dose-dependent

Brr2-IN-3 (Brr2 Inhibitor C9) is an allosteric inhibitor of the spliceosomal RNA helicase Brr2. Brr2 is implicated in autosomal-dominant retinitis pigmentosa (a group of progressive retinal degenerative disorders).

MCL0020 is a potent and selective melanocortin MC4 receptor antagonist (IC50 values are 11.63, 1115, and >10,000 nM at MC4, MC3, and MC1 receptors, respectively). It significantly reverses stress-induced anorexia without affecting food intake in free-feeding rats and exhibits anxiolytic-like activity in vivo.

AKT Kinase Inhibitor is an Akt inhibitor with antitumor activity that selectively inhibits cell proliferation in a dose-dependent manner.

AT-121 is a dual μ-opioid and neuropeptide receptor partial agonist (Kis 16.49 and 3.67 nM, respectively). It stimulates [35S]GTPγS binding to cell membranes expressing either μ-opioid receptors or neuropeptide receptors (EC50s of 19.6 and 34.7 nM, respectively.) AT-121 (0.003-0.03 mg/kg) reduced capsaicin-induced thermal anisocoria in a dose-dependent manner, but did not increase scratching activity in rhesus monkeys. In rhesus monkey drug self-administration tests, AT-121 at doses of 0.3 to 10 μg/kg per injection lacked reinforcing effects (a potential marker of abuse) and did not reduce the reinforcing effects of food pellets.AT-121 (0.01 or 0.03 mg/kg) did not induce hyperalgesia, a marker of tolerance, in rhesus monkeys.AT-121 is a safe non-addictive pain reliever with anti-injury and analgesic effects.

Punicalin exerts anti-inflammatory, antioxidative, and anti-hepatotoxic activities, it shows inhibitory activity on HIV-1 reverse transcriptase in a dose-dependent manner, with an IC50 of 0.11 microg/ml (0.14 microM).

Tirzepatide sodium is the sodium salt form of a dual glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP) receptor agonist peptide drug that enhances insulin secretion and improves glycemic control by simultaneously activating GIP and GLP-1 receptors. In research and clinical settings, Tirzepatide sodium has also demonstrated effects in reducing body weight and improving metabolic parameters, and is used in studies related to type 2 diabetes and metabolic disorders.

Kv3 modulator 1 is an imidazolidinedione-type orthosteric modulator of Kv3 voltage-gated potassium channels. Kv3 modulator 1 reverses mechanical hyperalgesia in rat models of neuropathic and inflammatory pain, with rapid onset and sustained, dose-dependent effects. Kv3 modulator 1 can be used to study the mechanisms underlying inflammatory pain and neurological disorders such as epilepsy and schizophrenia.

Dirlotapide (CP742033) is an MTP inhibitor, an intestine-selective microsomal triglyceride transfer protein inhibitor that reduces food intake by increasing peptide YY release, and is used for weight reduction in diabetic dogs.

RH1 (NSC 697726) is a bioreductive anticancer compound that exhibits dose-dependent biphasic effects in vitro, inducing apoptosis at higher doses and senescence at lower doses.

LOM612 is a potent and specific FOXO relocator that induces nuclear translocation of the FOXO3a reporter protein as well as endogenous FOXO3a and FOXO1 in a dose-dependent manner in U2OS cells, down-regulates the expression of c-Myc and cyclin D1, and has anti-proliferative effects in human cancer cell lines.

RPH-2823, a basic amphotericin analog, is diuretic, natriuretic, and potassium-preserving, inducing a dose-dependent decrease in SCC and an increase in trans-epithelial resistance.

Molindone ((±)-Molindone) is a therapeutic antipsychotic used to treat schizophrenia by blocking the action of dopamine in the brain. molindone is often used in combination with serotonin in a dose-dependent manner to increase errors and decrease response rates.

Stemazole is a novel small molecule human stem/progenitor cell proliferation activator that promotes the survival of human embryonic stem cells and maintains stemness, and promotes the survival of oligodendrocyte precursor cells in vitro. Stemazole significantly increased cell survival and clone formation in a dose-dependent manner, reduced apoptosis, and promoted recovery of motor dysfunction and myelin repair. Stemazole can be used as a therapeutic agent in demyelinating disorders, promoting OPC survival in vitro and regeneration in vivo.

AMC-01 has potential antiviral activity and induces dose- and time-dependent inactivation of eIF2-α via phosphorylation of serine residue 51. AMC-01 can be used to study atherosclerosis and Parkinson's syndrome.

CGP 20376 is a benzothiazole compound, an anthelmintic, with dual dose-dependent modulation of in vitro effects on the respiratory burst of eosinophils and antifibrillatory properties.

Opc 8490 is a cardiotonic agent and a positive inotropic vasodilator that increases Ca current (ICa) in a dose-dependent and reversible manner and prolongs atrial action potential in a concentration-dependent manner.

Vesnarinone (Arkin) (INN) is a mixed phosphodiesterase 3 inhibitor and ion-channel modifier that has modest, dose-dependent, positive inotropic activity, but minimal negative chronotropic activity. It also suppresses cell proliferation and induces apoptosis by inducing the expression of p21, an inhibitor of cyclin-dependent kinase activity in p53-mediated cell cycle arrest.

AKN-028 is an orally active and potent FLT3 tyrosine kinase inhibitor ( IC 50 = 6 nM). AKN-028 causes dose-dependent inhibition of FLT3 autophosphorylation.

Sterculic acid, a stearoyl-CoA desaturase-1 (SCD1) inhibitor, effectively suppresses delta-9 desaturase (Δ9D) activity in a dose-dependent manner, exhibiting an inhibition concentration (IC50) value of 0.9 μM [1].

α-NETA is a potent choline acetyltransferase (ChA) inhibitor and an ALDH1A1 and chemokine-like receptor 1 (CMKLR1) antagonist.Anti-cancer activity,Cholinesterase and acetylcholinesterase (AChE) inhibition,Dose-dependent reduction of body weight and fasting blood glucose levels in STZ-induced diabetic mice,Significantly reduced expression of renal injury markers,May be CEP-9722 can be used for the study of diabetic nephropathy.

Spiroglumide, a CCKB-gastrin antagonist that inhibits dose-dependent pentagastrin-induced acid hypersecretion with an ID50 of 20.1 (8.67-46.4) mg / kg, could be used to explore the physiological role of gastrin in the regulation of human gastric acid secretion.

Tiflucarbine is a potential non-selective 5-HT agonist with antidepressant activity.Tiflucarbine dose-dependently increased the specific activity of soluble calmodulin (CaM)-dependent phosphodiesterase in rat brain.

Sergliflozin A is a selective SGLT2 inhibitor that induces diabetes in a dose-dependent manner. It reduces hyperglycemia.

Pincainide is a novel beta-aminoaniline that inhibits, in a dose-dependent manner, diseases caused by abnormal norepinephrine vascular smooth muscle function.