rodent-active

AHR antagonist 5 free base is an orally active AHR antagonist with IC50 of approximately 35-150 nM in human and rodent cell lines, and exhibits anticancer activity.

SB-277011 hydrochloride (SB-277011A hydrochloride) is a potent, selective, and orally active dopamine D3 receptor (D3R) antagonist that crosses the blood-brain barrier, with Ki values of 10.7 nM for rodent D3R and 11.2 nM for human D3R. It is 80-100 times more selective for D3 receptors than other dopamine receptors, acting on D3 receptors (pKi: 8.0), D2 receptors (pKi: 6.0), 5-HT1B receptors (pKi < 5.2), and 5-HT1D receptors (pKi: 5.9).

Apoptone is a synthetic analogue of 3β-androstanediol which is an orally bioavailable anticancer agent. Apoptone is active in rodent models of prostate and breast cancer [1].

PF-0463481 is safe and well-tolerated and has the potential for the study of diabetic nephropathy. PF-0463481 is an effective and orally active dual CCR2 CCR5 antagonist. It also has comparable human and rodent CCR2 potency (rat IC50=20.8 nM). PF-0463481

Tebuquine is an antimalarial agent. Tebuquine is active against P. falciparum in vitro. Tebuquine in vitro shows a chloroquine-like effect, but not in vivo, suggesting that its mode of action in vivo is different from that of chloroquine. Tebuquine has no

PF-0463481 succinate is a potent and orally active dual antagonist of CCR2 CCR5, exhibiting comparable human and rodent CCR2 potency with an IC50 of 20.8 nM.

Lu AF27139 is an effective and selective antagonist of P2X7 receptor (IC50s of 12 and 2.4 nM for human and rat, Kis of 22, 54, and 13 nM for mouse, human, and rat, respectively). Lu AF27139 can be used in CNS diseases studies.

CVN417 is an orally active antagonist of nAChR containing the α6 subunit, modulating phasic dopaminergic neurotransmission in an impulse-dependent fashion. It inhibits Ca(2+) efflux through nAChR subunits, displaying IC50 values of 0.086 μM (α6), 2.56 μM (α3), and 0.657 μM (α4). CVN417 has shown efficacy in reducing resting tremor in rodent models, suggesting a potential to ameliorate movement disorders in conditions like Parkinson's disease [1].

ML753286 has high permeability and low to medium clearance in rodent and human liver S9 fractions. ML753286 is an orally active and selective inhibitor of BCRP (IC50: 0.6 μM). It is also stable in plasma across species.

APJ receptor agonist 5 (compound 3) is a potent and orally active apelin receptor (APJ) agonist (EC 50: 0.4 nM) with excellent pharmacokinetic profiles in rodent heart failure (HF) models and an acceptable safety profile in preclinical toxicology studies, improving cardiac function and useful for HF disease research.

MAO-B-IN-4 (Compound 26) is a reversible monoamine oxidase B (MAO-B) inhibitor with potent in vitro activity, characterized by an IC50 value of 9 nM. This orally active compound exhibits favorable metabolic stability, a satisfactory safety profile, and effective brain permeability. Demonstrating antidepressant effects in rodent models, MAO-B-IN-4 is suitable for research into Alzheimer's disease [1].

CP-346086 dihydrate is a potent, orally active inhibitor of microsomal triglyceride transfer protein (MTP), with an IC50 of 2.0 nM for both human and rodent MTP, effectively lowering plasma cholesterol and triglyceride levels in vivo.

APJ Receptor Agonist 4 is a potent, orally active apelin receptor (APJ) agonist, demonstrating an EC50 of 0.06 nM and a Ki of 0.07 nM. It exhibits excellent pharmacokinetic profiles in rodent heart failure (HF) models and has shown an acceptable safety profile in preclinical toxicology studies. This compound effectively improves cardiac function, making it valuable for research into HF disease.

Hemoregulatory peptide 5b is a synthetic analog of granulocyte chalone which initially identified in extracts of rodent bone marrow and human leukocytes. Monomer inhibits both formations of GM-CFC colonies and cytotoxic drug-induced recruitment of murine

Deethylindanomycin is a polyether antibiotic that has been found in S. setonii. It is active against a variety of Gram-positive bacteria, including various strains of S. aureus and Streptococcus, as well as one strain of S. pneumoniae (MICs = 4, 4, and 2 μg ml, respectively). It is also active against coccidia in vitro, inhibiting E. tenella development, but is inactive against E. tenella infection in chicks when administered at a dose of 200 μg g in the diet. Deethylindanomycin acts as an ionophore in lipid bilayer membranes and is more selective for potassium ions than calcium, magnesium, and sodium ions. It induces histamine release from rodent mast cells and human basophils in vitro in a calcium-dependent manner.

ARUK3001185 (Compound 8l) is a potent, selective, orally active, and brain-penetrant Notum inhibitor (IC50 = 6.7 nM), suitable for oral dosing in rodent models of disease [1].

Connexin mimetic peptide 40,37GAP26, a biologically active peptide, matches the GAP26 domain of the extracellular loop of major vascular connexins Cx37 and Cx40, referred to as 37,40Gap26 based on Cx homology. It has been utilized to examine gap junctions' involvement in propagating endothelial hyperpolarizations induced by cyclopiazonic acid (CPA) in the rodent iliac artery wall. Abundant gap junction plaques comprising Cx37 and Cx40 are present in the endothelium, and the peptide exerts inhibitory actions on subintimal hyperpolarization.

'(6R)-ML753286, an isomer of ML753286, is an orally active, selective Breast Cancer Resistance Protein (BCRP) inhibitor, demonstrating an IC50 of 0.6 μM. It exhibits high permeability and low to medium clearance in rodent and human liver S9 fractions, with cross-species plasma stability [1].'