hydrate

Meclofenamate sodium is a potent non-steroidal anti-inflammatory agent, which can specifically inhibit chemokine-induced human polymorphonuclear leukocyte function: chemotaxis, degranulation, and superoxide anion free radical production.

Cefadroxil is a first generation aminocephalosporin with good patient compliance, a long-acting therapeutic effect, high solubility and relatively broad spectrum of anti-bacterial activity. Cefadroxil is also a substrate of the intestinal peptide transporter PepT1, which is primarily responsible for the drug's uptake across the apical membrane of small intestine.

A-317491 sodium salt hydrate is a non-nucleotide P2X3 and P2X2/3 receptor antagonist that inhibits receptor-mediated calcium flux.

Bavisant dihydrochloride hydrate (JNJ31001074AAC) is a highly selective, orally active antagonist of the human H3 receptor with a novel mechanism of action related to wakefulness and cognition, and it has potential as a treatment for ADHD. In a clinical trial, the mean change from baseline in the total ADHD-RS-IV score at day 42 was -8.8 in the placebo group versus -9.3, -11.2, and -12.2 in the bavisant 1 mg/day, 3 mg/day, and 10 mg/day groups, respectively; however, the change in the 10 mg/day group was not statistically superior to placebo (p=0.161). Statistical comparisons of the 1 mg/day and 3 mg/day groups with placebo based on a step-down closed testing procedure were not performed. Bavisant has completed a phase II ADHD trial, but no results have been reported [1]. Clinical trial: A Study to Characterize the Pharmacokinetics and Effect of Food on JNJ-31001074 in Healthy Volunteers. Phase 2. IC50 Value: Target: H3 receptor in vitro.

BIX-01338 hydrate is an inhibitor of histone lysine methyltransferase.

Fanapanel hydrate is a highly selective antagonist of AMPA/kainate with little activity against NMDA(Ki of 3.2 nM, 100 nM, and 8.5 μM against quisqualate, kainate, and NMDA, respectively).

Zoniporide hydrochloride hydrate is a potent and selective sodium-hydrogen exchanger type 1 (NHE-1) inhibitor. Zoniporide hydrochloride hydrate inhibits human NHE-1 with IC50 of 14 nM.

Ivacaftor hydrate is an orally bioavailable CFTR potentiator. It also is used for cystic fibrosis treatment.

Ribociclib succinate hydrate is a highly specific CDK4/6 inhibitor (IC50s: 10 nM and 39 nM, respectively). It also is over 1,000-fold less potent against the cyclin B/CDK1 complex.

Napsagatran hydrate is a novel and specific thrombin inhibitor.

Pritelivir mesylate hydrate is active against herpes simplex virus types 1 and 2 (IC50: 0.02 μM against HSV1-2). Pritelivir mesylate hydrate is an inhibitor of the viral helicase-primase complex. Pritelivir mesylate hydrate shows antiviral activity in vit

Hydroxypyruvic acid lithium hydrate is an intermediate in the metabolism of serine, glycine, and threonine. It is a substrate for serine-pyruvate aminotransferase and glyoxylate reductase/hydroxypyruvate reductase.

(2R,4R)-APDC hydrate ((2R,4R)-4-Aminopyrrolidine-2,4-dicarboxylic acid hydrate) is an agonist for group II metabotropic glutamate receptors (mGluR). It influences cell proliferation by inhibiting glutamate release, enhancing motor responses generated by D1 receptor activation, or reducing brain-derived neurotrophic factor (BDNF) levels. This compound is applicable in research on epilepsy and other neurological disorders.

Gemigliptin (LC15-0444) tartrate hydrate is a selective, reversible, and competitive inhibitor of dipeptidyl peptidase 4 (DPP-4), with an IC50 value of 10.3 nM for human recombinant DPP-4. It exhibits strong anti-glycation properties and is used in research on advanced glycation end product-related diabetic complications.

Grazoprevir, a second generation hepatitis C virus protease inhibitor acting at the NS3/4a protease targets, has good activity against a range of hepatitis C virus genotype variants, including some that are resistant to most currently used antiviral medic

Fluconazole (hydrate) is a triazole antifungal agent used for oral treatment and prevention of both superficial and systemic fungal infections, including but not limited to balanitis, various Candida infections, Cryptococcus infections, dermatomycosis, and fungal infections of the respiratory and urinary tracts. As the hydrate salt form of fluconazole, it exhibits antifungal activity by inhibiting the growth and development of pathogenic fungi, such as Candida species, at minimal inhibitory concentrations often exceeding 100 mg/l. Notably, it disrupts the branching and hyphal formation in C. albicans at concentrations as low as 0.3 mg/l, indicating its potency compared to other antifungals like miconazole and ketoconazole which are effective at 100-fold lower concentrations. Clinical studies have not shown a significant increase in the risk of most birth defects with oral fluconazole, although there may be an associated risk of tetralogy of Fallot. Its efficacy against Cryptococcus gattii in koalas suggests it may be ineffective as a sole therapeutic agent at a dosage of 10 mg/kg orally every 12 h. Toxicity symptoms from overdose can include hallucinations and paranoid behavior.

Adenosine kinase is the key metabolizing enzyme regulating cellular adenosine concentrations. Inhibition of adenosine kinase can selectively enhance the protective actions of adenosine during tissue trauma without producing the nonspecific effects associa

Felbamate hydrate is an effective nonsedative anticonvulsant. It is a clinical effect that may be related to the inhibition of N-methyl-D-aspartate.

Zanamivir hydrate is neuraminidase inhibitors. It is used worldwide for the treatment and prophylaxis of influenza caused by influenza A and B viruses.

Prasterone is an endogenous steroid hormone. Prasterone acts as an agonist at ERβ, NMDA, and σ1 receptors, a partial agonist at ERα and AR, and antagonist at GABA-A receptors. It displays a variety of biologocial activities, including enhancing working me

Ambazone hydrate has anti-cancer activity.

DX-9065A is a factor Xa inhibitor. DX-9065a inhibits proinflammatory events induced by factor Xa and gingipains. DX-9065a is a competitive inhibitor of the Spectrozyme FXa (SpFXa) cleavage by both fXa and prothrombinase with similar K(i) values of approxi

Quinaprilat is the active metabolite of quinapril, an angiotensin-converting enzyme inhibitor used in the treatment of congestive heart failure and hypertension.

CGP77675 hydrate is an orally active, potent inhibitor of Src family kinases. It inhibits the phosphorylation of peptide substrates and autophosphorylation of purified Src (IC50: 5-20 and 40 nM, respectively), as well as Src, EGFR, KDR, v-Abl, and Lck with IC50s of 0.02, 0.15, 1.0, 0.31, and 0.29 μM, respectively. CGP77675 hydrate may be useful for treating diseases associated with elevated bone loss and has anticancer activity [1].