variant

Ensitrelvir (S-217622) is an orally active inhibitor of SARS-CoV-2 3CL protease with IC50 of 13 nM.

Quinaldic acid is an endogenous metabolite.Quinaldic acid is a metal chelator.

MK-2206 dihydrochloride (MK-2206 2HCl) is a variant Akt inhibitor that inhibits Akt1, Akt2, and Akt3 (IC50=8/12/65 nM) with orally active, highly potent and selective potency. MK-2206 dihydrochloride exhibits antitumor activity.

Linvencorvir is a hepatitis B virus (HBV) core protein variant modifier used to treat chronic HBV infection.

BI-4020 is a fourth-generation, orally active, and non-covalent inhibitor of EGFR tyrosine kinase. It exhibits activity against the triple mutant EGFR del19 T790M C797S variant (IC50=0.2 nM in BaF3 cell lines), the double mutant EGFR del19 T790M and primary mutant EGFR del19 (IC50=1 nM), and EGFR wt (IC50=190 nM). BI-4020 also shows high kinome selectivity and good DMPK properties.

AF-710B is a specific variant of M1 muscarinic and Sigma-1 receptor agonist used in the study of neurological disorders such as Alzheimer's disease dementia and schizophrenia.

BMS-929075 is an orally active HCV NS5B replicase (HCV NS5B replicase) palm site variant inhibitor with potency, high oral bioavailability and pharmacokinetic parameters.BMS-929075 shows cytotoxicity.

PSB-16133 sodium is a selective P2Y purine receptor variant antagonist with an IC of 233 nM.

AZD 3043 (THRX 918661) is a variant modulator of the γ-aminobutyric acid type A receptor, a novel sedative-hypnotic and a potential short-acting anesthetic that produces hypnosis and EEG suppression in rats.AZD 3043 potentiates the γ-aminobutyric acid type A receptor and inhibits neuronal nicotinic acetylcholine receptors.

SKF83959, a benzazepine analog, is a selective and potent partial agonist of the dopamine D1 receptor with Ki values of 1.18, 7.56, 920, and 399 nM for rat D1, D5, D2, and D3 receptors, respectively.SKF83959 is a potent variant modulator of the sigma (σ)-1 receptor, which ameliorates cognitive dysfunction for the study depression and Alzheimer's disease.

2-Nitrobenzoic acid (o-Nitrobenzoic acid) is a antiproliferation agent. 2-Nitrobenzoic acid shows IC50 of 8.3 μM to jurkat cell line expressing T type calcium channel alpha 1H or its splice variant delta 25.

PZL-A, an activator of mtDNA synthesis, restored the function and activity of the most common POLγ mutant variant and activated mtDNA synthesis in the cells of pediatric patients with fatal diseases, thereby enhancing the oxidative phosphorylation mechanism and the biogenesis of cellular respiration, and can be used to treat progressive diseases associated with mtDNA depletion.

OVA G4 peptide acetate(148274-82-2 free base) (SIIGFEKL acetate) is a variant of the agonist ovalbumin (OVA) peptide (257-264), SIINFEKL. OVA Peptide is a class I (Kb)-restricted peptide epitope of ovalbumin presented by the class I MHC (major histocompatibility complex) molecule, H-2Kb (class I genes of the mouse MHC).

CMP-Sialic acid sodium salt (CMP-Neu5Ac sodium salt) is a variant inhibitor of UDP-GlcNAc 2-epimerase, the activated form of sialic acid, which is widely found in animals and is involved in the metabolism of organisms.

Edaravone, a novel and potent free radical scavenger, effectively prevents MMP-9-related brain hemorrhage in rats treated with tissue plasminogen activator. Its deuterium-labeled variant, Edaravone D5, retains the original compound's attributes while offering isotopic labeling benefits.

Sofosbuvir's enantiomer, a variant of the prescription medication Sofosbuvir used for chronic hepatitis C treatment, currently lacks reported biological activity.

Ethacrynic acid, a diuretic, functions as an inhibitor of L-type voltage-dependent and store-operated calcium channels, facilitating the relaxation of airway smooth muscle (ASM) cells. It exhibits anti-inflammatory effects, notably reducing retinoid-induced ear edema in mice, and inhibits glutathione S-transferases (GSTs), making it a potent suppressor of the NF-kB signaling pathway. Additionally, ethacrynic acid modulates leukotriene formation. A variant, Ethacrynic acid D5, is distinguished by its deuterium labeling.

Ezetimibe D4, a deuterium-labeled variant of Ezetimibe, functions as an inhibitor of Niemann-Pick C1-like1 (NPC1L1) and is recognized for its potent activation of Nrf2.

Glutaminase-IN-1 (CB839 derivative), a novel 1,3,4-selenodiazepine inhibitor of the renal-type glutaminase (KGA) variant, exhibited antitumor activity in an aggressive H22 hepatocellular carcinoma xenograft model.

KRAS inhibitor-6 is a potent inhibitor of the KRAS G12C variant.

Loperamide D6 hydrochloride, a deuterium-labeled variant of Loperamide hydrochloride, acts as an opioid receptor agonist utilized for diarrhea treatment.

Mitoquinone mesylate (MitoQ10 mesylate) is a potent TRAP1 inhibitor (IC50=0.2 μM). Mitoquinone mesylate is an antioxidant that prevents oxidative damage and targets mitochondria of TPP.

Posaconazole-D4, a deuterium-labeled variant of Posaconazole, is a broad-spectrum, second-generation triazole with antifungal activity.

Posaconazole-D5, a deuterium-labeled variant of Posaconazole, is a second-generation, broad-spectrum triazole compound with antifungal activity.