Prothionamide-d₅  (Synonyms: 丙硫异烟胺-d₅; Protionamide-d₅)

Prothionamide-d₅ is deuterium labeled Prothionamide (HY-B0306). Prothionamide is an orally active thioamide antibacterial agent. Prothionamide is a substrate of OCT1 with a K_m value of 805.8 μM. Prothionamide reacts with NAD to form a covalent adduct, with the adduct being a tight-binding inhibitor of Mycobacterium tuberculosis and Mycobacterium leprae InhA. Prothionamide can effectively inhibit the growth of Mycobacterium tuberculosis (MIC = ~0.5 µg/mL) and Mycobacterium leprae. Prothionamide is used in the research of tuberculosis and leprosy^{[1][2][3][4][5]}.

Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs^[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

185.30

C₉H₇D₅N₂S

1330261-26-1

14222-60-7

丙硫异烟胺-d₅； 扑痨硫胺-d₅

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Wang F, et al. Mechanism of thioamide drug action against tuberculosis and leprosy.J Exp Med. 2007 Jan 22;204(1):73-8.  [Content Brief]

  [2]. Fajardo TT, et al. A clinical trial of ethionamide and prothionamide for treatment of lepromatous leprosy. Am J Trop Med Hyg. 2006 Mar;74(3):457-61.  [Content Brief]

  [3]. Parvez MM, et al. Comprehensive Substrate Characterization of 22 Antituberculosis Drugs for Multiple Solute Carrier (SLC) Uptake Transporters In Vitro. Antimicrob Agents Chemother. 2018 Aug 27;62(9):e00512-18.  [Content Brief]

  [4]. Grosset , et al. The role of low dosage prothionamide with and without 4, 4'-diaminio dipheimyl sulphone for use with isoniazld in the treatment of experimental mouse tuberculosis. Tubercle, 1982, 63(1): 37-43.

  [5]. Krasavin M, et al. Conjugation of a 5-nitrofuran-2-oyl moiety to aminoalkylimidazoles produces non-toxic nitrofurans that are efficacious in vitro and in vivo against multidrug-resistant Mycobacterium tuberculosis. Eur J Med Chem. 2018 Sep 5;157:1115-1126.  [Content Brief]