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Delamanid (Synonyms: OPC-67683)

Catalog No.GC19122 Copy One-Click Copy Product Info

Delamanid, a newer mycobacterial cell wall synthesis inhibitor, inhibits the synthesisi of mucolic acids, cruciala component of the cell wall of the Mycobacterium tuberculosis complex.

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Delamanid Chemical Structure

Cas No.: 681492-22-8

Size Price Stock Qty
10mM (in 1mL DMSO)
$33.00
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1mg
$12.00
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2mg
$16.00
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5mg
$28.00
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10mg
$46.00
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25mg
$81.00
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50mg
$119.00
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100mg
$179.00
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Sample solution is provided at 25 µL, 10mM.



Description of Delamanid

Delamanid, a newer mycobacterial cell wall synthesis inhibitor, inhibits the synthesisi of mucolic acids, cruciala component of the cell wall of the Mycobacterium tuberculosis complex.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. [3] 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]

References:
[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.

Chemical Properties of Delamanid

Cas No. 681492-22-8 SDF
Synonyms OPC-67683
Canonical SMILES FC(F)(F)OC1=CC=C(OC2CCN(C3=CC=C(OC[C@@]4(C)CN5C(O4)=NC([N+]([O-])=O)=C5)C=C3)CC2)C=C1
Formula C25H25F3N4O6 M.Wt 534.48
Solubility DMSO : ≥ 50 mg/mL (93.55 mM);Water : < 0.1 mg/mL (insoluble) Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table of Delamanid

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1 mg 5 mg 10 mg
1 mM 1.871 mL 9.3549 mL 18.7098 mL
5 mM 374.2 μL 1.871 mL 3.742 mL
10 mM 187.1 μL 935.5 μL 1.871 mL
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In vivo Formulation Calculator (Clear solution) of Delamanid

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.

Product Documents

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Reviews

Review for Delamanid

Average Rating: 5 ★★★★★ (Based on Reviews and 23 reference(s) in Google Scholar.)

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