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A2A Adenosine Receptor Antagonist

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By Targets:	Adenosine Receptor (67) Androgen Receptor (1) Calcium Channel (2) Cytochrome P450 (1) Drug Intermediate (1) Drug Metabolite (1) Endogenous Metabolite (1) ERK (1) IFNAR (1) Interleukin Related (1) Isotope-Labeled Compounds (2) JNK (1) MMP (1) Monoamine Oxidase (1) Phosphodiesterase (PDE) (1) PI3K (3) Reference Standards (10)
By Research Areas:	Cancer (29) Cardiovascular Disease (6) Infection (1) Inflammation/Immunology (13) Metabolic Disease (1) Neurological Disease (36)

Inhibitors & Agonists

Natural
Products

Isotope-Labeled Compounds

Targets Recommended: Adenosine Kinase Adenosine Deaminase Adenosine Receptor

Cat. No.	Nom du produit	Target	Áreas de investigación	Chemical Structure

HY-19532

ZM241385 10+ Cited Publications	Adenosine Receptor	Neurological Disease Cancer
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-19533

SCH 58261 Maximum Cited Publications 17 Publications Verification	Adenosine Receptor	Cancer
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 15+ Cited Publications KW-6002	Adenosine Receptor	Neurological Disease
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-101978

Ciforadenant 5+ Cited Publications CPI-444; V81444	Adenosine Receptor	Cancer
Ciforadenant (CPI-444) is a potent, orally active and selective **adenosine A2A receptor (A2AR*) antagonist*, which induces antitumor responses .

HY-10889

Preladenant 5+ Cited Publications SCH-420814	Adenosine Receptor	Neurological Disease Cancer
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-109139

Taminadenant 1 Publications Verification NIR178; PBF509	Adenosine Receptor	Neurological Disease Cancer
Taminadenant (NIR178; PBF509) is a highly potent and orally active **adenosine A_2A receptor** (A_2AR) antagonist. Taminadenant can antagonize A2AR agonist-mediated cAMP accumulation and impedance responses with K_B values of 72.8 nM and 8.2 nM, respectively. Taminadenant reverses motor impairments in several rat models of movement disorders, including catalepsy, tremor, and hemiparkinsonism. Taminadenant can also inhibit tumor growth when combined with Spartalizumab (HY-P9972). Taminadenant reactivate the antitumor immune response .

HY-100678

CGS 15943	Adenosine Receptor PI3K	Inflammation/Immunology Cancer
CGS 15943 is an orally bioavailable non-xanthine **Adenosine Receptor** antagonist. Its K_i for human A1, A2A, A2B, and A3 Adenosine Receptors are 3.5, 4.2, 16, and 50 nM in transfected CHO cells, respectively. .

HY-101980

Imaradenant 3 Publications Verification HTL1071; AZD4635	Adenosine Receptor	Cancer
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-103166

PSB-603 3 Publications Verification	Adenosine Receptor	Inflammation/Immunology
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-121119

MRS 1523 5 Publications Verification	Adenosine Receptor Calcium Channel	Cardiovascular Disease Neurological Disease Inflammation/Immunology
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-103164

(E)-8-(3-Chlorostyryl)caffeine (E)-CSC	Adenosine Receptor Monoamine Oxidase	Neurological Disease
(E)-8-(3-Chlorostyryl)caffeine is a selective **adenosine A_2A receptor** antagonist. (E)-8-(3-Chlorostyryl)caffeine inhibits monoamine oxidase B (MAO-B) with a K_i value of 70 nM by a pathway that is independent of its actions on the A_2A receptor. (E)-8-(3-Chlorostyryl)caffeine has the potential for Parkinson's disease research .

HY-10995

Tozadenant 4 Publications Verification SYN115	Adenosine Receptor	Neurological Disease
Tozadenant is an **adenosine A_2A** receptor antagonist, with K_i of 11.5 nM on human A_2A and 6 nM on rhesus A_2A.

HY-10857

Vipadenant 1 Publications Verification BIIB-014; CEB-4520	Adenosine Receptor	Neurological Disease
Vipadenant (BIIB-014; CEB-4520) is an **adenosine receptor** antagonist, with K_is of 1.3 nM and 68 nM for A_2A and A₁, respectively.

HY-14858

Derenofylline 2 Publications Verification SLV 320	Adenosine Receptor	Cardiovascular Disease
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-102024

A2A receptor antagonist 1 CPI-444 analog	Adenosine Receptor	Neurological Disease Cancer
A2A receptor antagonist 1 (CPI-444 analog) is an antagonist of both **adenosine A_2A receptor** and A₁ receptor with K_i values of 4 and 264 nM, respectively .

HY-103169

SCH442416 2 Publications Verification	Adenosine Receptor	Neurological Disease
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-119413

9-Ethyladenine	Adenosine Receptor	Neurological Disease
9-Ethyladenine is a precursor of competitive antagonists of **adenosine receptors (A₁, A₂, A₃), with no significant inhibitory effect on adenine phosphoribosyltransferase (APRT*). 9-Ethyladenine derivatives have high affinity and selectivity for A₁ (K_i=27 nM), A₂A* (K_i=46 nM), and A₃ (K_i=86 nM) receptors. 9-Ethyladenine does not inhibit brain APRT activity, can be used in the study of adenosine receptor-related diseases (such as nervous system diseases) models .

HY-103162

ANR94	Adenosine Receptor	Neurological Disease
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-148088

M1069 1 Publications Verification	Adenosine Receptor	Cancer
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-W004425

DMPX 3,7-Dimethyl-1-propargylxanthine	Adenosine Receptor	Neurological Disease
DMPX (3,7-Dimethyl-1-propargylxanthine) is a selective A_2A adenosine receptor (A_2A AR) antagonist that crosses the blood-brain barrier, with a K_i of 11 μM for rat A₂ adenosine receptor and a K_i of 45 μM for rat A₁ adenosine receptor. By blocking A2A receptors in specific brain regions, DMPX protects dopaminergic and GABAergic neurons from mitochondrial dysfunction. DMPX is applicable to research related to depression, Parkinson's disease and Huntington's disease .

HY-14365

TC-G 1004	Adenosine Receptor	Neurological Disease
TC-G 1004 (compound 16j) is an orally active **A_2A adenosine receptor** antagonist, with K_i values of 0.44 nM and 80 nM for hA_2A and hA₁, respectively .

HY-10888S

Istradefylline-13C,d3 KW-6002-¹³C,d₃	Isotope-Labeled Compounds Adenosine Receptor	Neurological Disease
Istradefylline- ¹³C,d₃ is the ¹³C- and deuterium labeled Istradefylline. Istradefylline is a very potent, selective and orally active adenosine A2A receptor antagonist with Ki of 2.2 nM in experimental models of Parkinson's disease.

HY-111767

BAY-545	Adenosine Receptor	Inflammation/Immunology
BAY-545 is a potent and selective A_2B adenosine receptor antagonist, with an IC₅₀ of 59 nM. BAY-545 also exhibits IC₅₀s of 66, 400, 280 nM for human, mouse, rat A_2B adenosine receptor in cells, respectively, and a K_i of 97 nM for human A_2B adenosine receptor, with more selectivity over A₁, A_2A, and A₃ adenosine receptor .

HY-117184

MSX-2	Adenosine Receptor	Neurological Disease
MSX-2 is A2A **adenosine receptor** antagonist, with K_i of 5 nM in human that plays an important role in Parkinson's disease .

HY-105003

ST 1535	Adenosine Receptor	Neurological Disease
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-149916

A2AR-antagonist-1	Adenosine Receptor	Cancer
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) .

HY-148954

PBF-999	Adenosine Receptor Phosphodiesterase (PDE)	Cancer
PBF-999 is a phosphodiesterase10A (PDE-10A) and adenosine A2A receptor (A2AR) dual antagonist.

HY-14408

Lu AA47070	Adenosine Receptor	Neurological Disease
Lu AA47070 is a phosphonooxymethylene prodrug of a potent and selective Adenosine A2A receptor antagonist. Lu AA47070 reverses the motor and motivational effects produced by dopamine D2 receptor blockade .

HY-135387

4-Desmethyl Istradefylline	Drug Metabolite	Neurological Disease
4-Desmethyl Istradefylline is a metabolite of Istradefylline. 4-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-20176

2,4-Dichlorothieno[3,2-d]pyrimidine	Drug Intermediate Adenosine Receptor PI3K	Infection
2,4-Dichlorothieno[3,2-d]pyrimidine is a thienopyrimidine scaffold and a key synthetic precursor, which is widely used for constructing 4-arylthieno[3,2-d]pyrimidine compounds. 2,4-Dichlorothieno[3,2-d]pyrimidine serves for the development of 4-arylthieno[3,2-d]pyrimidine-based human adenosine *A2a* receptor antagonists, as well as thienopyrimidine-based PI3K-α inhibitors. In addition, 2,4-Dichlorothieno[3,2-d]pyrimidine has potential application value in studies related to whipworm disease .

HY-148076

A2A receptor antagonist 3	Adenosine Receptor	Cancer
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-144064

Adenosine receptor antagonist 2	Adenosine Receptor	Cancer
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-120652

A3AR antagonist 3	Adenosine Receptor	Inflammation/Immunology
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-10888R

Istradefylline (Standard) KW-6002 (Standard)	Reference Standards Adenosine Receptor	Neurological Disease
Istradefylline (Standard) is the analytical standard of Istradefylline. This product is intended for research and analytical applications. 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-14873

Tonapofylline BG 9928	Adenosine Receptor	Cardiovascular Disease Metabolic Disease
Tonapofylline (BG 9928) is an orally active and selective **adenosine A₁ receptor** antagonist with a K_i of 7.4 nM for human adenosine A₁ receptor (hA₁), which displays 915-fold selectivity versus human adenosine A_2A receptor and 12-fold selectivity versus human adenosine A_2B receptor and is used in development for the treatment of heart failure .

HY-19532R

ZM241385 (Standard)	Adenosine Receptor	Neurological Disease Cancer
ZM241385 (Standard) is the analytical standard of ZM241385. This product is intended for research and analytical applications. ZM241385 is a potent, high affinity and selective adenosine A2a receptor (A2AR) antagonist with a Ki value of 1.4 nM .

HY-179248

Adenosine receptor antagonist 7	Adenosine Receptor ERK JNK MMP	Cancer
Adenosine receptor antagonist 7 is an orally active triple *A1/A2A/A2B* adenosine receptor antagonist with K_i values of 1.5, 0.6 and 21 nM. Adenosine receptor antagonist 7 shows potent inhibitory activity (IC₅₀ = 0.8 nM) of cAMP production in A2AR-HEK293 cells. Adenosine receptor antagonist 7 can enhance infiltration of effector T cells and increase the CD8+/Treg ratio companied with Avelumab (HY-108730). Adenosine receptor antagonist 7can be used for the research of cancer, such as colon cancer .

HY-144672

A2A receptor antagonist 2	Adenosine Receptor	Inflammation/Immunology Cancer
A2A receptor antagonist 2 (Compound 57) is a potent, highly selective **adenosine A_2A receptor** (A_2AR) antagonist with an IC₅₀ of 8.3 nM .

HY-U00341

ST4206	Adenosine Receptor	Neurological Disease
ST4206 is a potent and orally active **adenosine A2A receptor** antagonist, with K_is of 12 nM and 197 nM for adenosine A2A receptor and adenosine A1 receptor, respectively. ST4206 has the potential for Parkinson׳s disease research .

HY-111088

LUF5981	Adenosine Receptor	Others
LUF5981 is a relatively potent **adenosine A2A receptor (A2A)** antagonist with pIC₅₀ value of 6.7 .

HY-112840

ST3932	Adenosine Receptor	Neurological Disease
ST3932 is a metabolite of ST1535, acts as an antagonist of **adenosine A_2A receptor, with K_i*s of 8 nM and 33 nM for A_2A* and A₁ receptors, respectively.

HY-174413

A2AAR antagonist 3	Adenosine Receptor	Cancer
A2AAR antagonist 3 is a selective and potent A_2A adenosine receptor (A_2A AR) antagonist with an IC₅₀ of 1.57 nM. A2AAR antagonist 3 demonstrates high and selective binding affinities to the A_2A AR. A2AAR antagonist 3 demonstrates favorable stability in rat liver microsomes in vitro and acceptable pharmacokinetic profiles in vivo. A2AAR antagonist 3 can be used in cancer research.

HY-14409

Lu AA41063	Adenosine Receptor	Neurological Disease
Lu AA41063 is an adenosine A2A receptor antagonist that may be useful in the treatment of Parkinson's disease. Lu AA41063 has a K_i value of 5.9 nM and targets the human A2A receptor.

HY-U00189

Sch412348	Adenosine Receptor	Neurological Disease
Sch412348 is a potent competitive antagonist of the human **adenosine A_2A** receptor (K_i=0.6 nM) and has >1000-fold selectivity over all other adenosine receptors.

HY-147541

A2A/A3 AR antagonist-1	Adenosine Receptor	Inflammation/Immunology
A2A/A3 AR antagonist-1 (compound 23) is a dual A_2A/A₃ adenosine receptor (AR) fluorescent ligand, with K_is of 90 nM and 31.8 nM for hA_2A AR and hA₃ AR, respectively .

HY-10889R

Preladenant (Standard) SCH-420814 (Standard)	Adenosine Receptor Reference Standards	Neurological Disease Cancer
Preladenant (Standard) is the analytical standard of Preladenant. This product is intended for research and analytical applications. Preladenant is a potent and competitive antagonist of the human adenosine A2A receptor with a Ki of 1.1 nM and has over 1000-fold selectivity over other adenosine receptors.

HY-19533R

SCH 58261 (Standard)	Adenosine Receptor	Cancer
SCH 58261 (Standard) is the analytical standard of SCH 58261. This product is intended for research and analytical applications. 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-151387

A2AAR antagonist 1	Adenosine Receptor	Neurological Disease
A2AAR antagonist 1 (compound 21a) is an A2AAR (adenosine A2A receptor) antagonist with a K_i value of 20 nM. A2AAR antagonist 1 shows high ligand efficiency, and it can be used for the research of neurodegenerative diseases .

HY-10857R

Vipadenant (Standard) BIIB-014 (Standard); CEB-4520 (Standard)	Adenosine Receptor Reference Standards	Neurological Disease
Vipadenant (Standard) is the analytical standard of Vipadenant. This product is intended for research and analytical applications. Vipadenant (BIIB-014; CEB-4520) is an adenosine receptor antagonist, with Kis of 1.3 nM and 68 nM for A2A and A1, respectively.

HY-175195

Adenosine receptor antagonist 6	Adenosine Receptor Interleukin Related IFNAR Cytochrome P450	Inflammation/Immunology Cancer
Adenosine receptor antagonist 6 is an orally active and selective **A_2A adenosine receptor (A_2AAR*) antagonist, with a K_i* of 19.18 nM. Adenosine receptor antagonist 6 inhibits 5’-N-ethylcarboxamide adenosine (NECA) (HY-103173)-mediated cAMP production (IC₅₀ = 0.089 μM) and immunosuppression, while promoting IL-2 and IFN-γ secretion. Adenosine receptor antagonist 6 abolishes the immunosuppressive effects of adenosine on T-cell activation and cytokine release. Adenosine receptor antagonist 6 inhibits tumor growth in a CT26/MC38 xenograft model. Adenosine receptor antagonist 6 can be used for the study of colon cancer .

Cat. No.	Nom du produit	Category	Target	Chemical Structure

HY-119413

9-Ethyladenine	Productos naturales Microorganisms Neurological Disease Classification of Application Fields Disease Research Fields Source Classification	Adenosine Receptor
9-Ethyladenine is a precursor of competitive antagonists of **adenosine receptors (A₁, A₂, A₃), with no significant inhibitory effect on adenine phosphoribosyltransferase (APRT*). 9-Ethyladenine derivatives have high affinity and selectivity for A₁ (K_i=27 nM), A₂A* (K_i=46 nM), and A₃ (K_i=86 nM) receptors. 9-Ethyladenine does not inhibit brain APRT activity, can be used in the study of adenosine receptor-related diseases (such as nervous system diseases) models .

Cat. No.	Nom du produit	Chemical Structure

HY-10888S

Istradefylline-13C,d3
Istradefylline- ¹³C,d₃ is the ¹³C- and deuterium labeled Istradefylline. Istradefylline is a very potent, selective and orally active adenosine A2A receptor antagonist with Ki of 2.2 nM in experimental models of Parkinson's disease.

HY-19532S

ZM241385-d7
ZM241385-d7 is a deuterated form of ZM241385 (HY-19532). ZM241385 is a potent, high affinity and selective adenosine A_2a receptor (A_2AR) antagonist with a K_i value of 1.4 nM .

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A2A Adenosine Receptor Antagonist

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Isotope-Labeled Compounds

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