Cat. No.: HY-14881A

Bedaquiline fumarate

(Synonyms: R403323; TMC207 fumarate; R207910 fumarate)

56 Cited Publications

Customer Review

Based on 56 publication(s) in Google Scholar

Bedaquiline fumarate, a diarylquinoline antibiotic that targets ATP synthase, is effective for the treatment of Mycobacterium tuberculosis infections.

For research use only. We do not sell to patients.

Purity: 99.99%
CAS No.: 845533-86-0
Formula: C₃₆H₃₅BrN₂O₆
Molecular Weight:671.58

Storage:

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Bedaquiline fumarate Chemical Structure

CAS No.: 845533-86-0

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Biological Activity
- Description
- In Vitro
Chemical Information
Publications (56)
Solvent & Solubility
- In Vitro
- In Vivo
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

Bedaquiline fumarate, a diarylquinoline antibiotic that targets ATP synthase, is effective for the treatment of Mycobacterium tuberculosis infections.

All Antibiotic Isoforms :

In Vitro

Bedaquiline inhibits the growth of TDR M. tuberculosis strains, with MIC values ranging from 0.125 to 0.5 mg/L^[1]. Among slowly growing mycobacteria (SGM), bedaquiline exhibits the highest activity against Mycobacterium avium with MIC₅₀ and MIC₉₀ values of 0.03 and 16 mg/L, respectively. Among rapidly growing mycobacteria (RGM), Mycobacterium abscessus subsp. abscessus (M. abscessus) and Mycobacterium abscessus subsp. massiliense (M. massiliense) seem more susceptible to bedaquiline than Mycobacterium fortuitum, with MIC₅₀ and MIC₉₀ values of 0.13 and >16 mg/L, respectively, for both species. Bedaquiline also shows moderate in vitro activity against NTM species^[2]. Bedaquiline has an excellent in vitro activity against Mycobacterium tuberculosis, including multidrug resistant M tuberculosis^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Chemical Information

CAS No. 845533-86-0
Appearance Solid
Molecular Weight 671.58
Formula C₃₆H₃₅BrN₂O₆
Color White to off-white
SMILES

OC(/C=C/C(O)=O)=O.BrC1=CC=C(N=C(OC)C([C@H]([C@@](C2=CC=CC3=C2C=CC=C3)(O)CCN(C)C)C4=CC=CC=C4)=C5)C5=C1
Synonyms

R403323; TMC207 fumarate; R207910 fumarate
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Publications (56)

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Journal Impact Factor

Cell

Clp-targeting BacPROTACs impair mycobacterial proteostasis and survival. [Abstract]

2023 May 11;186(10):2176-2192.e22. PMID: 37137307
Autophagy

Duloxetine ameliorates cerebral ischemic injury by inhibiting autophagy. [Abstract]

2026 Mar 5. PMID: 41787744
Nat Commun

Phenotypic drug susceptibility testing for Mycobacterium tuberculosis variant bovis BCG in 12 hours. [Abstract]

2025 May 10;16(1):4366. PMID: 40348759

Bedaquiline fumarate purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 May 10;16(1):4366. [Abstract]

Bedaquiline (BDQ) was effective on susceptible M. smegmatis already at 1× MIC (0.05 μg/mL).
Nat Commun

Intracellular localisation of Mycobacterium tuberculosis affects efficacy of the antibiotic pyrazinamide. [Abstract]

2021 Jun 21;12(1):3816. PMID: 34155215

Bedaquiline fumarate purchased from MedChemExpress. Usage Cited in: Nat Commun. 2021 Jun 21;12(1):3816. [Abstract]

Bedaquiline (BDQ) (2.5 μg/mL, 24 h) significantly enhanced Pyrazinamide (PZA)/Pyrazinoic acid (POA) accumulation in intracellular Mtb.
Adv Sci (Weinh)

Single-Mitochondrion ATP Profiling Directs Discovery of Targetable OXPHOS Dependency in Cancers. [Abstract]

2026 Apr;13(21):e13341. PMID: 41684301
mLife

Identification of a phenyl ester covalent inhibitor of caseinolytic protease and analysis of the ClpP1P2 inhibition in mycobacteria. [Abstract]

2025 Apr 15;4(2):155-168. PMID: 40313980
Eur J Med Chem

Design, synthesis and biological evaluation of (Quinazoline 4-yloxy)acetamide and (4-oxoquinazoline-3(4H)-yl)acetamide derivatives as inhibitors of Mycobacterium tuberculosis bd oxidase. [Abstract]

2022 Nov 15:242:114639. PMID: 35973312
Int J Pharm

A quality-by-design strategic approach for the development of bedaquiline-pretomanid nanoparticles as inhalable dry powders for TB treatment. [Abstract]

2024 Mar 25:653:123920. PMID: 38387819
J Clin Microbiol

Luciferase reporter mycobacteriophage (TM4:: GeNL) enables rapid assessment of drug susceptibilities and inducible macrolide resistance in Mycobacterium abscessus complex. [Abstract]

2025 Aug 20:e0084125. PMID: 40833127

Bedaquiline fumarate purchased from MedChemExpress. Usage Cited in: J Clin Microbiol. 2025 Aug 20:e0084125. [Abstract]

M. abscessus bedaquiline MIC90 values from TM4::GeNL DST, Sensititre RAPMYCO2 DST, MAB_2299c gene mutation-sMAB_4384 and MAB_2299c genotypes. Among the isolates tested, 35% (9/26) demonstrated Bedaquiline (BDQ) MICs greater than 0.5 µg/mL.
Commun Biol

The acetyltransferase CysE modulates virulence and drug resistance of Mycobacterium tuberculosis by interfering with oxidative stress responses. [Abstract]

2025 Oct 6;8(1):1425. PMID: 41053365

Bedaquiline fumarate purchased from MedChemExpress. Usage Cited in: Commun Biol. 2025 Oct 6;8(1):1425. [Abstract]

Minimum Inhibitory Concentration (MIC) determination of the ΔcysE in comparison to WT and Complement strains against anti-TB drugs: Bedaquilline (BDQ) (7 days).
Commun Biol

Development of tolerance to bedaquiline by overexpression of trypanosomal acetate: succinate CoA transferase in Mycobacterium smegmatis. [Abstract]

2025 Feb 6;8(1):187. PMID: 39915674
Front Microbiol

In vitro Antibacterial Activity of an FDA-Approved H+-ATPase Inhibitor, Bedaquiline, Against Streptococcus mutans in Acidic Milieus. [Abstract]

2021 Feb 25;12:647611. PMID: 33717046
Front Microbiol

Mycobacterial Cell Wall Synthesis Inhibitors Cause Lethal ATP Burst. [Abstract]

2018 Aug 15:9:1898. PMID: 30158918
Pharmaceuticals (Basel)

Bedaquiline-Loaded Solid Lipid Nanoparticles Drug Delivery in the Management of Non-Small-Cell Lung Cancer (NSCLC). [Abstract]

2023 Sep 15;16(9):1309. PMID: 37765117
Antibiotics (Basel)

Differential Regulation of Oxidative Burst by First Line Drugs Used Against Multi Drug-Resistant Tuberculosis in Naïve Human Innate Immune Cells. [Abstract]

2026 Jun 9;15(6):590. PMID: 42353714
Front Cell Infect Microbiol

Imaging the NADH:NAD+ Homeostasis for Understanding the Metabolic Response of Mycobacterium to Physiologically Relevant Stresses. [Abstract]

2016 Nov 8:6:145. PMID: 27878107
mBio

Bioenergetic Heterogeneity in Mycobacterium tuberculosis Residing in Different Subcellular Niches. [Abstract]

2021 Jun 29;12(3):e0108821. PMID: 34060333
ACS Infect Dis

Toward a Bactericidal Oral Drug Combination for the Treatment of Mycobacterium abscessus Lung Disease. [Abstract]

2025 Apr 1. PMID: 40168319
ACS Infect Dis

Intranasal Administration of Bedaquiline-Loaded Fucosylated Liposomes Provides Anti-Tubercular Activity while Reducing the Potential for Systemic Side Effects. [Abstract]

2024 Sep 13;10(9):3222-3232. PMID: 39136125
ACS Infect Dis

Identification of Chemical Scaffolds Targeting Drug-Resistant and Latent Mycobacterium tuberculosis through High-Throughput Whole-Cell Screening. [Abstract]

2024 Feb 9;10(2):513-526. PMID: 38238154
ACS Infect Dis

Two-Way Regulation of MmpL3 Expression Identifies and Validates Inhibitors of MmpL3 Function in Mycobacterium tuberculosis. [Abstract]

2021 Jan 8;7(1):141-152. PMID: 33319550
Nanomedicine (Lond)

3D spheroid model reveals enhanced efficacy of mannose-decorated nanoparticles for TB treatment. [Abstract]

2025 Apr;20(8):777-789. PMID: 40099656
Antimicrob Agents Chemother

Incorporation of macrophage immune stresses into an intracellular assay of drug tolerance in Mycobacterium tuberculosis. [Abstract]

2025 Sep 11:e0079525. PMID: 40934365

Bedaquiline fumarate purchased from MedChemExpress. Usage Cited in: Antimicrob Agents Chemother. 2025 Sep 11:e0079525. [Abstract]

Bedaquiline (BDQ) showed efficacy against Mtb in activated BMDM^hs. Macrophages were infected with bacteria and treated with BDQ (0.63 and 2.5 μg/mL, 0-12 days).
Antimicrob Agents Chemother

Limited predictive power of known resistance genes for phenotypic drug resistance in clinical Mycobacterium abscessus complex from Beijing in China. [Abstract]

2025 Jul 2;69(7):e0184724. PMID: 40422286
Antimicrob Agents Chemother

An enoyl-ACP reductase inhibitor, NITD-916, expresses anti- Mycobacterium abscessus activity. [Abstract]

2025 Jul 2;69(7):e0024925. PMID: 40407337
Antimicrob Agents Chemother

Multidrug tolerance conferred by loss-of-function mutations in anti-sigma factor RshA of Mycobacterium abscessus. [Abstract]

2024 Dec 5;68(12):e0105124. PMID: 39470195
Antimicrob Agents Chemother

TBAJ-587, a novel diarylquinoline, is active against Mycobacterium abscessus. [Abstract]

2024 Dec 5;68(12):e0094524. PMID: 39470202
Antimicrob Agents Chemother

Activity of Oral Tebipenem-Avibactam in a Mouse Model of Mycobacterium abscessus Lung Infection. [Abstract]

2023 Feb 16;67(2):e0145922. PMID: 36688684
Antimicrob Agents Chemother

Nitric Oxide-Dependent Electron Transport Chain Inhibition by the Cytochrome bc1 Inhibitor and Pretomanid Combination Kills Mycobacterium tuberculosis. [Abstract]

2021 Aug 17;65(9):e0095621. PMID: 34152815
Antimicrob Agents Chemother

Heterologous Expression of ethA and katG in Mycobacterium marinum Enables the Rapid Identification of New Prodrugs Active against Mycobacterium tuberculosis. [Abstract]

2021 Mar 18;65(4):e01445-20. PMID: 33495223
Antimicrob Agents Chemother

TBAJ-876, a 3,5-Dialkoxypyridine Analogue of Bedaquiline, Is Active against Mycobacterium abscessus. [Abstract]

2020 Mar 24;64(4):e02404-19. PMID: 31964791
Antimicrob Agents Chemother

TBAJ-876 Displays Bedaquiline-Like Mycobactericidal Potency without Retaining the Parental Drug's Uncoupler Activity. [Abstract]

2020 Jan 27;64(2):e01540-19. PMID: 31712198
Antimicrob Agents Chemother

TBAJ-876 Retains Bedaquiline's Activity against Subunits c and ε of Mycobacterium tuberculosis F-ATP Synthase. [Abstract]

2019 Sep 23;63(10):e01191-19. PMID: 31358589
Microbiol Spectr

Evaluation of the post-antibiotic effect against Mycobacterium abscessus by a bioluminescence method. [Abstract]

2026 Apr 7;14(5):e0380525. PMID: 41944630
J Biol Chem

High efficacy of the F-ATP synthase inhibitor TBAJ-5307 against non-tuberculous mycobacteria in vitro and in vivo. [Abstract]

2024 Feb;300(2):105618. PMID: 38176652
Microbiol Spectr

GaMF1.39's antibiotic efficacy and its enhanced antitubercular activity in combination with clofazimine, Telacebec, ND-011992, or TBAJ-876. [Abstract]

2023 Dec 12;11(6):e0228223. PMID: 37982630
Microbiol Spectr

In Vitro Synergy Testing of Eravacycline in Combination with Clarithromycin and Rifabutin against Mycobacterium abscessus Complex. [Abstract]

2021 Sep 3;9(1):e0004521. PMID: 34132613
Vet Res

Mitochondrial dysfunction induced by bedaquiline as an anti-Toxoplasma alternative. [Abstract]

2023 Dec 19;54(1):123. PMID: 38115043
ACS Chem Biol

Investigate Natural Product Indolmycin and the Synthetically Improved Analogue Toward Antimycobacterial Agents. [Abstract]

2022 Jan 21;17(1):39-53. PMID: 34908399
Dis Model Mech

An anti-tuberculosis compound screen using a zebrafish infection model identifies an aspartyl-tRNA synthetase inhibitor. [Abstract]

2021 Dec 1;14(12):dmm049145. PMID: 34643222
Infect Immun

Mouse models of tuberculosis uniformly featuring hypoxic necrotic lesions and poor response to chemotherapy. [Abstract]

2026 Feb 9:e0057425. PMID: 41660838
J Pharm Biomed Anal

Characterization of stress degradation products of bedaquiline fumarate and bedaquiline by LC-PDA and LC-MS. [Abstract]

2023 Oct 25:235:115658. PMID: 37619292
SLAS Discov

A Novel Flow Cytometric Assay to Identify Inhibitors of RBPJ-DNA Interactions. [Abstract]

2020 Sep;25(8):895-905. PMID: 32567455
bioRxiv

Expanding the scope of Mycobacterium abscessus reference strains to improve pulmonary disease modeling. [Abstract]

2025 Nov 19:2025.11.19.689313. PMID: 41332525
bioRxiv

Mouse Models Uniformly Featuring Human-like Lesions Harboring Drug-tolerant Mycobacterium tuberculosis. [Abstract]

2025 Oct 17:2025.10.17.683099. PMID: 41279700
Authorea

2025 Sep 17.
bioRxiv

2025 July 04.
bioRxiv

2025 February 06.
bioRxiv

Netupitant Exhibits Potent Activity on Mycobacterium tuberculosis Persisters. [Abstract]

2024 Oct 30:2024.10.30.620736. PMID: 39554043
Research Square Preprint

2023 May 2.
Zoonoses

2023 Feb 2.
Università Vita-Salute San Raffaele

2022 Apr 08. 34.
Research Square Preprint

2022 Feb.
University of Manitoba

2022 Jan.
Research Square Preprint

2021 Nov.
University of Madras

2019, Jan.

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (148.90 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.4890 mL

7.4451 mL

14.8903 mL

5 mM

0.2978 mL

1.4890 mL

2.9781 mL

10 mM

0.1489 mL

0.7445 mL

1.4890 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.75 mg/mL (4.09 mM); Clear solution

This protocol yields a clear solution of ≥ 2.75 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (27.5 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: 2.75 mg/mL (4.09 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.75 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (27.5 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.75 mg/mL (4.09 mM); Clear solution

This protocol yields a clear solution of ≥ 2.75 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (27.5 mg/mL) to 900 μL Corn oil, and mix evenly.

Protocol 4

Add each solvent one by one: 5% DMSO 40% PEG300 5% Tween-80 50% Saline

Solubility: ≥ 2.75 mg/mL (4.09 mM); Clear solution

Protocol 5

Add each solvent one by one: 5% DMSO 95% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.75 mg/mL (4.09 mM); Clear solution

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (273 KB)
SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Jang JC, et al. Bedaquiline susceptibility test for totally drug-resistant tuberculosis Mycobacterium tuberculosis. J Microbiol. 2017 Apr 20. [Content Brief]

[2]. Chahine EB, et al. Bedaquiline: a novel diarylquinoline for multidrug-resistant tuberculosis. Ann Pharmacother. 2014 Jan;48(1):107-15. [Content Brief]

[3]. Pang Y, et al. In Vitro Activity of Bedaquiline against Nontuberculous Mycobacteria in China. Antimicrob Agents Chemother. 2017 Apr 24;61(5). [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.4890 mL	7.4451 mL	14.8903 mL	37.2256 mL
	5 mM	0.2978 mL	1.4890 mL	2.9781 mL	7.4451 mL
	10 mM	0.1489 mL	0.7445 mL	1.4890 mL	3.7226 mL
	15 mM	0.0993 mL	0.4963 mL	0.9927 mL	2.4817 mL
	20 mM	0.0745 mL	0.3723 mL	0.7445 mL	1.8613 mL
	25 mM	0.0596 mL	0.2978 mL	0.5956 mL	1.4890 mL
	30 mM	0.0496 mL	0.2482 mL	0.4963 mL	1.2409 mL
	40 mM	0.0372 mL	0.1861 mL	0.3723 mL	0.9306 mL
	50 mM	0.0298 mL	0.1489 mL	0.2978 mL	0.7445 mL
	60 mM	0.0248 mL	0.1241 mL	0.2482 mL	0.6204 mL
	80 mM	0.0186 mL	0.0931 mL	0.1861 mL	0.4653 mL
	100 mM	0.0149 mL	0.0745 mL	0.1489 mL	0.3723 mL

Keywords

Bedaquiline fumarate

56 Cited Publications

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Bedaquiline fumarate

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Publications Citing Use of MedChemExpress (MCE) Bedaquiline fumarate

All Antibiotic Isoforms

Biological Activity

Chemical Information

Publications (56)

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Bedaquiline fumarate

Bioactive Compound Library Max

Bioactive Compound Library

Anti-Infection Compound Library

FDA-Approved Drug Library

Drug Repurposing Compound Library

Antibacterial Compound Library

NMPA-Approved Drug Library

Orally Active Compound Library

FDA Approved & Pharmacopeial Drug Library

Antibiotics Library

Drug-Induced Liver Injury (DILI) Compound Library

Rare Diseases Drug Library

EMA-Approved Drug Library

Heterocyclic Compound Library

Off-patent Drug Library

Anti-tuberculosis Compound Library

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

FDA-Approved Drug Library Plus

FDA-Approved Drug Library Mini

High-Throughput Bioactive Compound Library

Cardiotoxic Compound Library

Publications Citing Use of MedChemExpress (MCE) Bedaquiline fumarate

All Antibiotic Isoforms

Biological Activity

Chemical Information

Publications (56)

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Bedaquiline fumarate Related Classifications

HY-14881A Related Classifications