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DprE1-IN-2 is an effective DprE1 inhibitor.

DprE1-IN-377790 is a novel DprE1 inhibitor, killing M. tuberculosis.

DprE1-IN-11 (compound 3) is an orally active DprE1 inhibitor that exhibits antitubercular activity against both MTB H37Rv and MDR-MTB strains (MIC <0.029-0.095 μM).

DprE1-IN-13 (Compound 42) is an inhibitor of decaprenyl-phosphoryl-β-d-ribose oxidase (DprE1) with an IC50 value of 12.72 μM. It effectively inhibits Mycobacterium tuberculosis H37Ra, with a MIC50 of 1.071 μM.

DprE1-IN-14 (Compound 77) is a DprE1 inhibitor with an IC₅₀ of 2.5 nM against M. tuberculosis. It demonstrates antitubercular activity with an MIC₉₀ of 0.3 μM against the M. tuberculosis mc²⁶²³⁰ strain. Primarily exhibiting bacteriostatic activity, DprE1-IN-14 shows time-dependent bactericidal effects at concentrations 10 times the MIC. This compound is applicable in antituberculosis research.

DprE1-IN-4 is a potent, non-covalent inhibitor of DprE1 (IC50: 0.90 μg/mL). DprE1-IN-4 has acceptable pharmacokinetic properties and has a significant bactericidal effect in a mouse model of acute tuberculosis.

DprE1-IN-1 is a potent, orally active DprE1 inhibitor that demonstrates good hepatocyte stability, low cytotoxicity, and low hERG channel inhibition. It also exhibits effective anti-branched bacilli activity in macrophages, reducing the bacterial load by 1.29 log10 CFU.

DprE1-IN-9 (compound B18) is an efficient, reversible inhibitor of DprE1, interacting with the enzyme's receptor cavity. It exhibits potent antimycobacterial properties, demonstrating activity against non-pathogenic H37Ra (MIC=0.18 µg/mL) and pathogenic strains, including H37Rv, as well as clinical MDR and XDR isolates [1].

DprE1-IN-5 (Compound 10), a potent DprE1 inhibitor, exhibits anti-TB activity with an MIC of 4 μM against the Mtb H37Rv strain and demonstrates antimycobacterial efficacy against drug-resistant strains. Additionally, it possesses high microsomal stability [1].

DprE1-IN-6 (Compound 56) is a DprE1 inhibitor with anti-TB activity, showing a minimum inhibitory concentration (MIC) of 1 μM against the Mtb H37Rv strain and efficacy against drug-resistant mycobacterial strains. Additionally, it has high microsomal stability and medium clearance [1].

DprE1-IN-7 (Compound 64) is a DprE1 inhibitor with potent anti-tuberculosis (TB) activity, demonstrating a minimum inhibitory concentration (MIC) of 1 μM against the Mtb H37Rv strain. It exhibits antimycobacterial effects on drug-resistant strains, shows high microsomal stability, and has medium clearance [1].

DprE1-IN-10 (hit 2), an inhibitor of Decaprenylphosphoryl-β-D-ribose-2′-epimerase (DprE1), holds potential for the study of tuberculosis.

TBA-7371 (DprE1-IN-1) is a potent inhibitor of DprE1 and PDE6.

AGN 210676 is a selective agonist of prostaglandin EP2(EC50 : 5 nM).

Laropiprant (MK-0524) is a potent and selective antagonist of prostaglandin D2 (PGD2) receptor (DP) such as and DP/DP1 receptor(Ki = 0.57 nM) and TP Receptor(Ki = 2.95 nM).

Guanabenz hydrochloride (NE56490) is an orally active α2-adrenoceptor agonist with hypotensive effects.

Droxidopa (L-DOPS) is an effective orally active norepinephrine precursor capable of crossing the blood-brain barrier. It can increase standing blood pressure, improve symptoms of orthostatic hypotension, and enhance standing ability. Droxidopa is commonly used in studies of neurogenic orthostatic hypotension (nOH) and alternative treatments for attention-deficit/hyperactivity disorder (ADHD).

L-644,698 is a selective agonist of human prostanoid DP receptor.

BTZ043 is a DprE1 inhibitor with nanomolar bactericidal activity against Mycobacterium tuberculosis in vitro.

Macozinone (PBTZ169) inhibits decaprenylphosphoryl-β-d-ribose 2′-oxidase (DprE1), more efficiently than BTZ043.

Osilodrostat (LCI699) is a potent inhibitor of human 11β-hydroxylase (CYP11B1) and aldosterone synthase (CYP11B2) with IC50 values ​​of 2.5 and 0.7 nM, respectively, and has been approved by the FDA for the treatment of Cushing's disease.

TCA1 (TCA 1) is a small molecule with activity against drug-resistant and persistent tuberculosis.

GUANABENZ is a Central alpha-2 Adrenergic Agonist. The mechanism of action of guanabenz is as an Adrenergic alpha2-Agonist.

BTZ043 Racemate (Benzothiazinone 10526038) is a decaprenylphosphoryl-β-D-ribose 2'-epimerase (DprE1) inhibitor, used as a new antimycobacterial agent.