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Delamanid

Catalog No. T4202 CAS 681492-22-8

Synonyms: OPC-67683

Delamanid (OPC-67683) is an anti-tuberculosis agent derived from the nitro-dihydro-imidazooxazole class of compounds that inhibits mycolic acid synthesis of bacterial cell wall.

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Delamanid, CAS 681492-22-8

Pack Size	Availability	Price/USD
5 mg	In stock	$ 39.00
10 mg	In stock	$ 64.00
25 mg	In stock	$ 126.00
50 mg	In stock	$ 225.00
100 mg	In stock	$ 365.00
500 mg	In stock	$ 855.00
1 mL * 10 mM (in DMSO)	In stock	$ 46.00

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Purity: 100%

Purity: 99.87%

Purity: 99.36%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	Delamanid (OPC-67683) is an anti-tuberculosis agent derived from the nitro-dihydro-imidazooxazole class of compounds that inhibits mycolic acid synthesis of bacterial cell wall.
In vitro	In vitro: inhibits the synthesisi of mucolic acids, cruciala component of the cell wall of the Mycobacterium tuberculosis complex.[1] In in-vitro studies, delamanid shows more potent antibacterial activity against drug-susceptible and drug-resistant strains of M. tuberculosis.[2] Delamanid do not affect rifampin, pyrazinamide, and isoniazid exposure; the ethambutol AUCτ and Cmax values are about 25% higher with delamanid coadministration.
In vivo	In vivo: Twice-daily oral dosing of delamanid at 30 mg kg-1 for 5 days resulted in sterile cures in a mouse model of VL. [4]
Kinase Assay	In a 200 μL reaction volume, 1 μM TEM-1 is incubated with and without 5 μM Avibactam for 5 min at 37°C and subjected to two ultrafiltration cartridge (UFC) steps to remove excess inhibitor (Ultrafree-0.5 with Biomax membrane, 5-kDa cutoff). Centrifugation at 10,600× g for 8 min is performed at 4°C. After each ultrafiltration step, 20 μL retentate is diluted with 180 μL assay buffer to restore the original enzyme concentration. After two UFC treatments, the amount of free Avibactam is quantified by LC/MS/MS and found to be <5% of the original concentration. Loss of protein during UFC is assessed by measuring TEM-1 activity (on 4,000-fold dilution) in the acyl-enzyme sample compare with a non-UFC-treated enzyme, and loss is found to be <5%[1].

Synonyms	OPC-67683
Molecular Weight	534.48
Formula	C25H25F3N4O6
CAS No.	681492-22-8

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 50 mg/mL (93.55 mM)

References and Literature

1. Sotgiu G et al. Delamanid (OPC-67683) for treatment of multi-drug-resistant tuberculosis. Expert Rev Anti Infect Ther. 2015 Mar;13(3):305-15. 2. Xavier AS et al. Delamanid: A new armor in combating drug-resistant tuberculosis. J Pharmacol Pharmacother. 2014 Jul;5(3):222-4 3. Mallikaarjun S et al. Delamanid Coadministered with Antiretroviral Drugs or Antituberculosis Drugs Shows No Clinically Relevant Drug-Drug Interactions in Healthy Subjects. Antimicrob Agents Chemother. 2016 Sep 23;60(10):5976-85. 4. Patterson S et al.The anti-tubercular drug delamanid as a potential oral treatment for visceral leishmaniasis. Elife. 2016 May 24;5.

Citations

1. Zhang R, Luo S, Wang N, et al.Epidemiology of Nontuberculous Mycobacteria in Nanjing and MAB_0540 Mutations Associated with Clofazimine Resistance in Mycobacterium abscessus.Infection and Drug Resistance.2023: 2751-2764. 2. Santamaría-Aguirre J, Jacho D, Méndez M A, et al.Solid Lipid Nanoparticles Enhancing the Leishmanicidal Activity of Delamanid.Pharmaceutics.2023, 16(1): 41.

Related compound libraries

This product is contained In the following compound libraries：

Drug Repurposing Compound Library EMA Approved Drug Library Inhibitor Library Clinical Compound Library Fluorochemical Library Immunology/Inflammation Compound Library Orally Active Compound Library FDA-Approved & Pharmacopeia Drug Library Anti-Infection Compound Library ReFRAME Related Library

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Keywords

Delamanid 681492-22-8 Microbiology/Virology Anti-infection Antibacterial Antibiotic Bacterial inhibit Inhibitor OPC67683 OPC-67683 OPC 67683 inhibitor

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