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PF mouse models

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12

Inhibitors & Agonists

1

Inhibitory Antibodies

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-118952A
    PF-06456384 trihydrochloride

    		Sodium Channel Neurological Disease
    PF-06456384 trihydrochloride is an extremely potent and selective Nav1.7 sodium channel blocker (IC50: 0.01 nM for hNaV1.7; 75 nM for rNaV1.7; <0.1 nM for mNaV1.7). PF-06456384 trihydrochloride shows no significant analgesic efficacy in the mouse Formalin pain model .
    PF-06456384 trihydrochloride
  • HY-178821
    ROCK2-IN-12

    		ROCK TGF-beta/Smad STAT Inflammation/Immunology
    ROCK2-IN-12 (Compound A25) is a selective ROCK2 inhibitor with an IC50 of 7.0  nM for ROCK2 over ROCK1. ROCK2-IN-12 has potent antifibrotic effects via the TGF-β/Smad and ROCK2/STAT3 signaling pathways. ROCK2-IN-12 significantly reduces collagen deposition and reverses fibrotic progression in Bleomycin (HY-108345)-induced pulmonary fibrosis (PF) mouse models. ROCK2-IN-12 can be used for lung diseases like pulmonary fibrosis research .
    ROCK2-IN-12
  • HY-12788
    PF-04449613

    		Phosphodiesterase (PDE) Neurological Disease
    PF-04449613 is a selective PDE9A inhibitor with an IC50 of 22 nM[1]. PF-04449613 improved motor learning ability in a mouse model[2].
    PF-04449613
  • HY-170780
    DSM1465

    		Parasite Dihydroorotate Dehydrogenase Infection
    DSM1465 (Compound 82) is a potent, selective inhibitor of P. falciparum dihydroorotate dehydrogenase (PfDHODH) with an IC50 value of 15 nM, inhibits P. falciparum 3D7 (Pf3D7) parasites with an EC50 value of 1.4 nM. DSM1465 shows potent in vivo activity in the humanized P. falciparum mouse model .
    DSM1465
  • HY-143286A
    PF15 TFA

    		PROTACs FLT3 Cancer
    PF15 TFA is a PROTAC connected by ligands for FLT3 kinase and CRBN. PF15 TFA is a high selective FLT3-ITD degrader，with a DC50 of 76.7 nM. PF15 TFA significantly inhibits the proliferation of FLT3-ITD-positive cells，can down-regulate the phosphorylation of FLT3 and STAT5. PF15 TFA also inhibits tumor growth in mouse models and can be used in study of leukemia .
    PF15 TFA
  • HY-143286
    PF15

    		PROTACs FLT3 Cancer
    PF15 is a PROTAC connected by ligands for FLT3 kinase and CRBN. PF15 is a high selective FLT3-ITD degrader, with a DC50 of 76.7 nM. PF15 significantly inhibits the proliferation of FLT3-ITD-positive cells, can down-regulate the phosphorylation of FLT3 and STAT5. PF15 also inhibits tumor growth in mouse models and can be used in study of leukemia .
    PF15
  • HY-12788A
    (S)-PF-04449613

    		Phosphodiesterase (PDE) Neurological Disease
    (S)-PF-04449613 is the left-handed isomer of PF-04449613 (HY-12788). PF-04449613 is a selective PDE9A inhibitor with an IC50 of 22 nM. PF-04449613 improves motor learning ability in a mouse model .
    (S)-PF-04449613
  • HY-172953
    Insecticidal agent 24

    		Parasite Infection
    Insecticidal agent 24 is an orally active pyridylspiroindoline frontrunner. Insecticidal agent 24 has antiplasmodial activity (Pf NF54 IC50: 0.08 μM). Insecticidal agent 24 inhibits hERG activity (IC50: 6.5 μM). Insecticidal agent 24 reduces parasitemia in a humanized immunodeficient NSG mouse Plasmodium falciparum infection model .
    Insecticidal agent 24
  • HY-178147
    Antimalarial agent 52

    		Parasite Infection
    Antimalarial agent 52 is an orally active formation of synthetic hemozoin (β-hematin) inhibitor with an IC50 of 6.6 μM. Antimalarial agent 52 exhibits in vitro antiplasmodial activity against P. falciparum Pf3D7, PfDd2 strains and P. knowlesi with IC50s of 6.1, 6.4 and 3.3 nM. Antimalarial agent 52 remain highly effective against multidrug-resistant strains and demonstrates curative activity in the P. berghei mouse model .
    Antimalarial agent 52
  • HY-163765
    Antimalarial agent 41

    		PI4K Potassium Channel Infection
    Antimalarial agent 41 (Compound 17) exhibits antimalarial activity, which inhibits Plasmodium falciparum with an IC50 of 40 nM (NF54 strain) and 76 nM (K1 strain). Antimalarial agent 41 is an inhibitor for P. falciparum phosphatidylinositol-4-kinase β (Pf PI4K) and hERG channel, with an IC50 of 53 nM and 3 μM. Antimalarial agent 41 exhibits cytotoxicity to CHO cells with an IC50 of 34 μM. Antimalarial agent 41 ameliorates the malaria infection and exhibits good pharmacokinetic characters in mouse models .
    Antimalarial agent 41
  • HY-123965
    PF-06745013

    		MAP4K TNF Receptor Metabolic Disease Cancer
    PF-06745013 (Compound 37) is a MAP4K4 inhibitor without time-dependent inhibition (TDI) risk of CYP3A4 (IC50 of 0.4  nM for MAP4K4). PF-06745013 has no accumulation CNS-impaired and non-ATP competitive activities in mouse models. PF-06745013 can be used for inflammatory diseases like diabetes and cancers research .
    PF-06745013
  • HY-P992439
    PF-06747143

    		CXCR Cancer
    PF-06747143 is recombinant anti-human antibody targeting CXCR4. PF-06747143 blocks CXCL12-induced calcium flux, F-actin polymerization, chemotaxis, cell migration, and leukemic cell bone marrow homing. PF-06747143 reduces tumor burden and improves survival in mouse models of hematologic malignancies. PF-06747143 can be used for the research of chronic lymphocytic leukemia, acute myeloid leukemia, and hematologic malignancies .
    PF-06747143

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