1. Signaling Pathways
  2. GPCR/G Protein
  3. Adenosine Receptor
  4. Adenosine A1 receptor (A1R) Isoform

Adenosine A1 receptor (A1R)

 

Adenosine A1 receptor (A1R) Related Products (29):

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 A2A (A2AR) receptors.
  • HY-14858
    Derenofylline
    Antagonist 99.87%
    Derenofylline (SLV 320) is a potent, selective and orally active adenosine A1 receptor antagonist, with Ki values of 1 nM, 200 nM and 398 nM for human A1, A3 and A2A receptors respectively. Derenofylline suppresses cardiac fibrosis and attenuates albuminuria without affecting blood pressure in rats.
  • HY-139644
    MIPS521
    Agonist 98.21%
    MIPS521 is a positive allosteric modulator of adenosine A1 receptor (A1AR). MIPS521 also has a lower A1R allosteric affinity (pKB=4.95; KB=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 Kis 0.12 nM, 187 nM, 552 nM, 2300 nM, and 6500 nM for rA1, hA2B, rA2A, hA3 and rA3 receptors respectively. PSB36 can be used for the research of hyperalgesia.
  • HY-106186
    GW-493838
    Agonist
    GW-493838 is a potent Adenosine A1 (A1AR) agonist. GW-493838 has the potential for the research of neuropathic pain.
  • HY-W777125
    2-Chloro-3-deazaadenosine
    Agonist
    2-Chloro-3-deazaadenosine is agonists for adenosine receptor, with Kis of 0.3, 0.08, 25.5 and 1.9 μM, for A1, A2A, A2B, and A3 receptors, respectively.
  • HY-123127
    CVT-2759 analog
    Agonist
    CVT-2759 analog (compound 15) is a partial agonist of A1 adenosine receptor (Ki=167 nM) and can be used for the study of cardiac arrhythmias.
  • HY-103174
    MRS1334
    Antagonist ≥99.0%
    MRS1334 is a potent and selective human adenosine A3 receptor antagonist with Kis of 2.69 nM, >100 nM, >100 nM for hA3, rA1, rA2A, 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 Ki value of 6.6, 5400 nM for A1, A2A, respectively. FR194921 shows cognitive-enhancing and anxiolytic activity.
  • HY-147907
    Adenosine receptor inhibitor 1
    Inhibitor
    Adenosine receptor inhibitor 1 is a potent and selective adenosine receptor (AR) inhibitor with Ki values of >1000, 68.5, >1000, >1000 nM for A1AR, A2AAR, A2BAR, 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-103170
    LUF5834
    Agonist
    LUF5834 is a selective A2B adenosine receptor (A2BR) partial agonist (EC50 = 12 nM). LUF5834 is also a partial A1/A2A adenosine receptor agonist (lacking selectivity) with Ki values of 2.6 and 28 nM, respectively.
  • 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/A2A ARs with higher affinity for the A1- than the A2AAR. Adenosine receptor inhibitor 2 has Ki values of 52.2 nM for the A1AR and 167 nM for the A2AAR.
  • 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 pKi of 6.11.
  • 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 pKi of 6.29.
  • HY-111295
    LAS38096
    Antagonist
    LAS38096 is a potent, selective, and efficacious A2B Adenosine Receptor antagonist, with a Ki of 17 nM.
  • HY-120652
    A3AR antagonist 3
    Antagonist
    A3AR antagonist 3 (compound 21) is a selective A3 adenosine receptor (A3AR) antagonist with a Ki of 37 nM. A3AR antagonist 3 shows >60-fold selectivity in comparison to A1 and A2A adenosine receptors.
  • 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 pKi of 7.13.
  • HY-148076
    A2A receptor antagonist 3
    Antagonist
    A2A receptor antagonist 3 (Example 92) is an adenosine A2a receptor antagonist with a Ki of 0.4 nM. A2A receptor antagonist 3 also binds to A2b, A1 and A3 receptor with Kis 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 hA2A adenosine receptor (hA2AAR) antagonist with Kis of 6.4 nM, 4.819 μM, >30 μM for hA2AAR, hA1AR, hA3AR, respectively. hA2A/hCA XII modulator 1 is a potent human carbonic anhydrase XII (hCA XII) inhibitor with Kis 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.