Adenosine A_2A receptor (A_2AR) Antagonist

Adenosine A_2A receptor (A_2AR) Antagonists (24):

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-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-148088

M1069	Antagonist	98.04%
M1069 is a selective and orall active, dual A_2A/A_2B adenosine receptor antagonist with a selectivity of >100 fold against the A₁ and A₃ receptors. M1069 counteracts immune-suppressive mechanisms of adenosine, and exhibits anti-tumor activity.

HY-103175

PSB36	Antagonist	≥99.0%
PSB36 is a potent and selective antagonist of adenosine A₁ receptor, with K_is 0.12 nM, 187 nM, 552 nM, 2300 nM, and 6500 nM for rA₁, hA_2B, rA_2A, hA₃ and rA₃ receptors respectively. PSB36 can be used for the research of hyperalgesia.

HY-120652

A3AR antagonist 3	Antagonist
A3AR antagonist 3 (compound 21) is a selective A3 adenosine receptor (A3AR) antagonist with a K_i of 37 nM. A3AR antagonist 3 shows >60-fold selectivity in comparison to A1 and A2A adenosine receptors.

HY-N12422

A2AAR antagonist 2	Antagonist
3′-Methoxyfurano[4″,5″:3,4]chalcone (compound 2) is a selective A_2AAR antagonist (IC₅₀=33.5 nM) with high affinity. 3′-Methoxyfurano[4″,5″:3,4]chalcone is also a natural product obtained from the bark of Allium cepa L. 3′-Methoxyfurano[4″,5″:3,4]chalcone can promote T cell activation and can be used in cancer immunity research.

HY-158057

A2AR/A2BR antagonist 1	Antagonist
A_2AR/A_2BR antagonist 1 (compound 7ai) has a dual antagonistic effect on A_2AR/A_2BR, with the IC₅₀ values of 11.2 nM and 6.4 nM for A_2AR and A_2BR, respectively. A_2AR/A_2BR antagonist 1 promotes T cell-mediated cancer cell death.

HY-103162

ANR94	Antagonist
ANR94 is a potent and selective adenosine A_2A receptor (AA_2AR) antagonist with an K_i of 46 nM for hAA_2AR. ANR94 has the potential for the research of Parkinson's disease.

HY-103174

MRS1334	Antagonist	≥99.0%
MRS1334 is a potent and selective human adenosine A₃ receptor antagonist with K_is of 2.69 nM, >100 nM, >100 nM for hA₃, rA₁, rA_2A, respectively. MRS1334 blocks the protective effect of Cl-IB-MECA leading to significant bradycardia and elevated ST segment. MRS1334 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-144064

Adenosine receptor antagonist 2	Antagonist	99.37%
Adenosine receptor antagonist 2 is an orally active A2a/A2b adenosine receptor antagonist with IC₅₀s of 1 nM and 3 nM, respectively. Adenosine receptor antagonist 2 has anti-tumor activity.

HY-116800

FR194921	Antagonist	98.10%
FR194921 is a potent, selective and orally active and cross the blood-brain barrier Adenosine A1 antagonist with K_i value of 6.6, 5400 nM for A1, A2A, respectively. FR194921 shows cognitive-enhancing and anxiolytic activity.

HY-147544

A1AR antagonist 5	Antagonist
A1AR antagonist 5 (compound 20) is a potent and selective A1AR (A1 adenosine receptor) antagonist, with a pIC₅₀ of 5.83 and a pK_i of 6.11.

HY-105003

ST 1535	Antagonist
ST 1535 is a potent and orally active A2A adenosine receptor antagonist. ST 1535 shows antiparkinsonian activity and antitremorigenic effects. ST 1535 has the potential for the research of Parkinson’s disease.

HY-147543

A1AR antagonist 4	Antagonist
A1AR antagonist 4 (compound 22) is a potent and selective A1AR (A1 adenosine receptor) antagonist, with a pIC₅₀ of 5.51 and a pK_i of 6.29.

HY-111295

LAS38096	Antagonist
LAS38096 is a potent, selective, and efficacious A2B Adenosine Receptor antagonist, with a K_i of 17 nM.

HY-151139

LJ-4517	Antagonist
LJ-4517 is a potent A_2AAR antagonist, with a K_i of 18.3 nM. LJ-4517 is potent in displacing the binding of [³H]ZM241385 (HY-19532) at WT A_2AAR. LJ-4517 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-147545

A1AR antagonist 6	Antagonist
A1AR antagonist 6 (compound 15) is a potent and selective A1AR (A1 adenosine receptor) antagonist, with a pIC₅₀ of 6.38 and a pK_i of 7.13.

HY-148076

A2A receptor antagonist 3	Antagonist
A2A receptor antagonist 3 (Example 92) is an adenosine A2a receptor antagonist with a K_i of 0.4 nM. A2A receptor antagonist 3 also binds to A2b, A1 and A3 receptor with K_is of 37, 107 and 1467 nM, respectively.

HY-146979

hA2A/hCA XII modulator 1	Antagonist
hA2A/hCA XII modulator 1 (compound 14), a triazolopirazine, is a potent hA_2A adenosine receptor (hA_2AAR) antagonist with K_is of 6.4 nM, 4.819 μM, >30 μM for hA_2AAR, hA₁AR, hA₃AR, respectively. hA2A/hCA XII modulator 1 is a potent human carbonic anhydrase XII (hCA XII) inhibitor with K_is of 6.2 nM, 46 nM, 466 nM, 8.351 μM for hCA XII, hCA II, hCA IX and hCA I, respectively. hA2A/hCA XII modulator 1 has the potential for cancer research.

HY-149916

A2AR-antagonist-1	Antagonist
A2AR-antagonist-1 (compound 38) is an orally active adenosine A2A receptor (A2AR) antagonist (IC₅₀=29 nM). A2AR-antagonist-1 exhibits anti-tumor activity and mouse liver microsomal metabolic stability (t_1/2=86.1 min). A2AR-antagonist-1 is also a T cells activator, via inhibiting immunosuppressive molecules (LAG-3 and TIM-3) and enhancing effector molecules (GZMB, IFNG, and IL-2).

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