Cat. No.: HY-B1831A

Oritavancin diphosphate

(Synonyms: LY333328 diphosphate)

2 Cited Publications

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Based on 2 publication(s) in Google Scholar

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.

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Pureté: 99.71%
CAS No.: 192564-14-0
Formule: C₈₆H₁₀₃Cl₃N₁₀O₃₄P₂
Masse moléculaire:1989.09

Stockage:

4°C, sealed storage, away from moisture

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

Oritavancin diphosphate Chemical Structure

CAS No.: 192564-14-0

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Activité biologique
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
- Essai clinique
Chemical Information
Publications (2)
Solvant et solubilité
- In Vitro
- In Vivo
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

IC₅₀ & Target

Glycopeptide

Voir tous les produits spécifiques à Isoform Antibiotic :

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.

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..

Essai clinique

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 192564-14-0
Appearance Solid
Masse moléculaire 1989.09
Formule C₈₆H₁₀₃Cl₃N₁₀O₃₄P₂
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
Synonyms

LY333328 diphosphate
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage

4°C, sealed storage, away from moisture

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

Publications (2)

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Journal Impact Factor

Emerg Microbes Infect

The role of ArlRS in regulating oxacillin susceptibility in methicillin-resistant Staphylococcus aureus indicates it is a potential target for antimicrobial resistance breakers. [Abstract]

2019;8(1):503-515. PMID: 30924407
Res Sq

2025 Apr 07.

Solvant et solubilité

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

0.5027 mL

2.5137 mL

5.0274 mL

5 mM

0.1005 mL

0.5027 mL

1.0055 mL

10 mM

0.0503 mL

0.2514 mL

0.5027 mL

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.

Calculateur de molarité

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

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

Stock Solution Working Solution

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.

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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

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

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Working solution concentration: 0.22 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) .

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (288 KB)
SDS (394 KB)
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COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
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MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[1]. Bai J, et al. The role of ArlRS in regulating oxacillin susceptibility in methicillin-resistant Staphylococcus aureus indicates it is a potential target for antimicrobial resistance breakers[J]. Emerg Microbes Infect. 2019;8(1):503-515. [Content Brief]

[2]. Van Bambeke F, et al. Cellular pharmacokinetics and pharmacodynamics of the glycopeptide antibiotic oritavancin (LY333328) in a model of J774 mouse macrophages[J]. Antimicrob Agents Chemother. 2004 Aug;48(8):2853-60. [Content Brief]

[3]. Heine HS, et al. Efficacy of oritavancin in a murine model of Bacillus anthracis spore inhalation anthrax. Antimicrob Agents Chemother. 2008 Sep;52(9):3350-7. [Content Brief]

[4]. Arhin FF, et al. Effect of polysorbate 80 on oritavancin binding to plastic surfaces: implications for susceptibility testing. Antimicrob Agents Chemother. 2008 May;52(5):1597-1603. [Content Brief]

[5]. Coyle EA, et al. Activity of oritavancin (LY333328), an investigational glycopeptide, compared to that of vancomycin against multidrug-resistant Streptococcus pneumoniae in an in vitro pharmacodynamic model. Antimicrob Agents Chemother. 2001 Mar;45(3):706-9. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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
H₂O	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.

Keywords

Oritavancin diphosphate

2 Cited Publications

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Oritavancin diphosphate

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Publications Citing Use of MedChemExpress (MCE) Oritavancin diphosphate

Voir tous les produits spécifiques à Isoform Antibiotic

Activité biologique

Chemical Information

Publications (2)

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

Oritavancin diphosphate

Bioactive Compound Library Max

Bioactive Compound Library

Anti-Infection Compound Library

Immunology/Inflammation Compound Library

FDA-Approved Drug Library

Drug Repurposing Compound Library

Antibacterial Compound Library

Orally Active Compound Library

FDA Approved & Pharmacopeial Drug Library

Antibiotics Library

Drug-Induced Liver Injury (DILI) Compound Library

EMA-Approved Drug Library

Non-steroidal Anti-Inflammatory Compound Library

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High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) Oritavancin diphosphate

Voir tous les produits spécifiques à Isoform Antibiotic

Activité biologique

Chemical Information

Publications (2)

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

Oritavancin diphosphate Related Classifications

HY-B1831A Related Classifications