2. Anti-infection
  3. Bacterial Antibiotic
  4. Oritavancin diphosphate

Oritavancin diphosphate  (Synonyms: LY333328 diphosphate)

Cat. No.: HY-B1831A Purity: 99.93%
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Oritavancin diphosphate (LY333328 diphosphate), a semisynthetic derivative of Vancomycin (HY-B0671), is an orally active glycopeptide antibiotic with bactericidal activity against gram-positive organisms. Oritavancin diphosphate shows antibacterial effect against B. anthracis, such as Ames strain with a MIC value of 0.015 g/mL. Oritavancin diphosphate inhibits cell wall synthesis and disrupts the membrane potential. Oritavancin diphosphate inhibits ArlS kinase activity thereby interfering the signal transduction. Oritavancin diphosphate enters cells by adsorptive endocytosis, which drives it to lysosomes, where it exerts antibiotic activity.

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

Oritavancin diphosphate Chemical Structure

Oritavancin diphosphate Chemical Structure

CAS No. : 192564-14-0

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Based on 1 publication(s) in Google Scholar

Other Forms of Oritavancin diphosphate:

Oritavancin diphosphate Related Antibodies

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1 Publications Citing Use of MCE Oritavancin diphosphate

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Description

Oritavancin diphosphate (LY333328 diphosphate), a semisynthetic derivative of Vancomycin (HY-B0671), is an orally active glycopeptide antibiotic with bactericidal activity against gram-positive organisms. Oritavancin diphosphate shows antibacterial effect against B. anthracis, such as Ames strain with a MIC value of 0.015 g/mL. Oritavancin diphosphate inhibits cell wall synthesis and disrupts the membrane potential. Oritavancin diphosphate inhibits ArlS kinase activity thereby interfering the signal transduction. Oritavancin diphosphate enters cells by adsorptive endocytosis, which drives it to lysosomes, where it exerts antibiotic activity[1][2][3][4][5].

IC50 & Target

Glycopeptide

 

In Vitro

Oritavancin diphosphate (25 μM, 30 min) dose-dependently inhibits the kinase activity of ArlS (3 μg) by 98% with an IC50 value of 5.47 μΜ in vitro[1].
Oritavancin diphosphate (0.7 μM, 42 h) decreases spx expression in the USA300-Pspx strain[1].
Oritavancin diphosphate (3.1 μM, 24 h) disrupts mature MRSA biofilms and facilitates bactericidal activity of oritavancin diphosphate and Oxacillin (HY-B0925A) against embedded S. aureus cells[1].
Oritavancin diphosphate’ (0-80 μg/mL, 2 h) incubation with increasing extracellular concentrations and the uptake by cells proceed in a cooperative manner in J774 macrophages[2].
Oritavancin diphosphate (25 mg/L, 24 h) exerts a marked bactericidal effect against intracellular S. aureus[2].

Oritavancin diphosphate accumulation by different cell types[2]

(The cells were incubated for 2 h at 37°C with 25 mg of the drug per liter in a medium containing 10% FCS)[2]

Cell type Accumulation ratio (no. of determinations)
J774 mouse macrophages 66.4±11.8 (12)
THP-1 human monocytes 84.3±7.0 (9)
Rat embryo fibroblasts 72.4±9.4 (6)
LLC-PK1 pig kidney proximal tubular cells 37.8±6.4 (3)
Caco-2 human colorectal cells. 13.8±0.4 (3)

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

Oritavancin diphosphate Related Antibodies
In Vivo

Oritavancin diphosphate (i.p. for 1 and 3 mg/kg or i.v. for 15 and 50 mg/kg, every 48 h for 14 days or a single dose for 30 days) provides significant protection in the mouse inhalation anthrax model[3].

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

Animal Model: Mouse inhalation anthrax model[3]
Dosage: i.p. for 1 and 3 mg/kg, i.v. for 15 and 50 mg/kg
Administration: i.p., every 48 h for 14 days; i.v., a single dose for 30 days administered 24 h after challenge with inhalation anthrax
Result: Provided significant protection with 1 and 3 mg/kg protecting 50 and 100% of the mice, respectively when administered i.p..
Provided significant protection with 15 and 50 mg/kg protecting 70 or 100% of the mice, respectively when administered i.v..
Clinical Trial
Molecular Weight

1989.09

Formula

C86H103Cl3N10O34P2
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O[C@@H]1[C@@H](O[C@@](O[C@@H](C)[C@@H]2O)([H])C[C@]2(C)NCC3=CC=C(C4=CC=C(Cl)C=C4)C=C3)[C@@H](O[C@H](CO)[C@H]1O)OC5=C(OC6=CC=C([C@H]([C@H]7NC([C@H](NC)CC(C)C)=O)O)C=C6Cl)C=C([C@](NC([C@@H](NC7=O)CC(N)=O)=O)([H])C(N[C@](C8=O)([H])C9=CC%10=C(O)C=C9)=O)C=C5OC%11=CC=C([C@H]([C@](C(N[C@@](C(O)=O)([H])C%12=C%10C(O)=CC(O)=C%12)=O)([H])N8)O[C@@](O[C@@H](C)[C@@H]%13O)([H])C[C@@]%13(N)C)C=C%11Cl.O=P(O)(O)O.O=P(O)(O)O
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)

Solvent & Solubility
In Vitro: 

H2O : 50 mg/mL (25.14 mM; Need ultrasonic)

DMSO : 33.33 mg/mL (16.76 mM; ultrasonic and warming and heat to 60°C; 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 0.5027 mL 2.5137 mL 5.0274 mL
5 mM 0.1005 mL 0.5027 mL 1.0055 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 (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.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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  • Dilution Calculator

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:

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

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: ≥ 2.08 mg/mL (1.05 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

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

    Solubility: ≥ 2.08 mg/mL (1.05 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

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).
Purity & Documentation

Purity: 99.93%

SDS (393 KB)

COA (264 KB) HNMR (404 KB) LCMS (93 KB)

Handling Instructions (2659 KB)
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 (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.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO / H2O 1 mM 0.5027 mL 2.5137 mL 5.0274 mL 12.5686 mL
5 mM 0.1005 mL 0.5027 mL 1.0055 mL 2.5137 mL
10 mM 0.0503 mL 0.2514 mL 0.5027 mL 1.2569 mL
15 mM 0.0335 mL 0.1676 mL 0.3352 mL 0.8379 mL
H2O 20 mM 0.0251 mL 0.1257 mL 0.2514 mL 0.6284 mL
25 mM 0.0201 mL 0.1005 mL 0.2011 mL 0.5027 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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Oritavancin diphosphate 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:

Oritavancin diphosphate192564-14-0LY333328 diphosphateBacterialAntibioticorally activesemisynthetic derivativeantibioticbactericidal activitycell wall synthesismembrane potentialArlSgram-positive organismsInhibitorinhibitorinhibit

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