Olopatadine HCl (ALO4943A; KW4679)

Alias:
Cat No.:V1222 Purity: ≥98%
Olopatadine HCl (Pataday; Patanase; KW-4679; ALO-4943A; ALO4943A; KW4679), the hydrochloride salt of olopatadine, is a 2nd-generation, selective histamine H1 receptor (IC50 of 559 μM for the release of histamine) antagonist and also a mast cell stabilizer used to treat itching associated with allergic conjunctivitis (eye allergies), it may also be used for the treatment of steroid rebound (red skin syndrome).
Olopatadine HCl (ALO4943A; KW4679) Chemical Structure CAS No.: 140462-76-6
Product category: Histamine Receptor
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
250mg
500mg
1g
Other Sizes

Other Forms of Olopatadine HCl (ALO4943A; KW4679):

  • Olopatadine-d3 hydrochloride (Olopatadine d3 hydrochloride (hydrochloride))
  • Olopatadine (ALO4943A; KW4679)
Official Supplier of:
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Top Publications Citing lnvivochem Products
Purity & Quality Control Documentation

Purity: ≥98%

Product Description

Olopatadine HCl (Pataday; Patanase; KW-4679; ALO-4943A; ALO4943A; KW4679), the hydrochloride salt of olopatadine, is a 2nd-generation, selective histamine H1 receptor (IC50 of 559 μM for the release of histamine) antagonist and also a mast cell stabilizer used to treat itching associated with allergic conjunctivitis (eye allergies), it may also be used for the treatment of steroid rebound (red skin syndrome).

Biological Activity I Assay Protocols (From Reference)
Targets
Histamine receptor
ln Vitro

In vitro activity: Olopatadine is one of the second-generation histamine H1 receptor antagonists that are treated for allergic disorders. Olopatadine significantly inhibited the ear swelling and the increased production of IL-4, IL-1beta, IL-6, GM-CSF and NGF in the lesioned ear. Olopatadine was highly and rapidly absorbed in healthy human volunteers. The urinary excretion of olopatadine accounted for not less than 58% and the contribution of metabolism was considerably low in the clearance of olopatadine in humans. Olopatadine is one of the few renal clearance drugs in antiallergic drugs. Olopatadine was shown to be useful for the treatment of allergic rhinitis and chronic urticaria in double-blind clinical trials. AL-4943A inhibits histamine release in a concentration-dependent fashion (IC50 = 559 microM) from human conjunctival mast cell preparations in vitro. Passive anaphylaxis in guinea pig conjunctiva was attenuated by AL-4943A applied 30 min prior to intravenous or topical ocular antigen challenge (ED50 values 0.0067% and 0.0170%, w/v, respectively).

ln Vivo

Animal Protocol


References

[1]. Effect of olopatadine and other histamine H1 receptor antagonists on the skin inflammation induced by repeated topical application of oxazolone in mice. Pharmacology, 2005. 75(1): p. 45-52.

[2]. Pharmacological, pharmacokinetic and clinical properties of olopatadine hydrochloride, a new antiallergic drug. Jpn J Pharmacol, 2002. 88(4): p. 379-97.

[3]. The in vitro and in vivo ocular pharmacology of olopatadine (AL-4943A), an effective anti-allergic/antihistaminic agent. J Ocul Pharmacol Ther, 1996. 12(4): p. 389-400.

These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C21H24CLNO3
Molecular Weight
373.87
Exact Mass
373.14
Elemental Analysis
C, 67.46; H, 6.47; Cl, 9.48; N, 3.75; O, 12.84
CAS #
140462-76-6
Related CAS #
Olopatadine-d3 hydrochloride; 1331635-21-2; (Z)-Olopatadine-d3 hydrochloride; Olopatadine; 113806-05-6
Appearance
Solid powder
SMILES
CN(C)CC/C=C\1/C2=CC=CC=C2COC3=C1C=C(C=C3)CC(=O)O.Cl
InChi Key
HVRLZEKDTUEKQH-NOILCQHBSA-N
InChi Code
InChI=1S/C21H23NO3.ClH/c1-22(2)11-5-8-18-17-7-4-3-6-16(17)14-25-20-10-9-15(12-19(18)20)13-21(23)24;/h3-4,6-10,12H,5,11,13-14H2,1-2H3,(H,23,24);1H/b18-8-;
Chemical Name
2-[(11Z)-11-[3-(dimethylamino)propylidene]-6H-benzo[c][1]benzoxepin-2-yl]acetic acid;hydrochloride
Synonyms

ALO4943A; KW-4679; ALO-4943A; KW4679; Olopatadine HCl; Olopatadine Hydrochloride; Pataday; Patanase; KW 4679; ALO 4943A; ALO4943A

HS Tariff Code
2934.99.9001
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Note: Please store this product in a sealed and protected environment, avoid exposure to moisture.
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: 50~75 mg/mL (133.7~200.6 mM)
Water: ~13 mg/mL (~34.8 mM)
Ethanol: ~8 mg/mL (~21.4 mM)
Solubility (In Vivo)
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.69 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (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 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.

Solubility in Formulation 2: ≥ 2.5 mg/mL (6.69 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (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 20% SBE-β-CD physiological saline solution and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.

View More

Solubility in Formulation 3: ≥ 2.5 mg/mL (6.69 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.


Solubility in Formulation 4: 17.14 mg/mL (45.84 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication.

 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 2.6747 mL 13.3736 mL 26.7473 mL
5 mM 0.5349 mL 2.6747 mL 5.3495 mL
10 mM 0.2675 mL 1.3374 mL 2.6747 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:

  • Calculate the Mass of a compound required to prepare a solution of known volume and concentration
  • Calculate the Volume of solution required to dissolve a compound of known mass to a desired concentration
  • Calculate the Concentration of a solution resulting from a known mass of compound in a specific volume
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?
  • Enter 350.26 in the Molecular Weight (MW) box
  • Enter 10 in the Concentration box and choose the correct unit (mM)
  • Enter 5 in the Volume box and choose the correct unit (mL)
  • Click the “Calculate” button
  • The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

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:
  • Enter 10 into the Concentration (Start) box and choose the correct unit (mM)
  • Enter 25 into the Concentration (End) box and select the correct unit (mM)
  • Enter 25 into the Volume (End) box and choose the correct unit (mL)
  • Click the “Calculate” button
  • 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
Instructions to calculate molar mass (molecular weight) of a chemical compound:
  • To calculate molar mass of a chemical compound, please enter the chemical/molecular formula and click the “Calculate’ button.
Definitions of molecular mass, molecular weight, molar mass and molar weight:
  • Molecular mass (or molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
  • Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
/

Reconstitution Calculator allows you to calculate the volume of solvent required to reconstitute your vial.

  • Enter the mass of the reagent and the desired reconstitution concentration as well as the correct units
  • Click the “Calculate” button
  • The answer appears in the Volume (to add to vial) box
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.)
+
+
+

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.

Clinical Trial Information
NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03186755 Recruiting Drug: Hyaluronic acid 0.05%
& Ectoine 2.0%
Drug: Olopatadine hydrochloride
ophthalmic solution 0.1%
Conjunctivitis, Allergic
Conjunctivitis, Vernal
Michael Marchand, MD June 11, 2017 Phase 4
NCT06126952 Recruiting Drug: Treatment A: Azelastine
hydrochloride 0.15% nasal
spray (Azelair)
Drug: Treatment B: Placebo (Azelastine
0.15% vehicle) nasal spray
Seasonal Allergic Rhinitis MEDA Pharma GmbH & Co. KG October 30, 2023 Phase 2
NCT00775658 Completed Drug: olopatadine
Drug: placebo
Allergic Rhinitis
Allergic Conjunctivitis
Vanderbilt University Medical
Center
January 2008 Not Applicable
NCT01697969 Completed Drug: Olopatadine
hydrochloride ophthalmic
solution, 0.2%
Allergic Conjunctivitis Alcon Research September 2012 Phase 4
NCT00609128 Completed Drug: olopatadine Allergic Conjunctivitis University of Wisconsin,
Madison
September 2000 Not Applicable
Biological Data
  • Olopatadine HCl

    Mean treatment differences in ocular itching after conjunctival allergen challenge.Allergy Rhinol (Providence). 2016 Summer; 7(2): e107–e114.
  • Olopatadine HCl
    Ocular itching examined after conjunctival allergen challenge.Allergy Rhinol (Providence). 2016 Summer; 7(2): e107–e114.
  • Olopatadine HCl
    Effects of olopatadine ophthalmic solution 0.1% and 0.2% on ovalbumin-induced conjunctival vascular hyperpermeability in passively sensitized rats.Asia Pac Allergy. 2012 Apr; 2(2): 115–121
Contact Us Back to top