as-101

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.

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

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).

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.

Foslevcromakalim (QLS-101), an ATP-sensitive potassium channel opener, serves as a proagent for ocular hypotensive effects [1] [2].

11-cisRetinol is an isomer of vitamin A . It is formed from vitamin A,viaatrans-retinyl ester intermediate, by the enzyme RPE65 in the retinal pigment epithelium and then converted to 11-cis retinal as part of the visual cycle.1,211-cisRetinol is an agonist of salamander and human red rod opsins expressed in COS cells and an inverse agonist of salamander red cone opsin, as well as human red and green cone opsins expressed in COS cells.3It promotes pigment formation in cone, but not rod, photoreceptors. 1.Rando, R.R.The biochemistry of the visual cycleChem. Rev.101(7)1881-1896(2001) 2.Guignard, T.J.P., Jin, M., Pequignot, M.O., et al.FATP1 inhibits 11-cis retinol formation via interaction with the visual cycle retinoid isomerase RPE65 and lecithin: Retinol acyltransferaseJ. Biol. Chem.285(24)18759-18768(2010) 3.Ala-Laurila, P., Cornwall, M.C., Crouch, R.K., et al.The action of 11-cis-retinol on cone opsins and intact cone photoreceptorsJ. Biol. Chem.284(24)16492-16500(2009)

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.

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

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

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.

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, also known as ENS-101, is an experimental medication which originated from Roche and is under development by Evotec AG for the treatment of major depressive disorder. It acts as a selective NMDA receptor subunit 2B (NR2B) antagonist.

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. .

VH 101, a thiol (compound 20), serves as a VHL ligand essential for PROTAC synthesis [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].

Caveolin-1 (82-101) amide (human, mouse, rat), also known as Caveolin-1 scaffolding domain peptide, mitigates aging-related detrimental alterations in various organs and inhibits tyrosine kinases [1].

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].

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.

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.

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.

Kynurenic acid, an active metabolite of tryptophan, is synthesized through a kynurenine intermediate by kynurenine aminotransferases (KATs). It acts as an antagonist of both NMDA and AMPA receptors, as well as α7 nicotinic acetylcholine receptors (nAChRs; EC50s = 235, 101, and 7 µM, respectively), and functions as an agonist for the aryl hydrocarbon receptor (AhR) and G protein-coupled receptor 35 (GPR35; EC50s = 1.4 and 39 µM, respectively). In a neonatal rat model of cerebral hypoxic-ischemia, induced by carotid artery ligation, administration of kynurenic acid at 300 mg kg prevents weight loss in the lesioned hemisphere. Additionally, at concentrations of 1 and 5 mg ml, it protects against neurodegeneration in the rhabdomere of the eye in an Htt93QtransgenicDrosophila model of Huntington's disease. Elevated levels of kynurenic acid in the cerebrospinal fluid have been observed in patients with schizophrenia.

Sotiburafusp alfa is a humanized bispecific fusion protein comprising a VEGFR-1 extracellular domain fragment (129-228, 1-100 in the current sequence) connected through a 101 GGSGGSGGSGGSGGS 115 peptide linker to the N-terminus (116-564) of a humanized IgG1-kappa anti-human PD-L1 heavy chain with L352>A and L353>A mutations. Additionally, sotiburafusp alfa functions as an angiogenesis inhibitor [1].

Becotatug (JMT-101) is an IgG1 antibody targeting EGFR, which can be conjugated to Afatinib and Osimertinib, serving as a synthetic antibody-drug conjugate (ADC) [1].