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pharmacokinetic parameters

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11

Inhibitors & Agonists

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Inhibitory Antibodies

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-P99814

    AMG-701

    CD3 Inflammation/Immunology Cancer
    Pavurutamab (AMG-701) is a bispecific T cell engager molecule that anti-CD3 and anti-B cell maturation antigens (BCMA). Pavurutamab has an extended half-life based on Pacanalotamab (HY-P99798). The Fc of Pavurutamab is coupled to molecules to improve pharmacokinetic parameters. Pavurutamab has potential applications in immune regulation and multiple myeloma (MM) .
    Pavurutamab
  • HY-123367

    Platelet-activating Factor Receptor (PAFR) Others
    Rubraxanthone is a compound with multiple biological activities. Its pharmacokinetic parameters were determined in mice and it showed a certain concentration variation pattern in plasma after oral administration.
    Rubraxanthone
  • HY-118683

    Potassium Channel Others
    KR-31378 is a neuroprotectant with dose-dependent pharmacokinetic properties and relevant activity in rats. After intravenous and oral administration of KR-31378 in rats, its pharmacokinetic parameters showed dose-dependent changes, such as decreased clearance with increasing doses, good oral absorption, and comparable AUCs for intravenous and oral administration at different doses.
    KR-31378
  • HY-A0148B

    (-)-SKF-102886 free base; (-)-WR-171669

    Parasite Infection
    (-)-Halofantrine ((-)-SKF-102886 free base; (-)-WR-171669) is an inhibitor of the malignant malaria parasite (P. falciparum) and targets multidrug-resistant P. falciparum. The pharmacokinetic parameters of (-)-Halofantrine in rats vary depending on the route of administration, distinguishing it from other isomers .
    (-)-Halofantrine
  • HY-170895

    HSP Na+/K+ ATPase Cancer
    Hsp90-IN-38 (compound 20m) is a HSP90 (heat shock protein) inhibitor. Hsp90-IN-38 exhibits strong HSP90 binding affinity with a Kd of 87 nM. Hsp90-IN-38 inhibits ATPase with an IC50 of 0.13 μM. Hsp90-IN-38 inhibits HCT116, MCF-7, SKBr3, K562 and A549 cells with IC50s of 0.187, 0.072, 0.105, 0.403 and 031 μM, respectively .
    Hsp90-IN-38
  • HY-151625

    PARP Apoptosis Cancer
    PARP-2-IN-3 (Compound 12) is a potent PARP-2 inhibitor with an IC50 of 0.07 μM. PARP-2-IN-3 induces apoptosis and necrosis in cancer cells. PARP-2-IN-3 shows appropriate predicted pharmacokinetic parameters and oral bioavailability .
    PARP-2-IN-3
  • HY-117831

    Bacterial Antibiotic Endogenous Metabolite Infection
    NSC-79887 is a nucleoside hydrolase (NH) inhibitor with activity against Bacillus anthracis. NSC-79887 is considered a good candidate inhibitor of nucleoside hydrolases for biological testing and further development. The pharmacokinetic (ADMET) prediction of NSC-79887 showed that all physicochemical parameters were within the acceptable range for human use .
    NSC-79887
  • HY-146662

    PGE synthase Inflammation/Immunology
    HPGDS inhibitor 3 is an orally active and highly potent peripherally restricted hematopoietic prostaglandin D synthase (H-PGDS) inhibitor with IC50 value of 9.4 nM and EC50 of 42 nM, respectively. HPGDS inhibitor 3 exhibits good selectivity, good pharmacokinetic parameters in mouse, rat, and dog, and no CNS toxicity. HPGDS inhibitor 3 has anti-inflammatory activity .
    HPGDS inhibitor 3
  • HY-128794

    Sodium Channel Neurological Disease
    PF-05150122 is a novel potent and selective human Nav1.7 channel blocker with the activity of inhibiting human pain signaling. PF-05150122 exhibited favorable biopharmacokinetic parameters in microdose studies, providing a basis for exploring its application in acute or chronic pain inhibition. The pharmacokinetic model of PF-05150122 predicted that at the corresponding oral dose, it could effectively reduce the 50% inhibitory concentration (IC50) of Nav1.7, demonstrating its inhibitory potential .
    PF-05150122
  • HY-121535

    Sodium Channel Calcium Channel Others
    Levosemotiadil, an S-isomer of semotiadil, exhibits stronger binding affinity to human serum albumin (HSA) compared to its R-isomer counterpart. This study utilized high-performance frontal analysis (HPFA) to demonstrate that levosemotiadil binds approximately three times more strongly to HSA than semotiadil. The binding parameters were evaluated using Scatchard analysis, revealing specific interactions with the diazepam binding site on HSA. The presence of diazepam decreased the binding affinity of both enantiomers, while warfarin did not alter their binding characteristics. These findings highlight levosemotiadil's potential as a Ca- and Na-channel blocker with significant binding preferences for HSA, crucial for understanding its pharmacokinetics and therapeutic effects .
    Levosemotiadil
  • HY-174425

    Cytochrome P450 Cancer
    CYP1B1-IN-9 is a highly selective and competitive CYP1B1 Inhibitor with IC50 values of 1.48 nM, > 100 μM, and > 80 μM for CYP1B1, CYP1A1, and CYP1A2, respectively. CYP1B1-IN-9 significantly inhibits the migration and invasion of A549/T cells. CYP1B1-IN-9 has the ability to resensitize Paclitaxel (HY-B0015)-resistant cells, and good metabolic stability and safety, and shows favorable pharmacokinetic parameters. CYP1B1-IN-9 can be used for the study of tumor-drug resistance .
    CYP1B1-IN-9

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