Adenosine A₁ receptor (A₁R)

Adenosine A₁ receptor (A₁R) Related Products (23):

By Type:	Pan (7) Selective (12)
By Effects:	Inhibitors (3) Agonists (6) Antagonists (13) Modulator (1)

Cat. No.	Product Name	Effect	Purity

HY-N0092

Inosine	Agonist	99.61%
Inosine is an endogenous purine nucleoside produced by catabolism of adenosine. Inosine has anti-inflammatory, antinociceptive, immunomodulatory and neuroprotective effects. Inosine is an agonist for adenosine A₁ (A₁R) and A_2A (A_2AR) receptors.

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-139644

MIPS521	Agonist	99.65%
MIPS521 is a positive allosteric modulator of adenosine A₁ receptor (A₁AR). MIPS521 also has a lower A₁R allosteric affinity (pK_B=4.95; K_B=11 μM). MIPS521 exhibits pain-relieving effects in vivo through modulation of the increased levels of endogenous adenosine.

HY-103180

2-Chloro-N-cyclopentyl-2′-C-methyladenosine	Agonist	99.79%
2'-MeCCPA is a potent and selective A1 adenosine receptors (A1AR) agonist. 2'-MeCCPA efficiently inhibits cAMP modulation in both direct pathway medium spiny neurons (dMSNs) and indirect pathway medium spiny neurons (iMSNs).

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-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-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-147908

Adenosine receptor inhibitor 2	Inhibitor
Adenosine receptor inhibitor 2 (compound 14b) is a potent AR (adenosine receptor) inhibitor. Adenosine receptor inhibitor 2 shows dual affinity toward A₁/A_2A ARs with higher affinity for the A₁- than the A_2AAR. Adenosine receptor inhibitor 2 has K_i values of 52.2 nM for the A₁AR and 167 nM for the A_2AAR.

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-147907

Adenosine receptor inhibitor 1	Inhibitor
Adenosine receptor inhibitor 1 is a potent and selective adenosine receptor (AR) inhibitor with K_i values of >1000, 68.5, >1000, >1000 nM for A₁AR, A_2AAR, A_2BAR, A₃AR, respectively. Adenosine receptor inhibitor 1 shows antinociceptive activity, anti-inflammatory effect and peripheral analgesic effect. Adenosine receptor inhibitor 1 has the potential for the research of cancer or neurodegenerative diseases.

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-103170

LUF5834	Agonist
LUF5834 is a selective A_2B adenosine receptor (A2BR) partial agonist (EC₅₀ = 12 nM). LUF5834 is also a partial A₁/A_2A adenosine receptor agonist (lacking selectivity) with K_i values of 2.6 and 28 nM, respectively.

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-113608

VCP171	Modulator
VCP171 is a potent adenosine A1 receptor (A1R) positive allosteric modulator (PAM). VCP171 is effective at decreasing excitatory synaptic currents in Lamina II of neuropathic pain model. VCP171 can be used for researching neuropathic pain.

HY-143324

A2AAR/HDAC-IN-1	Inhibitor
A2AAR/HDAC-IN-1 (compound 14c) is an orally active, potent and balanced A_2AAR/HDAC dual inhibitor, with a K_i of 163.5 nM for A_2AAR and an IC₅₀ of 145.3 nM for HDAC1. A2AAR/HDAC-IN-1 shows anticancer activity.

HY-115494

Neladenoson dalanate hydrochloride	Agonist
Neladenoson dalanate (Neladenoson bialanate; BAY-1067197) hydrochloride is a orally active agonist precursor of partial Adenosine A1 Receptor. Neladenoson dalanate hydrochloride has a good pharmacokinetic and safety profile, can be used for the chronic heart diseases.

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