as-101

Ossirene (AS101), a potent in vitro and in vivo immunomodulator, is a novel inhibitor of IL-1beta converting enzyme.

LAS101057 is a novel orally available and potent and selective A2B receptor antagonist for the study of asthma.

Diphenylmethane ,with CAS No. 101-81-5, is a fragment molecule that serves as an important scaffold for molecular linking, expansion, and modification. Diphenylmethane provides a structural basis and research tool for the design and screening of novel drug candidates, and is commonly used in drug discovery, drug synthesis, and related research.

Nortriptyline hydrochloride (ELF-101 hydrochloride) is a metabolite of AMITRIPTYLINE that is also used as an antidepressive agent. Nortriptyline is used in major depression, dysthymia, and atypical depressions.

VH 101, phenol is a VHL ligand based on VH032. It is able to utilize linkers to ligands of target proteins to yield PROTAC molecules such as PROTAC 1. PROTAC 1 is a partial degrader of SMARCA2 and SMARCA4.

Compound I-25, also known as SMARCA2-IN-2, is a SMARCA2 inhibitor (IC 50: 101-500 μM) with applications in cancer research.

Prodipine (also known as BY-101) is a diphenylpiperidine derivative used as a compound for treating Parkinson's disease.

STAT3-IN-37 (Compound 101) is an inhibitor of STAT3, with an IC50 of 15 nM as measured by DNA-HTRF assay and 2 nM as determined through human whole blood SOCS3 qPCR assay.

PAD4-IN-5 (Example 18) is a PAD4 inhibitor with an IC50 of ≤10 nM at 50 µM Ca2+ and 101-500 nM at 1 mM Ca2+ against human PAD4 (hPAD4). This compound is applicable in the study of autoimmune diseases such as rheumatoid arthritis (RA).

AR antagonist 14 serves as a ligand for the target protein in PROTAC applications. It can be coupled with VH 101-amide-piperidine-Pip-alkyne to synthesize the PROTAC degrader [ARD-69].

Zeleciment basivarsen (DYNE-101) is an antibody oligonucleotide conjugate (AOC), consisting of a Fab antibody named Zeleciment that binds to the transferrin receptor 1 (TfR1) on muscle cells, and an antisense oligonucleotide known as Basivarsen. This compound targets the RNA of the mutant dystrophia myotonica-protein kinase (DMPK) for RNase H-mediated degradation, and is utilized in the study of myotonic dystrophy type 1 (DM1).

Viquidacin ( NXL-101) is an oral/intravenous antibiotic that targets Gram-positive bacteria such as MRSA. In 2008, Novexel announced it had discontinued the development of Viquidacin (NXL 101).

11-cis Retinol is an isomer of vitamin A, serving as an agonist for red rod optochromin and an inverse agonist for red cone optochromin.

OY-101, an orally active compound, serves as a potent and specific inhibitor of P-glycoprotein (P-gp). It has the capability to sensitize drug-resistant tumors and counteract tumor multidrug resistance efficiently. Compared to Tetrandrine [1], OY-101 demonstrates enhanced water-solubility, cytotoxicity, and reversal activity.

Ceftolozane, also known as FR-264,205 and CXA-101; is an antibiotic drug from the cephalosporin family, approved for the treatment of infections with gram-negative bacteria, or gram-positive bacteria. Ceftolozane is of great benefit due to its ability to target bacteria that have become resistant to conventional antibiotics. Ceftolozane is combined with the β-lactamase inhibitor tazobactam, as multi-drug resistant bacterial infections will generally show resistance to all β-lactam antibiotics unless this enzyme is inhibited. .

EVT-101 free base, also known as ENS-101, is an experimental compound for investigations involving major depressive disorder. EVT-101 free base functions as a selective antagonist of the NMDA receptor subunit 2B (NR2B). EVT-101 free base is applicable to neuropharmacology, glutamatergic neurotransmission, and central nervous system signaling research.

INU-101 is an 11β-HSD1 inhibitor. In KKAy mice, ob/ob mice, and ZDF rats, oral administration of INU-101 led to enhanced insulin sensitivity and the lowering of the fasting level of glucose in the blood. INU-101 therefore shows promise as a potential treatment for type 2 diabetes and metabolic syndrome.

KR-67607, also known as NTX-101 is novel selective 11β-hydroxysteroid dehydrogenase 1 (11β-HSD1) inhibitor. KR-67607 decreased 4-hydroxynonenal expression and increased antioxidant and mucus secretion in BAC-treated rat eyes. KR-67607 showed its protective effects against ischemia-reperfusion-induced eye injury. KR-67607 effectively reduced cortisol levels in mouse eyes and maintained the trabecular meshwork (TM) structure in the presence of transient ischemic stress. Furthermore, KR-67607 reversed the elevation of intra-ocular pressure (IOP), suggesting that the TM structure maintained by KR-67607 prevented the excessive rise in IOP that exacerbates glaucoma.

Vidofludimus hemicalcium (4sc-101; SC12267) is an orally active compound that acts as a dihydroorotate dehydrogenase (DHODH) inhibitor and serves as a novel modulator of the farnesoid X receptor (FXR). This immunomodulatory agent is utilized in the research of autoimmune disorders, including inflammatory bowel disease (IBD), and is explored for its potential in fatty liver disease research through FXR targeting.

VMY-1-101 is a synthesized fluorescent CDK inhibitor. VMY-1-101 demonstrates potent CDK inhibitory activity, enhanced induction of G2/M arrest and modest apoptosis as compared to purvalanol B.

EVT-101 is a GluN2B antagonist, binding at the same GluN1/GluN2B dimer interface as ifenprodil but adopting a remarkably different binding mode involving a distinct subcavity and receptor interactions.

Foslevcromakalim (QLS-101) is an adenosine triphosphate-sensitive potassium channel (KATP) opener that is converted to its active form by alkaline phosphatase in vivo. It reduces intraocular pressure in normotensive mice and is suitable for glaucoma research.

HCV Core Protein (107-114), identified as the binding site within the region 101-118, is a minimally immunogenic fragment of the primary linear HCV core regions. This segment, comprising two residues that vary between genotypes I/II and III/VI, represents a potential focal point for the dissemination of HCV serotypes [1].

WM-586 is a covalent inhibitor of WDR5 that impedes the WDR5-MYC binding. It selectively reduces the interaction between WDR5 and MYC with an IC50 value of 101 nM, as determined by the HTRF assay [1].