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high A1 selectivity

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8

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Natural
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Click Chemistry

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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-117570

    PDI Neurological Disease
    KSC-34, a covalent modifier of protein disulfide isomerase A1 (PDIA1), is also a selective and potent a-site inhibitor of PDIA1 with an IC50 of 3.5 μM. KSC-34 displays a 30-fold selectivity for a domain over a′ domain and displays high selectivity for PDIA1 in complex proteomes with minimal engagement of other members of the PDI family . KSC-34 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    KSC-34
  • HY-119413

    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 (Ki=27 nM), A2A (Ki=46 nM), and A3 (Ki=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 .
    9-Ethyladenine
  • HY-19842

    CVT 3619

    Adenosine Receptor Cardiovascular Disease Metabolic Disease
    GS-9667 (CVT 3619), a novel N 6-5'-substituted adenosine analog, is a selective, partial agonist of the A1 adenosine receptor (A1AdoR). GS-9667 binds to adipocyte membranes with high (KH=14 nM) and low (KL=5.4 μM) affinities. GS-9667 reduces cyclic AMP content and release of nonesterified fatty acids from epididymal adipocytes with IC50 values of 6 nM and 44 nM, respectively. GS-9667 inhibits lipolysis and has the potential for Type 2 diabetes (T2DM) and dyslipidemia via lowering of free fatty acids (FFA) .
    GS-9667
  • HY-136702

    Adenosine Receptor Inflammation/Immunology
    L-97-1 is a A1 adenosine receptor (A1AR) antagonist. L-97-1 is a water-soluble small molecule compound with high affinity and high selectivity against human A1 adenosine receptors. L-97-1 works by blocking A1 adenosine receptors. In patients with asthma, adenosine is an important signaling molecule capable of causing bronchoconstriction by activating A1AR. L-97-1 reduces airway hyperreactivity (BHR) by competitively binding to A1AR, thereby alleviating or blocking adenosine-induced bronchoconstriction and inflammation .
    L-97-1
  • HY-123038

    Adenosine Receptor Inflammation/Immunology
    CVT-5440 is a xanthine based, selective, high affinity A2B adenosine receptors (AdoR) antagonist with a Ki of 50 nM (selectivity A1> 200; A2A>200; A3>167). CVT-5440 has the potential for asthma research .
    CVT-5440
  • HY-180423

    Adenosine Receptor Neurological Disease
    IRFI-165 is a potent and selective A1 adenosine receptor antagonist with a Ki of 7.9 nM for rat A1 AR. IRFI-165 exhibies high selectivity versus A2A and A3 receptors. IRFI-165 induces antidepressant activity in vivo. IRFI-165 can be used for the research of psychiatric and neurological disorders .
    IRFI-165
  • HY-182687

    Adenosine Receptor Neurological Disease
    MRS7469 is a highly selective A1 adenosine receptor (A1AR) agonist with over 2000-fold selectivity over other adenosine receptor subtypes. MRS7469 stably binds to the orthosteric binding site of A1AR, and exhibits extremely high affinity for both humans and mice (e.g., human pKi is 8.67, mouse pKi is 9.43). By activating central A1AR, MRS7469 significantly induces hypothermia, motor inhibition and psychomotor dysfunction, and can be widely used in research related to depression and other relevant fields .
    MRS7469
  • HY-182518

    Adenosine Receptor Neurological Disease
    MDL-102234 is a potent and selective adenosine A1 receptor antagonist with a Ki value of 23.2 nM at the adenosine A1 receptor. MDL-102234 can be used for the study of cognition enhancement-related neural functions .
    MDL-102234

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