of 15 nM, and displays 323-, 53- and 100-fold more selective for A2A receptor than A1, A2B, and A3 receptors, respectively.

HY-10888

Istradefylline	Antagonist	99.70%
Istradefylline is a very potent, selective and orally active adenosine A2A receptor antagonist with K_i of 2.2 nM in experimental models of Parkinson's disease.

HY-129393

Etrumadenant	Antagonist	99.79%
Etrumadenant (AB928) is an orally bioavailable, selective dual adenosine receptor (A2aR/A2bR) antagonist. Etrumadenant relieves adenosine-mediated immune suppression. Etrumadenant has immunomodulatory and antitumor activities.

HY-100937

DPCPX	Antagonist	99.02%
DPCPX (PD 116948), a xanthine derivative, is a highly potent and selective Adenosine A1 receptor antagonist, with a K_i of 0.46 nM in ³H-CHA binding to A1 receptors in rat whole brain membranes.

HY-101978

Ciforadenant	Antagonist	99.85%
Ciforadenant (CPI-444) is a potent, orally active and selective adenosine A2A receptor (A2AR) antagonist, which induces antitumor responses.

HY-101980

Imaradenant	Antagonist	99.68%
AZD4635 (HTL1071) is a potent, selective and orally active adenosine A2A receptor (A2AR) antagonist. AZD4635 binds to human A2AR with a K_i of 1.7 nM and shows >30-fold selectivity over other adenosine receptors.

HY-14121

MRS 1754	Antagonist	98.31%
MRS 1754 is a selective antagonist radioligand for A_2B adenosine receptor with very low affinity for A₁ and A₃ receptors of both humans and rats.

HY-103166

PSB-603	Antagonist	≥99.0%
PSB-603 is a potent and highly selective A_2B adenosine receptor antagonist exhibiting a K_i value of 0.553 nM and virtually no affinity for the human and rat A₁ and A_2A and the human A₃ receptors up to a concentration of 10 μM.

HY-103169

SCH442416	Antagonist	99.68%
SCH442416 is a potent, selective and brain-penetrant antagonist of adenosine A_2A receptor (A_2AR), with K_is of 0.048 and 0.5 nM for human and rat A_2AR respectively. SCH442416 displays more than 23000-fold selectivity over A₁R, A_2BR, and A₃R (K_i=1111, 10000, and 10000 nM, respectively). SCH442416 can be used for imaging of adenosine A_2A receptors in rat and primate brain.

HY-10889

Preladenant	Antagonist	99.23%
Preladenant is a potent and competitive antagonist of the human adenosine A2A receptor with a K_i of 1.1 nM and has over 1000-fold selectivity over other adenosine receptors.

HY-B0140

Aminophylline	Antagonist	99.90%
Aminophylline is a competitive and non-selective phosphodiesterase (PDE) inhibitor. Aminophylline is a competitive adenosine receptor antagonist. Aminophylline has apulmonary vasodilator action as well as a bronchodilator action and has the potential for asthma research.

HY-103186

MRS-1706	Antagonist	98.23%
MRS-1706 is a potent and selective adenosine A_2B receptor inverse agonist. MRS-1706 has K_i values of 1.39, 112, 157, and 230 nM for human A_2B, A_2A, A₁ and A₃ receptors respectively. MRS-1706 blocks adenosine-mediated cAMP induction.

HY-137442

Inupadenant	Antagonist	99.54%
Inupadenant is an orally active, highly selective A_2A receptor antagonist. Inupadenant is not brain-penetrant. Inupadenant has potent anti-tumor activity.

HY-14858

Derenofylline	Antagonist	99.87%
Derenofylline (SLV 320) is a potent, selective and orally active adenosine A₁ receptor antagonist, with K_i values of 1 nM, 200 nM and 398 nM for human A₁, A₃ and A_2A receptors respectively. Derenofylline suppresses cardiac fibrosis and attenuates albuminuria without affecting blood pressure in rats.

HY-124543

MRS-1191	Antagonist	98.00%
MRS-1191 is a potent and selective A₃ adenosine receptor antagonist with a K_B value of 92 nM, a K_i value of 31.4 nM for human A₃ receptor and an IC₅₀ of 120 nM for CHO cells. MRS-1191 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

HY-121119

MRS 1523	Antagonist	99.93%
MRS 1523 is a potent and selective adenosine A₃ receptor antagonist with K_i values of 18.9 nM and 113 nM for human and rat A₃ receptors, respectively. In rat this corresponds to selectivities of 140- and 18-fold vs A₁ and A_2A receptors, respectively. MRS 1523 can exert antihyperalgesic effect through N-type Ca channel block and action potential inhibition in isolated rat dorsal root ganglion (DRG) neurons.

HY-B1505

Acefylline	Antagonist	99.96%
Acefylline, a xanthine derivative, is an adenosine receptor antagonist. Acefylline is a peptidylarginine deiminase (PAD) activator. Acefylline is also a bronchodilator and cardiac stimulant that inhibits rat lung cAMP phosphodiesterase isoenzymes. Acefylline can be used in asthma research.

HY-10081

GS-6201	Antagonist	98.47%
GS-6201 (CVT-6883) is a selective adenosine A2B receptor antagonist. GS-6201 displays high affinity and selectivity for the human adenosine A2B receptors (K_i=22 nM). GS-6201 reduces caspase-1 activity in the heart, and attenuates cardiac remodeling after acute myocardial infarction (AMI) in the mouse. GS-62013 attenuates the airway reactivity induced by NECA, AMP, or allergen in sensitized mice.

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