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stereospecificity

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9

Inhibitors & Agonists

1

Oligonucleotides

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-128599

    PARP Cancer
    NMS-P515 is a potent, orally active and stereospecific PARP-1 inhibitor, with a Kd of 16 nM and an IC50 of 27 nM (in Hela cells). Anti-tumor activity .
    NMS-P515
  • HY-148755

    Others Cancer
    ERX-41 is an orally active and stereospecific small molecule targeting to lysosomal acid lipase A (LIPA). ERX-41 induces endoplasmic reticulum (ER) stress resulting in cell death, indicating a function independent of LIPA but dependent on its ER localization. ERX-41 involves in a targeted strategy for solid tumors .
    ERX-41
  • HY-12483

    PPAR Metabolic Disease
    SR1664 is a PPARγ antagonist. SR1664 binds to PPARγ and potently inhibits Cdk5-mediated PPARγ phosphorylation (IC50=80 nM; Ki= 28.67 nM) .
    SR1664
  • HY-15314
    Ranirestat
    1 Publications Verification

    AS-3201

    Aldose Reductase Neurological Disease Metabolic Disease
    Ranirestat (AS-3201) potent and orally active aldose reductase (AR) inhibitor with IC50s of 11 nM and 15 nM for rat lens AR and recombinant human AR, respectively, and a Ki of 0.38 nM for recombinant human AR. Ranirestat has the potential for diabetic sensorimotor polyneuropathy treatment. Ranirestat also has a neuroprotective effect on diabetic retinas .
    Ranirestat
  • HY-116284A

    Methyl β-D-glucoside hemihydrate

    Others Others
    Methyl β-D-glucopyranoside (Methyl β-D-glucoside) hemihydrate is a hemihydrate compound. Methyl β-D-glucopyranoside hemihydrate less reactive at higher PH. The formation of Methyl β-D-glucopyranoside hemihydrate is stereospecific .
    Methyl β-D-glucopyranoside hemihydrate
  • HY-118833

    Others Cardiovascular Disease
    RAC 109 is a local anesthetic. RAC 109 reduces ventricular conduction velocity and myocardial contractility in rabbits in a stereospecific manner (EC50=30 μM) .
    RAC 109
  • HY-W353804

    Nucleoside Antimetabolite/Analog Infection
    2'-Deoxy-β-L-uridine is a nucledside analogue and a specific substrate for the viral enzyme, shows no stereospecificity against herpes simplex 1 (HSV1) thymidine kinase (TK). 2′-Deoxy-β-L-uridine exerts antiviral activity via the interation of 5'-triphosphates with the viral DNA polymerase .
    2′-Deoxy-β-L-uridine
  • HY-P2987

    Endogenous Metabolite Metabolic Disease
    L-Amino acid oxidase is a homodimeric proteins containing flavin adenine dinucleotide. L-Amino acid oxidase can catalyze the stereospecific oxidative deamination of L-amino acids to α-keto acids and ammonia .
    L-Amino acid oxidase
  • HY-117811

    L-680574

    Others Others
    (R,R)-MK 287 is a tetrahydrofuran derivative that effectively inhibits the binding of [3H]C18-PAF to human platelets, polymorphonuclear leukocytes (PMNs), and lung membranes with K1 values of 6.1 ± 1.5, 3.2 ± 0.7, and 5.49 ± 2.3 nM, respectively. The inhibition is stereospecific and competitive. Its racemate, L-668,750, is less potent, and its enantiomer, L-680574, is only 1/20 as potent as MK 287. MK 287 inhibits the binding of [3H]C18-PAF to human PMN membranes, reducing the affinity of the radioligand without changing the number of receptor sites. The binding of other radioligands (e.g., LTB4, LTC4, C5a, FMLP) to their specific receptors is unchanged at 1-10 microM MK 287. [3H]MK 287 binds to human platelet and PMN membranes with KD values of 2.1 ± 0.6 and 2.9 ± 1.2 nM. When tested on isolated human cells, MK 287 potently and selectively inhibits PAF-induced platelet aggregation (ED50 = 56 ± 38 nM or ED50 = 1.5 ± 0.5 nM for gel-filtered platelets) and elastase release from PMNs (ED50 = 4.4 ± 2.6 nM). In vivo studies, MK 287 inhibited PAF-induced lethality in mice (ED50 = 0.8 mg/kg oral) and PAF-induced bronchospasm in guinea pigs (ED50 = 0.18 mg/kg intraduodenally and 0.19 mg/kg intravenously). The inhibition of PAF-induced bronchospasm was accompanied by a rightward shift in the concentration-response curve for PAF-induced platelet aggregation measured in vitro.
    (R,R)-MK 287

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