pharmacokinetic

An antibiotic produced by Streptomyces fradiae.

Belzutifan (MK-6482) is a potential treatment for clear cell renal cell carcinoma (ccRCC). Belzutifan is an orally active and selective HIF-2α inhibitor (IC50: 9 nM). Belzutifan , as a second-generation HIF-2α inhibitor, increases potency and improves pharmacokinetic profile.

TC ASK 10 is a potent, selective and orally active inhibitor of apoptosis signal-regulating kinase 1 (ASK1)(IC50 of 14 nM).

Atabecestat (JNJ-54861911) is a potent, brain-penetrant, and orally active β-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitor that achieves robust and high CSF Aβ reduction, is well-tolerated, and displays sustained pharmacokinetic (PK) and pharmacodynamic (PD) characteristics. Atabecestat (JNJ-54861911) has the potential for Alzheimer's Disease treatment[1].

Aβ-IN-1 is a novel, potent and orally active γ-secretase modulator (GSM). Aβ-IN-1 potently reduced Aβ42 levels with an IC 50 value of 0.091 μM in cultured cells without inhibiting CYP3A4. Aβ-IN-1 shows a sustained pharmacokinetic profile.

HS271 is a selective, highly potent and orally active IRAK4 inhibitor (IC50= 7.2 μM). HS271 shows excellent enzymatic and cellular activities, as well as excellent pharmacokinetic properties.

ZW4864 (free base) is an orally active and selective β-catenin B-Cell lymphoma 9 protein-protein interaction (β-catenin BCL9 PPI) inhibitor, with a K_i value of 0.76 μM and an IC_50 value of 0.87 μM [1]. ZW4864 (free base) also demonstrates good pharmacokinetic properties.

CCT365623 is an orally bioavailable Lysyl Oxidase inhibitor with good anti-LOX potency, selectivity, pharmacokinetic properties, as well as anti-metastatic efficacy.

BMS-929075 is an orally active HCV NS5B replicase (HCV NS5B replicase) palm site variant inhibitor with potency, high oral bioavailability and pharmacokinetic parameters.BMS-929075 shows cytotoxicity.

Fosfomycin calcium (Phosphomycin calcium salt) is a blood-brain barrier penetrating, broad-spectrum antibiotic by irreversibly inhibiting an early stage in cell wall synthesis.

Fosfomycin sodium is a bactericidal, low-molecular weight, broad-spectrum antibiotic, with putative activity against several bacteria, including multidrug-resistant Gram-negative bacteria, by irreversibly inhibiting an early stage in cell wall synthesis.

Ensartinib (X-396) is a potent dual ALK MET inhibitor with IC50 values of <0.4 nM for ALK and 0.74 nM for MET.

Torin 2(IC50=0.25 nM), a specific and effective mTOR inhibitor, is the 800-fold greater specific activity for mTOR than PI3K and improves pharmacokinetic properties. The EC50 of Torin 2 for ATM ATR DNA-PK inhibition is 28 nM 35 nM 118 nM, respectively.

TDI-10229 is a potent and orally available inhibitor of soluble adenylyl cyclase (sAC, ADCY10), displaying nanomolar inhibition of sAC in both biochemical and cellular assays (IC50 = 195 nM). TDI-10229 exhibits mouse pharmacokinetic properties sufficient to warrant its use as an in vivo tool compound.

GNF-5 is a specific non-ATP competitive inhibitor of Bcr-Abl (IC50: 0.22±0.1 uM, Wild-type Abl). It is an analog of GNF-2 with improved pharmacokinetic properties.

PDS-0330 is a claudin-1 small molecule inhibitor inhibitor.PDS-0330 inhibits claudin-1-dependent CRC progression and binds directly and specifically to claudin-1 with micromolar affinity.PDS-0330 exhibits well characterized pharmacokinetic properties with antitumor and Chemosensitizing activity.PDS-0330 interferes with claudin-1 Src association to inhibit CRC progression and metastasis.

FAPI-34, a fibroblast-activating protein (FAP) inhibitor, boasts advantageous pharmacokinetic and biochemical attributes.

NPR-C activator 1 (Compound 1) is a potent agonist (EC50 ~ 1 μM) of natriuretic peptide receptor C (NPR-C), which plays a crucial role in regulating vascular homeostasis, and demonstrates promising in vivo pharmacokinetic properties [1].

Aβ42-IN-1, compound 1v, is a novel, potent and orally active γ-secretase modulator (GSM). Aβ42-IN-1 potently reduced Aβ42 levels with an IC 50 value of 0.091 μM in cultured cells without inhibiting CYP3A4. Aβ42-IN-1 shows a sustained pharmacokinetic profile.

HCV-IN-7 is an orally active and potent pan-genotypic HCV NS5A inhibitor (IC50s: 3-47 pM) with a superior pan-genotypic profile, good pharmacokinetic properties, and favorable liver uptake.

3,4-Dehydro Cilostazol (OPC-13015), an active metabolite of Cilostazol, is used for pharmacokinetic studies[1].

Anti bacterial agent 236 (Compound 4l), an orally effective inhibitor of DNA gyrase and topoisomerase IV (with IC50 values of 3.2 and 300 nM in Staphylococcus aureus, respectively), exhibits broad-spectrum antibacterial activity. It also demonstrates favorable pharmacokinetic properties in mice.

Apoptosisinducer 25 (Compound 4H) demonstrates potent anticancer capabilities by inhibiting the proliferation of BGC-823 cancer cells with an IC50 of 0.37 μM. It induces apoptosis in BGC-823 cells, causes mitochondrial dysfunction, and arrests the cell cycle at the G2 M phase. Additionally, Apoptosisinducer 25 exhibits favorable pharmacokinetic properties in rats.

G-631 acts as a selective tankyrase inhibitor, effectively hindering tankyrase auto-PARsylation (poly ADP ribosylation) at an IC 50 of 7 nM and suppressing the Wnt signaling pathway. This compound also demonstrates favorable pharmacokinetic properties in mice.