pyrazinamide

Pyrazinamide (Pyrazinecarboxamide), an antimycobacterial, is utilized therapeutically as an antitubercular agent, which is a synthetic pyrazinoic acid amide derivative.

Pyrazinamide (Standard) is the standard substance of Pyrazinamide, and it is applicable for quantitative analysis, quality control, and related research in biochemical experiments. Pyrazinamide (Pyrazinecarboxamide), an antimycobacterial, is utilized therapeutically as an antitubercular agent, which is a synthetic pyrazinoic acid amide derivative.

Pyrazinamide-KLH is a hapten-carrier protein conjugate formed by coupling Pyrazinamide to keyhole limpet hemocyanin (KLH). As a hapten, Pyrazinamide alone cannot induce an immune response and must be conjugated to a large molecular protein to become a complete antigen with immunogenicity. Pyrazinamide-KLH may be supplied as a lyophilized powder or as a solution. The solution is prepared in 0.01 M PBS (pH 7.4) buffer at a typical concentration of 1 mg/mL.

Pyrazinamide-BSA is a hapten-carrier protein conjugate formed by coupling Pyrazinamide to bovine serum albumin (BSA). As a hapten, Pyrazinamide alone cannot induce an immune response and must be conjugated to a large molecular protein to become a complete antigen with immunogenicity. Pyrazinamide-BSA may be supplied as a lyophilized powder or as a solution. The solution is prepared in 0.01 M PBS (pH 7.4) buffer at a typical concentration of 1 mg/mL.

Pyrazinamide-d3 is a deuterated compound of Pyrazinamide. Pyrazinamide has a CAS number of 98-96-4. Pyrazinamide, an antimycobacterial, is utilized therapeutically as an antitubercular agent, which is a synthetic pyrazinoic acid amide derivative.

5-Hydroxypyrazine-2-Carboxylic Acid is a metabolite of anti-tuberculosis drug pyrazinamide.

OPC-167832 is a potent and orally active dprE1 Inhibitor with an IC50 of 0.258 μM. OPC-167832 has antituberculosis activity and can be used for the research of tuberculosis caused by Mycobacterium tuberculosis[1]. OPC-167832 exhibits very low MICs against laboratory strains of M. tuberculosis H37Rv (MIC: 0.0005 μg/ml) and Kurono (MIC: 0.0005 μg/ml) and strains with monoresistance to rifampin (RIF), isoniazid (INH), ethambutol (EMB), streptomycin (STR), and pyrazinamide (PZA) (MIC: 0.00024-0.001 μg/ml). However, OPC-167832 has minimal or no activity against standard strains of nonmycobacterial aerobic and anaerobic bacteria[1].The IC90 values of OPC-167832 against intracellular M. tuberculosis strains H37Rv and Kurono are 0.0048 and 0.0027 μg/ml, respectively. OPC-167832 shows bactericidal activity against intracellular M. tuberculosis at a low concentration, and the bactericidal activity is saturated at concentrations of 0.004 μg/ml or higher[1]. OPC-167832 (oral administration; 0.625-10 mg/kg) exhibits a good pharmacokinetic characteristic. The plasma reaches peak at 0.5 h to 1.0 h (tmax) and is eliminated with a half-life (t1/2) of 1.3 h to 2.1 h OPC-167832 distribution in the lungs is approximately 2 times higher than that in plasma, and the Cmax and AUCt of OPC-167832 in plasma and the lungs shows dose dependency[1].OPC-167832 (oral administration; 0.625-10 mg/kg; 4 weeks) significantly reduces lung CFU compared to the vehicle group. The dose-dependent decrease of lung CFU is observed from 0.625 mg/kg to 2.5 mg/kg. In a M. tuberculosis Kurono-infected ICR female mice model. OPC-167832 combines with DMD, BDQ, or LVX via oral gavage exhibits significantly higher efficacies than each single agent alone[1].[1].OPC-167832 (oral gavage; 2.5 mg/kg; combination with DCMB; 12 weeks) demonstrates the most potent efficacy when compares with DC, DCB. The lung CFU count after 6 weeks of treatment is below the detection limit, and at the end of just 8 weeks of treatment, the bacteria in the lungs of all the evaluated mice had already been eradicate[1]. [1]. Norimitsu Hariguchi, et al. OPC-167832, a Novel Carbostyril Derivative with Potent Antituberculosis Activity as a DprE1 Inhibitor.Antimicrob Agents Chemother. 2020 May 21;64(6):e02020-19.