1. Anti-infection
  2. Bacterial

BM635 

Cat. No.: HY-109587 Purity: 98.55%
Handling Instructions

BM635 is a MmpL3 inhibitor with outstanding anti-mycobacterial activity. BM635 has an MIC50 of 0.12 μM against M. tuberculosis H37Rv.

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

BM635 Chemical Structure

BM635 Chemical Structure

CAS No. : 1493762-74-5

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 285 In-stock
Estimated Time of Arrival: December 31
1 mg USD 110 In-stock
Estimated Time of Arrival: December 31
5 mg USD 330 In-stock
Estimated Time of Arrival: December 31
10 mg USD 550 In-stock
Estimated Time of Arrival: December 31
25 mg USD 1100 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1650 In-stock
Estimated Time of Arrival: December 31
100 mg   Get quote  
200 mg   Get quote  

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Customer Review

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

BM635 is a MmpL3 inhibitor with outstanding anti-mycobacterial activity. BM635 has an MIC50 of 0.12 μM against M. tuberculosis H37Rv.

IC50 & Target

MIC50: 0.12 μM (M. tuberculosis H37Rv)[1]

In Vivo

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].

Solvent & Solubility
In Vitro: 

DMSO : 31 mg/mL (78.98 mM; Need ultrasonic and warming)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.5477 mL 12.7385 mL 25.4771 mL
5 mM 0.5095 mL 2.5477 mL 5.0954 mL
10 mM 0.2548 mL 1.2739 mL 2.5477 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Cell Assay

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].

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

Animal Administration

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].

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

References
Molecular Weight

392.51

Formula

C₂₅H₂₉FN₂O

CAS No.

1493762-74-5

SMILES

CC(C1=CC=C(C2=CC(CN3CCOCC3)=C(C)N2C4=CC=C(F)C=C4)C=C1)C

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
BM635
Cat. No.:
HY-109587
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BM635

Cat. No.: HY-109587