Loteprednol etabonate

Alias: Loteprednol Etabonate; Lotemax; Alrex; HGP-1; Loterox; Locort;P 5604; HGP1; Lenoxin, CDDD 5604
Cat No.:V1700 Purity: ≥98%
Loteprednol etabonate (Lotemax; Alrex; HGP-1; Loterox; Locort;P-5604; HGP1; Lenoxin, CDDD-5604), the esther form of Loteprednol, is a potent glucocorticoid receptor agonist approved as a medication used in treatment of inflammation of the eye due to allergies.
Loteprednol etabonate Chemical Structure CAS No.: 82034-46-6
Product category: Calcium Channel
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
10mg
25mg
50mg
100mg
500mg
Other Sizes

Other Forms of Loteprednol etabonate:

  • Loteprednol Etabonate D5
Official Supplier of:
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

Loteprednol etabonate (Lotemax; Alrex; HGP-1; Loterox; Locort; P-5604; HGP1; Lenoxin, CDDD-5604), the esther form of Loteprednol, is a potent glucocorticoid receptor agonist approved as a medication used in treatment of inflammation of the eye due to allergies. Loteprednol possesses a metabolically labile function, the 17beta-ester, that is designed to be rapidly deactivated in the systemic circulation. Loteprednol etabonate exhibits a binding affinity which is 4.3 times that of dexamethasone.

Biological Activity I Assay Protocols (From Reference)
ln Vitro

In vitro activity: Loteprednol possesses a metabolically labile function, the 17beta-ester, that is designed to be rapidly deactivated in the systemic circulation. Loteprednol etabonate exhibits a binding affinity which is 4.3 times that of dexamethasone, both compounds having a Hill factor close to 1 whereas PJ90 and PJ91 does not show any affinity to the receptor.


Kinase Assay:


Cell Assay:

ln Vivo
Dogs receiving 5 mg/kg of loteprednol etabonate intravenously show a 2.8 h terminal half-life, 3.7 L/kg volume of distribution, and 0.9 L/h/kg total body clearance. not found in the urine. Dogs received the medication orally (5 mg/kg), and the plasma solely contained metabolites—no intact drug—which suggests a substantial first-pass impact.
Animal Protocol


References
[1]. Noble S, Goa KL. Loteprednol etabonate: clinical potential in the management of ocular inflammation. BioDrugs. 1998 Oct;10(4):329-39.
[2]. Szelenyi I, Hochhaus G, Heer S et al. Loteprednol etabonate: a soft steroid for the treatment of allergic diseases of the airways. Drugs Today (Barc). 2000 May;36(5):313-20.
[3]. Howes JF. Loteprednol etabonate: a review of ophthalmic clinical studies. Pharmazie. 2000 Mar;55(3):178-83.
[4]. Pavesio CE, Decory HH. Treatment of ocular inflammatory conditions with loteprednol etabonate. Br J Ophthalmol. 2008 Apr;92(4):455-9.
[5]. Comstock TL, Decory HH. Advances in corticosteroid therapy for ocular inflammation: loteprednol etabonate. Int J Inflam. 2012;2012:789623.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C24H31CLO7
Molecular Weight
466.95
CAS #
82034-46-6
Related CAS #
Loteprednol Etabonate-d5;2026643-11-6;Loteprednol Etabonate-d3
SMILES
ClC([H])([H])OC([C@]1(C([H])([H])C([H])([H])[C@@]2([H])[C@]3([H])C([H])([H])C([H])([H])C4=C([H])C(C([H])=C([H])[C@]4(C([H])([H])[H])[C@@]3([H])[C@]([H])(C([H])([H])[C@@]21C([H])([H])[H])O[H])=O)OC(=O)OC([H])([H])C([H])([H])[H])=O
Synonyms
Loteprednol Etabonate; Lotemax; Alrex; HGP-1; Loterox; Locort;P 5604; HGP1; Lenoxin, CDDD 5604
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO: 93 mg/mL (199.2 mM)
Water:<1 mg/mL
Ethanol: 4 mg/mL (8.6 mM)
Solubility (In Vivo)
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.35 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.

 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 2.1416 mL 10.7078 mL 21.4156 mL
5 mM 0.4283 mL 2.1416 mL 4.2831 mL
10 mM 0.2142 mL 1.0708 mL 2.1416 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

Calculator

Molarity Calculator allows you to calculate the mass, volume, and/or concentration required for a solution, as detailed below:

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An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?
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Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
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  • The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box
g/mol

Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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Definitions of molecular mass, molecular weight, molar mass and molar weight:
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  • Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
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In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
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Calculation results

Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
             (2) Be sure to add the solvent(s) in order.

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