orally available

Inavolisib (GDC-0077) is an orally available selective PI3Kα inhibitor with an IC50 value of 0.038 nM.It exerts its activity by binding to the ATP-binding site of PI3K, thereby inhibiting the phosphorylation of PIP2 to PIP3.

MSA-2 is an orally available non-nucleotide STING agonist. The non-covalent dimer of MSA-2 binds to STING with nanomolar affinity. It shows anti-tumor activity in syngeneic mouse tumor models, synergizes with anti-PD-1, stimulates tumor secretion of interferon-β, induces tumor regression, and has long-lasting anti-tumor immunity. [3]

Syrosingopine is a dual inhibitor of MCT1 and MCT4, 60 times more potent against MCT4, preventing lactate and H+ efflux. Syrosingopine is an orally available antihypertensive drug with potential for cancer research in combination with metformin.

Cl-amidine hydrochloride is an orally available PAD inhibitor that blocks histone 3 deimination and neutrophil extracellular trap formation and improves survival in septic mice. It induces apoptosis in cancer cells and induces miR-16 to cause cell cycle arrest.

Orforglipron (LY3502970; GLP-1 receptor agonist 1) is an orally available glucagon-like peptide (GLP-1) receptor agonist for the study of obesity and type 1 diabetes in adults.

Navtemadlin (AMG232) is a potent, selective and orally available inhibitor of p53-MDM2 interaction (IC50: 0.6 nM). It binds to MDM2 with a Kd of 0.045 nM.

EZM 2302 (GSK3359088) is a selective, and orally available arginine methyltransferase CARM1 inhibitor (IC50: 6 nM).[1]

SX-682 is an orally available allosteric inhibitor of CXCR1 and CXCR2 that blocks tumor myeloid suppressor cell recruitment and enhances T cell activation and anti-tumor immunity, with the potential to treat castration-resistant prostate cancer.

PT2399 shows effective antitumor activity in vivo. PT2399 is an effective and selective HIF-2α antagonist, which directly binds to the HIF-2α PAS B domain (IC50: 6 nM).

LSN3318839 is a potent and orally available glucagon-like peptide-1 receptor (GLP-1R) modulator.LSN3318839 enhances GLP-1R G-protein-coupled signaling and can be used to lower blood glucose.

GLPG3970 GLPG3970 is a novel orally available selective dual SIK2/SIK3 inhibitor.GLPG3970 has potential anti-inflammatory activity for the study of autoimmune diseases.

AU-224 is an orally available benzamide derivative that is a potent gastrointestinal prokinetic.

Beclobrate (Sgd 24774) is a novel orally available fibric acid derivative that has shown significant lipid and cholesterol-lowering activity in rodents and may be used in the study of primary hyperlipoproteinemia.

Tegadifur (40497S) is an orally available antitumor compound with antimetabolic effects, often used with uracil and in the treatment of rectal adenocarcinoma.

AZD8309 is a potent, orally available antagonist of the chemokine receptor CXCR2 that regulates neutrophil transport, significantly reduces MPO in the pancreas and lung, and decreases trypsin and elastase activity in the pancreas.AZD8309 can be used to study a range of inflammatory diseases.

Tilomisole (Wy 18251) is an orally available benzimidazole thiazole with anti-inflammatory activity and immunomodulatory activity.Tilomisole is used in the study of cancer and inflammation.

Verofylline (Verofyllinum) is an orally available, long-acting, multiacting, methylxanthine-substituted bronchodilator with inhibitory effects on PDE4 for the treatment of asthma disease research obesity.

Furaprofen is an orally available, selective and potent HCV inhibitor with anti-inflammatory activity, inhibits carrageenan-induced paw edema in rats and inhibits cotton pellet-induced granulomas in rats at higher doses.

MK-8353 (SCH900353) is a potent, selective, and orally available inhibitor of ERK1 2 with IC50 values of 23.0 nM and 8.8 nM, respectively.

Clopimozide (R-29764) acts as a calcium channel antagonist and inhibits [3H] nilandipine binding.Clopimozide is a novel and orally available long-acting antischizophrenic psychostatic compound.

CFTR corrector 4 is a potent and orally available transmembrane conductance regulator (CFTR) for cystic fibrosis and is a potent (R,R) type active enantiomer. CFTR corrector 4 increases CFTR levels on the cell surface and is a potential compound for the study of cystic fibrosis.

Dimethandrolone Undecanoate (DMAU) is a novel orally available androgen with progestational activity and is a potential male contraceptive compound.

BL-1020 Mesylate (CYP-1020 Mesylate) is an orally available GABA A receptor agonist and D2 antagonist that decreases dopamine activity and enhances GABAA activity.BL-1020 Mesylate has been used in the study of schizophrenia, Alzheimer's disease, and bi-directional cognitive impairment.

DDP-38003 dihydrochloride is an orally available histone lysine-specific demethylase 1A (KDM1A/LSD1) inhibitor (IC50: 84 nM).

WIN 54954 is an orally available antiviral agent that inhibits Coxsackievirus and inhibits viral translation or transcription.WIN 54954 may be useful in the study of small ribonucleic acid virus infections.

Mifentidine (DA 4577) is an orally available H2 receptor antagonist for the study of gastric emptying and experimental gastric and duodenal ulcers.

WAY-260022 is an orally available and selective norepinephrine transporter protein inhibitor that displays inhibitory effects on serotonin and dopamine transporter proteins.

Dazolicin HCl (Dazolicine HCl) is an orally available antiarrhythmic compound.

Elismetrep (MT-8554) is an orally available TRPM8 inhibitor with potential analgesic activity for the study of vasomotor symptoms in postmenopausal women.

Eribaxaban (PD348292) is an orally available factor Xa inhibitor for the prevention and treatment of venous thromboembolism.

Androgen receptor antagonist 1, an orally available full androgen receptor antagonist (IC50: 59 nM), is utilized in the synthesis of PROTAC AR degraders, achieving 24% and 47% AR protein degradation in LNCaP cells at concentrations of 1 μM and 10 μM, respectively.

SARS-CoV-2-IN-38 is an orally available SARS-CoV-2 inhibitor with potential antiviral activity for the study of SARS viral infections.

Floctafenine (R-4318) is an orally available nonsteroidal anti-inflammatory compound that is a COX-I and COX-2 inhibitor and interferes with the antiplatelet effects of aspirin.Floctafenine has analgesic activity and is used in the study of pain.

Fezolamine is a novel orally available non-tricyclic compound with antidepressant activity. It is three to two times more selective in blocking synaptosomal uptake of [3H]norepinephrine than uptake of [4H]3-hydroxytryptamine or [3H]dopamine in vitro. It blocked the inhibitory effects of rifampicin and tetraphenyl in classical behavioral tests using monoamine-depleted animals.

MK-0686 is an orally available bradykinin B1 receptor antagonist with potential anti-inflammatory activity.

Anidoxime HCl (USVP-E142) is a novel orally available compound with anti-analgesic activity.

SCH 221510 is an orally available, selective and potent NOP agonist with an EC50 of 12 nM and a Ki of 0.3 nM.SCH 221510 has anxiolytic activity and can be used to study neurological disorders.

(Rac)-Modipafantis an orally available and selective platelet-activating factor receptor (PAFR) antagonist that inhibits PAF-induced aggregation of washed platelets in rabbits, and can be used to study arthritis and ischemia reperfusion (I R) in the superior mesenteric artery (SMA) of the rat.

MB07803 is an orally available prodrug of an effective, noncompetitive inhibitor of fructose 1,6-bisphosphatase (FBPase) (EC50: 140 nM and t1/2 of 7.6±2.9 h).This compound is unstable in powder form and other related salt forms are recommended.

SB 243213 is an orally available and selective 5-HT2C receptor antagonist.SB 243213 has anxiolytic and antidepressant activity and is used in schizophrenia and movement disorders.

Isomazole is a novel orally available phosphodiesterase (PDE) inhibitor with calcium-sensitizing properties that inhibits PDE3 and PDE4.

Ezurpimtrostat hydrochloride (GNS561 hydrochloride) is an orally available palmitoyl protein thioesterase-1 inhibitor with antifibrotic, antiviral, and anticancer effects that blocks cancer cell proliferation by interacting with palmitoyl protein thioesterase to inhibit late autophagy and dose-dependently increase lysosomal accumulation.

Besifovir PM (LB80331 PM) is an analogue of Besifovir, a novel orally available acyclic nucleotide phosphonate for the treatment of chronic hepatitis B infection.

NP10679 is an orally available, selective, brain-penetrating, potent, and pH-sensitive N-methyl-D-aspartate (NMDA) receptor inhibitor of the GluN2B subunit.NP10679 inhibits histamine H1, hERG channels, and CYP enzymes, and may be useful in the study of epilepsy and ischemic stroke.

Pavinetant (MLE-4901) is an orally available neurokinin-3 receptor (NK3R) antagonist used to improve menopausal symptoms.

KB-5492 free base is an orally available and selective antiulcer agent that inhibits sigma receptors, inhibits [3H]1,3-di(2-tolyl)guanidine (DTG) binding to sigma receptors, and may be useful in the study of gastric lesions and gastric secretion.

CSN5i-3 is a potent, selective, and orally available inhibitor of the proteolytic subunit of the CSN complex, CSN5. It inhibits CSN-catalyzed Cul1 deneddylation with an IC50 value of 5.8 nM. CSN5i-3 has a killing effect on a variety of cancer cells and can be used as an anticancer drug. [2]

Leminoprazole is an orally available H+,K(+)-ATPase inhibitor that protects gastric mucosal cells from various cellular damages.