BM635 |
Katalog-Nr.GC32204
One-Click Copy Product Info
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BM635 ist ein MmpL3-Inhibitor mit herausragender antimykobakterieller AktivitÄt.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1493762-74-5
Sample solution is provided at 25 µL, 10mM.
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BM635 is a MmpL3 inhibitor with outstanding anti-mycobacterial activity. BM635 has an MIC50 of 0.12 μM against M. tuberculosis H37Rv.
BM635 has potent MIC (0.12 µM), Tox50:MIC ratio of >100, and good microsomal stability in mice (1.4 mL/min/g). When tested in an acute murine infection model at multiple doses, BM635 exhibits potent anti-tubercular activity, with an ED99 of 49 mg/Kg (IC95%: 43-54 mg/Kg)[1]. The half-life in vivo of BM635 is 1h, allowing a reasonable maximum concentration (Cmax=1.62 μM) and a moderate bioavailability (46%). Its poor aqueous solubility together with its high lipophilicity leads to low exposure in vivo[2].
[1]. Poce G, et al. Improved BM212 MmpL3 inhibitor analogue shows efficacy in acute murine model of tuberculosis infection. PLoS One. 2013;8(2):e56980. [2]. Poce G, et al. Pharmaceutical salt of BM635 with improved bioavailability. Eur J Pharm Sci. 2017 Mar 1;99:17-23.
Cell experiment: | The measurement of the minimum inhibitory concentration (MIC) for each tested compounds (including BM635) are performed in 96 wells flat-bottom, polystyrene microtiter plates. Ten two-fold drug dilutions in neat DMSO starting at 200 µM are performed. Five µL of these drug solutions are added to 95 µL of Middlebrook 7H9 medium. Isoniazid is used as a positive control, 8 two-fold dilutions of Isoniazid starting at 160 µg/mL are prepared and 5 µL of this control curve is added to 95 µL of Middlebrook 7H9 medium. Five µL of neat DMSO are added 95 µL of Middlebrook 7H9 medium in row 12 (growth and Blank controls). The inoculum is standardized to approximately 1×107 cfu/mL and diluted 1 in 100 in Middlebrook 7H9 broth to produce the final inoculum of H37Rv strain. One hundred µL of this inoculum is added to the entire plate but G-12 and H-12 wells (Blank controls). All plates are placed in a sealed box to prevent drying out of the peripheral wells and they are incubated at 37°C without shaking for six days. A resazurin solution is prepared by dissolving one tablet of resazurin in 30 mL sterile PBS (phosphate buffered saline). Of this solution, 25 µL are added to each well. Fluorescence is measured after 48 hours to determine the MIC value[1]. |
Animal experiment: | Mouse: Nine (one per dose) 8-10 week old B6 female mice are infected by intratracheal route with 105CFU H37Rv per mouse suspended in 50 µL phosphate buffer saline. BM635 is administered once a day at nine doses ranging from 40 to 300 mg/kg from day 1 to day 8 after infection, and 24 hours after the last dose the mice are sacrificed. To measure the infection burden in lungs, all lobes are aseptically removed and homogenized. The homogenates are supplemented with 5% glycerol and stored frozen (−80°C) until plating. Plates (10%OADC-7H11 medium) are incubated for 14 days at 37°C[1]. |
References: [1]. Poce G, et al. Improved BM212 MmpL3 inhibitor analogue shows efficacy in acute murine model of tuberculosis infection. PLoS One. 2013;8(2):e56980. | |
| Cas No. | 1493762-74-5 | SDF | |
| Canonical SMILES | CC(C1=CC=C(C2=CC(CN3CCOCC3)=C(C)N2C4=CC=C(F)C=C4)C=C1)C | ||
| Formula | C25H29FN2O | M.Wt | 392.51 |
| Löslichkeit | DMSO : 31 mg/mL (78.98 mM) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.5477 mL | 12.7385 mL | 25.4771 mL |
| 5 mM | 509.5 μL | 2.5477 mL | 5.0954 mL |
| 10 mM | 254.8 μL | 1.2739 mL | 2.5477 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
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 saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 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.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.50% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 7 reference(s) in Google Scholar.)