For research use only.
Catalog No.S5007 Synonyms: OPC-67683
CAS No. 681492-22-8
Delamanid (OPC-67683) is a new anti-tuberculosis drug with an excellent intracellular bactericidal activity and a high accumulation rate.
Purity & Quality Control
Choose Selective Bacterial Inhibitors
|Description||Delamanid (OPC-67683) is a new anti-tuberculosis drug with an excellent intracellular bactericidal activity and a high accumulation rate.|
Delamanid potently inhibits the synthesis of mycolic acid, a long-chain fatty acid of the M. tuberculosis (mycobacterium tuberculosis) cell wall. Delamanid at concentrations of less than 5 μM shows no inhibitory effects on the efflux ABC transporters P-gp, BCRP, and BSEP or on the hepatic or renal SLC transporters OATPs, OCTs, and OATs. Delamanid is not metabolized by NADPH-dependent reactions, including those catalyzed by CYP enzymes, in human or animal liver microsomes. Also, delamanid has no inhibitory effects on the metabolism of exogenous CYP substrate compounds by eight CYP isoforms (CYP1A2, CYP2A6, CYP2B6, CYP2C8/9, CYP2C19, CYP2D6, CYP2E1, and CYP3A), even at a concentration of 100 μmol/liter, well above the therapeutic concentration.
|In vivo||The water solubility of delamanid is poor and its absorption is increased more than two-fold by coadministration with food. The absolute bioavailability is unknown but estimated to be between 25% and 47%. In vivo, delamanid is more than 99% protein bound, with a high volume of distribution (Vz/F of 2100 L) and a half-life of 30-38 hours. Delamanid is excreted primarily in the stool, with less than 5% excretion in the urine. It is thought to be primarily metabolized by albumin, with secondary contributions from P450 enzymes, primarily CYP3A4. Animal studies indicate that delamanid is excreted in breast milk.|
|In vitro||DMSO||100 mg/mL (187.09 mM)|
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
In vivo Formulation Calculator (Clear solution)
|Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)|
|Dosage||mg/kg||Average weight of animals||g||Dosing volume per animal||ul||Number of animals|
|Step 2: Enter the in vivo formulation ()|
|% DMSO % % Tween 80 % ddH2O|
Working concentration： mg/ml；
Method for preparing DMSO master liquid: ： mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL，)
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 ddH2O，mix and clarify.
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.
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Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
Clinical Trial Information
|NCT Number||Recruitment||interventions||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT01424670||Completed||Drug: Delamanid + OBR|Drug: Placebo + OBR||Multidrug-resistant Tuberculosis||Otsuka Pharmaceutical Development & Commercialization Inc.||September 2 2011||Phase 3|
|NCT02573350||Completed||Drug: Delamanid||Tuberculosis Multidrug-Resistant||Otsuka Pharmaceutical Development & Commercialization Inc.||March 2009||Phase 2|
Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.
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