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Results for "

Pharmacokinetic optimization

" in MedChemExpress (MCE) Product Catalog:

5

Inhibitors & Agonists

1

Biochemical Assay Reagents

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-151798
    TDI-11861

    		Adenylate Cyclase Others
    TDI-11861 is an orally active soluble sAC inhibitor optimized and designed based on TDI-10229 (HY-132298), with an IC50 of 3.3 nM and a KD of 1.4 nM. TDI-11861 has advantages such as high affinity, slow dissociation, and good pharmacokinetics. TDI-11861 can be used for research on male contraception and related sAC pharmacology .
    TDI-11861
  • HY-W008201
    tert-Butyl 3-formylpyrrolidine-1-carboxylate

    		Drug Intermediate Inflammation/Immunology
    tert-Butyl 3-formylpyrrolidine-1-carboxylate is a drug intermediate that can be used for the synthesis nonpeptidic αvβ6 Integrin inhibitors .
    tert-Butyl 3-formylpyrrolidine-1-carboxylate
  • HY-167876
    PQR514

    		PI3K Cancer
    PQR514 is a potent PI3K inhibitor with anticancer activity. PQR514 is able to inhibit cancer cell proliferation. PQR514 showed significant antitumor activity in the OVCAR-3 xenograft model, with the required concentration being approximately one-eighth that of PQR309. PQR514 has good pharmacokinetic properties and minimal brain penetration, making it an optimized candidate compound for inhibiting systemic tumors .
    PQR514
  • HY-135495
    AM-0466

    		Sodium Channel Histamine Receptor Inflammation/Immunology
    AM-0466 is a sodium channel inhibitor with nanomolar levels of NaV1.7 inhibitory activity. AM-0466 exhibits potent pharmacodynamic activity in a NaV1.7-dependent histamine-induced itch model. AM-0466 also showed significant analgesic effects in capsaicin-induced pain models. After optimizing its pharmacokinetic properties, AM-0466 was advanced into in vivo targeting and efficacy models for testing .
    AM-0466
  • HY-13590
    CEP-7055

    		VEGFR Cancer
    CEP-7055 (compound 21) is a novel vascular endothelial growth factor R2 (VEGF-R2) tyrosine kinase inhibitor with potent inhibitory activity. Studies have found that the inhibitor activity can be significantly improved by optimizing the R9 substituent. Compound 21 has potent low nanomolar inhibition of human VEGF-R tyrosine kinase and shows good selectivity against multiple tyrosine and serine/threonine kinases. N,N-dimethylglycine ester 40 was prepared to improve its water solubility and oral bioavailability. In animal pharmacokinetic studies, a significant increase in the plasma level of 21 was observed after oral administration of 40. Compound 21 showed significant in vivo antitumor activity in multiple tumor models and has entered phase I clinical trials as a water-soluble N,N-dimethylglycine ester proagent of 40 (CEP-7055).
    CEP-7055

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