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.

RG-101 is a hepatocyte-targeted N-acetylgalactosamine conjugated oligonucleotide that functions as an antagonist for miR-122, an essential host factor in the replication of the hepatitis C virus (HCV).

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

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.

Complement component C3 plays a particularly versatile role in this process by keeping the cascade alert, acting as a point of convergence of activation pathways, fueling the amplification of the complement response, exerting direct effector functions, and helping to coordinate downstream immune responses[3]. In C3-/- mice alcohol-induced liver steatosis is absent or strongly reduced after chronic or acute alcohol exposure. This suggests that the complement system and its component C3 contribute to the development of alcohol-induced fatty liver and its consequences[4].AMY-101 TFA (Cp40 TFA) is a peptidic inhibitor of the central complement component C3 (KD: 0.5 nM). It shows a favorable anti-inflammatory activity in models with COVID-19 severe pneumonia with systemic hyper inflammation[5].a daily subcutaneous dose of AMY-101 (4 mg/kg bodyweight) was protective against NHP periodontitis, suggesting that patients treated for systemic disorders (e.g., paroxysmal nocturnal hemoglobinuria) can additionally benefit in terms of improved periodontal condition[6].Plasma concentrations of both C3 and Cp40 were measured periodically and complete saturation of plasma C3 was confirmed. No differences in hematological, biochemical, or immunological parameters were identified in the blood or tissues of animals treated with Cp40 when compared to those injected with vehicle alone. Further, skin wounds showed no signs of infection in those treated with Cp40.Cp40 treatment was associated with a trend toward accelerated wound healing when compared with the control group. In addition, a biodistribution study in a rhesus monkey indicated that the distribution of Cp40 in the body is associated with the presence of C3, concentrating in organs that accumulate blood and produce C3[7].

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.

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.

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.

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. .

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.

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].

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].

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.

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.

VH 101, a thiol (compound 20), serves as a VHL ligand essential for PROTAC synthesis [1].

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].

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.