BTZ043 RacemateDprE1 inhibitor CAS# 957217-65-1 |
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Quality Control & MSDS
3D structure
Package In Stock
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| Cas No. | 957217-65-1 | SDF | Download SDF |
| PubChem ID | 49769085 | Appearance | Powder |
| Formula | C17H16F3N3O5S | M.Wt | 431.39 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Solubility | DMSO : ≥ 30 mg/mL (69.54 mM) *"≥" means soluble, but saturation unknown. | ||
| Chemical Name | 2-(3-methyl-1,4-dioxa-8-azaspiro[4.5]decan-8-yl)-8-nitro-6-(trifluoromethyl)-1,3-benzothiazin-4-one | ||
| SMILES | CC1COC2(O1)CCN(CC2)C3=NC(=O)C4=CC(=CC(=C4S3)[N+](=O)[O-])C(F)(F)F | ||
| Standard InChIKey | GTUIRORNXIOHQR-UHFFFAOYSA-N | ||
| Standard InChI | InChI=1S/C17H16F3N3O5S/c1-9-8-27-16(28-9)2-4-22(5-3-16)15-21-14(24)11-6-10(17(18,19)20)7-12(23(25)26)13(11)29-15/h6-7,9H,2-5,8H2,1H3 | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
| Description | BTZ043 racemate is an inhibitor of decaprenylphosphoryl-β-D-ribose 2'-epimerase (DprE1). | |||||
| Targets | DprE1 | |||||
BTZ043 Racemate Dilution Calculator
BTZ043 Racemate Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 2.3181 mL | 11.5904 mL | 23.1809 mL | 46.3618 mL | 57.9522 mL |
| 5 mM | 0.4636 mL | 2.3181 mL | 4.6362 mL | 9.2724 mL | 11.5904 mL |
| 10 mM | 0.2318 mL | 1.159 mL | 2.3181 mL | 4.6362 mL | 5.7952 mL |
| 50 mM | 0.0464 mL | 0.2318 mL | 0.4636 mL | 0.9272 mL | 1.159 mL |
| 100 mM | 0.0232 mL | 0.1159 mL | 0.2318 mL | 0.4636 mL | 0.5795 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
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MIC: 1 ng/ml (2.3 nM) for M. tuberculosis H37Rv and 4 ng/ml (9.2 nM) for Mycobacterium smegmatis
The loss of human lives to tuberculosis (TB) continues unabated as a result of poverty, synergy with the HIV/AIDS pandemic, and the emergence of multidrug- and extensively drug-resistant strains of Mycobacterium tuberculosis. BTZ043 is the most advanced candidate for inclusion in combination therapies for both drug-sensitive and extensively drug-resistant TB.
In vitro: BTZ043 displayed similar activity against all clinical isolates of M. tuberculosis that were tested, including extensively drug-resistant and multidrug-resistant strains, indicating that it targets a previously unknown biological function. BTZ043 is bactericidal, reducing viability in vitro by more than 1000-fold in under 72 hours, which is comparable to the INH killing effect [1].
In vivo: The in vivo efficacy of BTZ043 was assessed 4 weeks after a low-dose aerosol infection of in the chronic BALB/c mice model of TB. Four weeks of treatment with BTZ043 reduced the bacterial load in the lungs and spleens by 1 and 2 logs, respectively, at the concentrations used. Additional findings suggest that BTZ efficacy is time- rather than dose-dependent [1].
Clinical trial: Up to now, BTZ043 is still in the preclinical development stage.
Reference:
[1] Makarov V, Manina G, Mikusova K, et al. Benzothiazinones kill Mycobacterium tuberculosis by blocking arabinan synthesis. Science. 2009 May 8;324(5928):801-4.
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Synthesis and structure-activity relationships evaluation of benzothiazinone derivatives as potential anti-tubercular agents.[Pubmed:23886691]
Bioorg Med Chem Lett. 2013 Sep 1;23(17):4919-22.
N-Alkyl and heterocycle substituted 1,3-benzothiazin-4-one (BTZ) derivatives were synthesized. The anti-mycobacterial activities of these compounds were evaluated by determination of minimal inhibitory concentration (MIC) for Mycobacterium tuberculosis H37Ra and M. tuberculosis H37Rv. It was found that an extended or branched alkyl chain analog could enhance the potency, and activities of N-alkyl substituted BTZs were not affected by either nitro or trifluoromethyl at 6-position. Trifluoromethyl plays an important role in maintaining anti-tubercular activity in the piperazine or piperidine analogs. Compound 8o, which contains an azaspirodithiolane group, showed a MIC of 0.0001 muM against M. tuberculosis H37Rv, 20-fold more potent than BTZ043 Racemate. These results suggested that the volume and lipophilicity of the substituents were important in maintaining activity. In addition, compound 8o was nontoxic to Vero cells and orally bioavailable in a preliminary pharmacokinetics study.
