1. Anti-infection
  2. Antibiotic Bacterial
  3. Capreomycin sulfate

Capreomycin sulfate is a macrocyclic peptide antibiotic that inhibits phenylalanine synthesis in mycobacterial ribosomal translation. Capreomycin sulfate has anti-amyloidogenic and pro-fibrinolytic activities, reducing amyloid-induced cytotoxicity by inhibiting the occurrence of amyloid fibrillation. Capreomycin sulfate can be used in the study of multidrug-resistant tuberculosis, type 2 diabetes, Alzheimer's disease and Parkinson's disease.

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Capreomycin sulfate

Capreomycin sulfate Chemische Struktur

CAS. Nr. : 1405-37-4

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Based on 5 publication(s) in Google Scholar

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Beschreibung

Capreomycin sulfate is a macrocyclic peptide antibiotic that inhibits phenylalanine synthesis in mycobacterial ribosomal translation. Capreomycin sulfate has anti-amyloidogenic and pro-fibrinolytic activities, reducing amyloid-induced cytotoxicity by inhibiting the occurrence of amyloid fibrillation. Capreomycin sulfate can be used in the study of multidrug-resistant tuberculosis, type 2 diabetes, Alzheimer's disease and Parkinson's disease[1][2][3][4][5].

IC50 & Target

Aminoglycoside

 

In Vitro

Capreomycin sulfate (10-200 μM; 80 h) inhibits the formation of insulin fibrils in human erythrocytes in a concentration-dependent manner (IC50=69.98 μM) and has a delayed fibrillation process[3].
Capreomycin sulfate (75-100 μM; 60 min) shows a dose-dependent protective effect against amyloid fibril-induced erythrocyte damage and hemolysis[3].
Capreomycin sulfate (100 μM; 0-48 h) effectively destroys fibrils in erythrocytes in a time-dependent manner[3].

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

Cell Viability Assay[3]

Cell Line: human erythrocyte
Concentration: 75 and 100 µM
Incubation Time: 30 min
Result: The hemolysis rates were 23.8% and 13.0% at 75µM and 100µM, respectively.
In Vivo

Capreomycin sulfate (1.4-14.5 mg/kg for insufflation; 20 mg/kg for i.m., 4 weeks) decreases the wet lung weight and lowers bacterial burden in the lungs of infected guinea pigs[2].

Pharmacokinetic Analysis in the guinea pig model[2]

Route Dose (mg/kg) AUC0-t (ng h/mL) CL_F (mL/h kg) K (h-1) t1/2 (h) MRT (h) Cmax (ng/mL) Tmax (h) MAT (h) F0-t
i.v. 20 49.29 0.42 0.92 0.75 0.88 53.36 0.08 / 1.00
i.m. 20 58.2 0.35 0.68 1.09 1.44 32.33 0.36 0.44 1.20
Insufflation 14.5 16.95 0.54 0.48 1.53 1.80 6.70 0.31 0.80 0.54
Insufflation 7.2 8.2 0.52 0.45 1.68 1.72 3.34 0.38 0.72 0.59
Insufflation 1.4 1.15 0.67 0.71 1.22 1.01 0.92 0.5 / 0.41

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

Animal Model: Male guinea pigs [836 ± 162.3 g; infected via the respiratory route with nebulized suspensions 2 × 105 CFU/mL of Mycobacterium tuberculosis (strain H37Rv)] [2]
Dosage: 1.4, 7.2, and 14.5 mg/kg for Insufflation; 20 mg/kg for Intramuscular injection
Administration: Insufflation or Intramuscular injection; 4 weeks
Result: Decreased the wet lung weight at 14.5 mg/kg, and smaller than receiving 1.4 mg/kg group and controls.
Lowered bacterial burden in the lungs (3.52 CFU/mL) at 14.5 mg/kg than controls (4.58 CFU/mL) and at 1.4 and 7.2 mg/kg (4.02 and 4.01 CFU/mL, respectively)
CAS. Nr.
Appearance

Solid

Color

White to off-white

SMILES

OS(O)(=O)=O.[R]C[C@H](N1)C(N[C@@H](CNC(CC(N)CCCN)=O)C(N/C(C(N[C@H](C(NC[C@H](N)C1=O)=O)[C@@H]2NC(NCC2)=N)=O)=C\NC(N)=O)=O)=O.OS(O)(=O)=O.[R=OH 1A].[R=H 1B]

Structure Classification
Initial Source

Streptomyces capreolus

Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

-20°C, sealed storage, away from moisture

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

Lösungsmittel & Löslichkeit
In Vitro: 

H2O : 100 mg/mL (Need ultrasonic)

  • Molaritätsrechner

  • Verdünnungsrechner

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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:  PBS

    Solubility: 100 mg/mL; Clear solution; Need ultrasonic

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

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Dosing volume
(per animal)

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Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
Reinheit & Dokumentation

Purity: 99.52%

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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.

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Produktname:
Capreomycin sulfate
Art. -Nr.:
HY-17566
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