2. Anti-infection
  3. Bacterial
  4. Mycobactin-IN-1

Mycobactin-IN-1, a pyrazoline analogue, is a mycobactin biosynthesis inhibitor against mycobacteria. Mycobactin-IN-1 binds to salicyl-AMP ligase (MbtA), a key enzyme in the mycobactin biosynthetic pathway. Mycobactin-IN-1 inhibits whole-cell drug efflux pumps in M. smegmatis. Mycobactin-IN-1 eradicates intracellularly surviving mycobacteria. Mycobactin-IN-1 shows an excellent in vivo pharmacokinetic profile. Mycobactin-IN-1 can be used for the research of tuberculosis.

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

Mycobactin-IN-1

Mycobactin-IN-1 Chemical Structure

CAS No. : 65840-95-1

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Mycobactin-IN-1 Related Antibodies

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Description

Mycobactin-IN-1, a pyrazoline analogue, is a mycobactin biosynthesis inhibitor against mycobacteria. Mycobactin-IN-1 binds to salicyl-AMP ligase (MbtA), a key enzyme in the mycobactin biosynthetic pathway. Mycobactin-IN-1 inhibits whole-cell drug efflux pumps in M. smegmatis. Mycobactin-IN-1 eradicates intracellularly surviving mycobacteria. Mycobactin-IN-1 shows an excellent in vivo pharmacokinetic profile. Mycobactin-IN-1 can be used for the research of tuberculosis[1].

In Vitro

Mycobactin-IN-1 (compound 44) ​​(0.125-256 μg/mL; 24 h, 72 h, 5 days, 8 days) strongly inhibits the growth of mycobacteria in both iron-deficient and iron-containing media. The MIC90 range of Mycobactin-IN-1 against Mycobacterium smegmatis, Mycobacterium tuberculosis, Mycobacterium aurum (ATCC 10437), and Mycobacterium bovis BCG is 4-128 μg/mL[1].
Mycobactin-IN-1 (4 μg/mL; 3 h) inhibits siderophore production in M. smegmatis with 54.70% efficacy[1].
Mycobactin-IN-1 (1 μg/mL) inhibits mycobacterial efflux pump activity[1].
Mycobactin-IN-1 (1-128 μg/mL; 48 h) has low cytotoxicity in normal cells[1].
Mycobactin-IN-1 (1-16 μg/mL; 72 h) effectively kills intracellular M. aurum in RAW\r\n264.7 macrophages with >90% inhibition at 16 μg/mL[1].

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

Mycobactin-IN-1 Related Antibodies

Cell Cytotoxicity Assay[1]

Cell Line: RAW 264.7 murine macrophages, THP-1 human monocytes
Concentration: 1-128 μg/mL
Incubation Time: 48 h
Result: Had GIC₉₀ values of 128 μg/mL (RAW 264.7) and 64 μg/mL (THP-1).

Parmacokinetics
Species Dose Route AUClast AUCinf T1/2 Vss CL F Cmax
Rat[1] 1 mg/kg i.v. 190 ng·h/mL 197 ng·h/mL 4.76 h 11.5 L/kg 84.8 mL/min/kg / /
Rat[1] 5 mg/kg p.o. 203 ng·h/mL 215 ng·h/mL 6.06 h / / 21 % 51.6 ng/mL
Molecular Weight

272.73

Formula

C15H13ClN2O
CAS No.
Appearance

Solid

Color

White to light yellow

SMILES

ClC1=CC=C(C2NN=C(C2)C3=C(O)C=CC=C3)C=C1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (366.66 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.6666 mL 18.3331 mL 36.6663 mL
5 mM 0.7333 mL 3.6666 mL 7.3333 mL
View the Complete Stock Solution Preparation Table

* 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Purity & Documentation
References

Complete Stock Solution Preparation Table

* 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.6666 mL 18.3331 mL 36.6663 mL 91.6657 mL
5 mM 0.7333 mL 3.6666 mL 7.3333 mL 18.3331 mL
10 mM 0.3667 mL 1.8333 mL 3.6666 mL 9.1666 mL
15 mM 0.2444 mL 1.2222 mL 2.4444 mL 6.1110 mL
20 mM 0.1833 mL 0.9167 mL 1.8333 mL 4.5833 mL
25 mM 0.1467 mL 0.7333 mL 1.4667 mL 3.6666 mL
30 mM 0.1222 mL 0.6111 mL 1.2222 mL 3.0555 mL
40 mM 0.0917 mL 0.4583 mL 0.9167 mL 2.2916 mL
50 mM 0.0733 mL 0.3667 mL 0.7333 mL 1.8333 mL
60 mM 0.0611 mL 0.3056 mL 0.6111 mL 1.5278 mL
80 mM 0.0458 mL 0.2292 mL 0.4583 mL 1.1458 mL
100 mM 0.0367 mL 0.1833 mL 0.3667 mL 0.9167 mL
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Mycobactin-IN-1 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Mycobactin-IN-165840-95-1BacterialtuberculosisMbtAM. smegmatissiderophore productionmycobactin biosynthesissalicylic acidiron-deficient mediamycobacteriasalicyl-AMP ligaseM. aurumInhibitorinhibitorinhibit

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