18 products were found matching "Cay11910"!

Substituted cathinones, like ethcathinone, are psychoactive compounds commonly used as recreational drugs. Some have amphetamine-like effects. 2-Ethylethcathinone (hydrochloride) is a substituted cathinone with potential for abuse. Its biological and toxicological properties have not been evaluated. This product is...

JWH 018 is a potent, synthetic cannabinoid which has been identified in herbal blends and incense. (±)-JWH 018 N-(2-hydroxypentyl) metabolite is a potential metabolite of JWH 018. Monohydroxylation of the alkyl side chain of JWH 018 occurs through cytochrome P450 action, resulting in metabolites, like (±)-JWH 018...

Olopatadine is a histamine H1 receptor antagonist (Ki =41 nM). It is 1,059- and 4,177-fold selective for histamine H1 over H2 and H3 receptors, respectively. Olopatadine inhibits histamine-induced phosphoinositide turnover in isolated human conjunctival epithelial cells, isolated human corneal fibroblasts, and human...

SJ 172550 is an inhibitor of MDMX that disrupts MDMX-p53 peptide interaction with an EC50 value of 4.3 µM. It forms a covalent, but reversible, cysteine adduct in the MDMX p53-binding domain, locking MDMX into a conformation that prevents binding to p53. SJ 172550 induces apoptosis, increases p53 target gene...

CBL0137 is a metabolically stable curaxin that activates p53 with an EC50 value of 0.37 µM and inhibits NF-kappaB with an EC50 of 0.47 µM. It functionally inactivates the facilitates chromatin transcription complex (FACT), driving the effects on p53 and NF-kappaB and promoting cancer cell death. CBL0137 has broad...

Sodium-hydrogen exchangers (NHE) are involved in maintaining sodium and pH balance in a variety of tissues. They are also known as sodium-hydrogen antiporters and solute carrier family 9 members. 5-(N,N-dimethyl)-Amiloride (DMA) inhibits NHE1, NHE2, and NHE3 with Ki values of 0.02, 0.25, and 14 µM, respectively....

Hypoxia-inducible factor 1alpha (HIF-1alpha) turnover is initiated by prolyl hydroxylases (PHD), which hydroxylate proline residues on HIF-1alpha, facilitating ubiquitination. PHD activity is linked to the tricarboxylic acid (TCA) cycle, since the intermediate alpha-ketoglutarate is a PHD substrate and succinate and...

(S)-Mephenytoin is a substrate of the cytochrome P450 (CYP) isoform CYP2C19, also known as mephenytoin 4-hydroxylase. CYP2C19 metabolizes a variety of therapeutic agents, including omeprazole, proguanil, diazepam, propranolol, citalopram, imipramine, and certain barbiturates. Genetic defects in CYP2C19 result in...

Retinoic acid receptor-related nuclear receptor gamma (RORgamma) plays a central role in T cell differentiation, particularly in the differentiation of pro-inflammatory TH17 cells, which are implicated in autoimmune diseases like multiple sclerosis and rheumatoid arthritis. SR 2211 selectively binds RORgamma (Ki =...

Triptolide is a diterpenoid triepoxide that has been found in T. wilfordii and has diverse biological activities. It inhibits dCTP pyrophosphatase 1 (Ki = 168 µM), an enzyme that prevents halogenated nucleotides from entering DNA synthesis. It reduces viability of A549, H1299, NCI H520, NCI H1650, and H1975 human...

Anastrozole is an aromatase/CYP19A1 inhibitor (IC50 = 15 nM for human placental aromatase/CYP19A1). It is selective for aromatase/CYP19A1 over the cytochrome P450 (CYP) isoforms CYP1A2, CYP2A6, CYP2C9, CYP2D6, and CYP3A (IC50s = 27-650 µM). Anastrozole (0.1 mg/kg) blocks ovulation in mature female rats and...

Ro 67-7476 is a positive allosteric modulator of metabotropic glutamate receptor 1 (mGluR1) that enhances glutamate-induced calcium release in HEK293 cells expressing rat mGluR1a (EC50 = 1.74 µM). It is selective for rat mGluR1 over rat mGluR2, mGluR4, and mGluR8 at a concentration of 10 µM. Ro 67-7476 increases the...