TBAJ-587


Catalog No. Size PriceQuantity
M29403-C Contact sales@xcessbio.com for quotation $100Unavailable

Description

TBAJ-587, a potent anti-tuberculosis agent, inhibits M.tb strain H37Rv growth with MIC90s of 0.006 and <0.02 µg/mL in MABA and LORA assay, respectively. TBAJ-587 inhibits hERG channel minimally, attenuates inhibition of the cardiac potassium channel protein coded by the hERG, which is important for cardiac repolarization.

Product information

CAS Number: 2252316-16-6

Molecular Weight: 614.50

Formula: C30H33BrFN3O5

Chemical Name: (1S,2S)-1-(6-bromo-2-methoxyquinolin-3-yl)-2-(2,6-dimethoxypyridin-4-yl)-4-(dimethylamino)-1-(2-fluoro-3-methoxyphenyl)butan-2-ol

Smiles: COC1C=C(C=C(N=1)OC)[C@](O)(CCN(C)C)[C@H](C1=CC=CC(OC)=C1F)C1=CC2=CC(Br)=CC=C2N=C1OC

InChiKey: JJEGOJPMKLRSPJ-POURPWNDSA-N

InChi: InChI=1S/C30H33BrFN3O5/c1-35(2)13-12-30(36,19-16-25(38-4)34-26(17-19)39-5)27(21-8-7-9-24(37-3)28(21)32)22-15-18-14-20(31)10-11-23(18)33-29(22)40-6/h7-11,14-17,27,36H,12-13H2,1-6H3/t27-,30-/m1/s1

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO : 43.33 mg/mL (70.51 mM; Need ultrasonic).

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

Bedaquiline is a drug of the diarylquinoline class that has proven to be clinically effective against drug-resistant tuberculosis, but has a cardiac liability due to its potent inhibition of the cardiac potassium channel protein hERG. TBAJ-587, an analogue of Bedaquiline, demonstrates more potent anti-tubercular activity, with greatly attenuated hERG blockade. TBAJ-587 inhibits hERG channel with an IC50 of 13 μM.

Products are for research use only. Not for human use.

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