Home >> Research Area >>Others>>Others>> BTZ043 Racemate

BTZ043 Racemate

DprE1 inhibitor CAS# 957217-65-1

BTZ043 Racemate

Catalog No. BCC2488----Order now to get a substantial discount!

Product Name & Size Price Stock
BTZ043 Racemate: 5mg $127 In Stock
BTZ043 Racemate: 10mg Please Inquire In Stock
BTZ043 Racemate: 20mg Please Inquire Please Inquire
BTZ043 Racemate: 50mg Please Inquire Please Inquire
BTZ043 Racemate: 100mg Please Inquire Please Inquire
BTZ043 Racemate: 200mg Please Inquire Please Inquire
BTZ043 Racemate: 500mg Please Inquire Please Inquire
BTZ043 Racemate: 1000mg Please Inquire Please Inquire
Related Products

Quality Control of BTZ043 Racemate

Number of papers citing our products

Chemical structure

BTZ043 Racemate

3D structure

Chemical Properties of BTZ043 Racemate

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.
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.
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.

Biological Activity of BTZ043 Racemate

DescriptionBTZ043 racemate is an inhibitor of decaprenylphosphoryl-β-D-ribose 2'-epimerase (DprE1).
TargetsDprE1    

BTZ043 Racemate Dilution Calculator

Concentration (start)
x
Volume (start)
=
Concentration (final)
x
Volume (final)
 
 
 
C1
V1
C2
V2

calculate

BTZ043 Racemate Molarity Calculator

Mass
=
Concentration
x
Volume
x
MW*
 
 
 
g/mol

calculate

Preparing Stock Solutions of BTZ043 Racemate

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.

Organizitions Citing Our Products recently

 
 
 

Calcutta University

University of Minnesota

University of Maryland School of Medicine

University of Illinois at Chicago

The Ohio State University

University of Zurich

Harvard University

Colorado State University

Auburn University

Yale University

Worcester Polytechnic Institute

Washington State University

Stanford University

University of Leipzig

Universidade da Beira Interior

The Institute of Cancer Research

Heidelberg University

University of Amsterdam

University of Auckland
TsingHua University
TsingHua University
The University of Michigan
The University of Michigan
Miami University
Miami University
DRURY University
DRURY University
Jilin University
Jilin University
Fudan University
Fudan University
Wuhan University
Wuhan University
Sun Yat-sen University
Sun Yat-sen University
Universite de Paris
Universite de Paris
Deemed University
Deemed University
Auckland University
Auckland University
The University of Tokyo
The University of Tokyo
Korea University
Korea University

Background on BTZ043 Racemate

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.

Featured Products
New Products
 

References on BTZ043 Racemate

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.

Description

BTZ043 Racemate is the racemate of BTZ043. BTZ043 is an inhibitor of decaprenyl-phosphoribose-epimerase (DprE1), and the antimicrobial activity of BTZ043 is more potent than BTZ043 Racemate.

Keywords:

BTZ043 Racemate,957217-65-1,Natural Products,Others, buy BTZ043 Racemate , BTZ043 Racemate supplier , purchase BTZ043 Racemate , BTZ043 Racemate cost , BTZ043 Racemate manufacturer , order BTZ043 Racemate , high purity BTZ043 Racemate

Online Inquiry for:

      Fill out the information below

      • Size:Qty: - +

      * Required Fields

                                      Result: