2. GPCR/G Protein Neuronal Signaling Immunology/Inflammation
  3. Histamine Receptor CXCR
  4. Olopatadine hydrochloride

Olopatadine hydrochloride  (Synonyms: ALO4943A; KW4679)

Cat. No.: HY-B0426A Purity: 99.83%
COA
SDS
Handling Instructions Technical Support

Olopatadine hydrochloride (ALO4943A; KW4679) is an orally active histamine H1 receptor antagonist and mast cell stabilizer. Olopatadine hydrochloride exerts antiallergic effects by blocking histamine H1 receptor-mediated activities. Olopatadine hydrochloride inhibits exocytosis, chemokine release, F-actin polymerization, CXCL10-induced calcium influx, and T cell chemotactic activity. Olopatadine hydrochloride also reduces the expression levels of CXCR3 on the surface of CD4+ and CD8+ T cells. Olopatadine hydrochloride inhibits scratching behavior, improves dermatitis scores, and suppresses intraepidermal neurite outgrowth. Olopatadine hydrochloride simultaneously decreases the levels of inflammatory markers, growth factors, histamine, and specific IgE, while increasing the expression of ErbB3A/HER3A. Olopatadine hydrochloride can be used in research related to seasonal pollinosis, chronic rhinitis, urticaria, allergic conjunctivitis, alopecia areata, and atopic dermatitis.

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

Olopatadine hydrochloride

Olopatadine hydrochloride Chemical Structure

CAS No. : 140462-76-6

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 In-stock
Solution
10 mM * 1 mL in DMSO In-stock
Solid
5 mg In-stock
10 mg In-stock
25 mg In-stock
50 mg In-stock
100 mg In-stock
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of Olopatadine hydrochloride:

Olopatadine hydrochloride Related Antibodies

Top Publications Citing Use of Products

View All Histamine Receptor Isoform Specific Products:

View All Isoforms
H1 Receptor H2 Receptor H3 Receptor H4 Receptor Histamine Receptor

View All CXCR Isoform Specific Products:

View All Isoforms
CXCR CXCR1 CXCR2 CXCR3 CXCR4 CXCR7 CXCR6

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Olopatadine hydrochloride (ALO4943A; KW4679) is an orally active histamine H1 receptor antagonist and mast cell stabilizer. Olopatadine hydrochloride exerts antiallergic effects by blocking histamine H1 receptor-mediated activities. Olopatadine hydrochloride inhibits exocytosis, chemokine release, F-actin polymerization, CXCL10-induced calcium influx, and T cell chemotactic activity. Olopatadine hydrochloride also reduces the expression levels of CXCR3 on the surface of CD4+ and CD8+ T cells. Olopatadine hydrochloride inhibits scratching behavior, improves dermatitis scores, and suppresses intraepidermal neurite outgrowth. Olopatadine hydrochloride simultaneously decreases the levels of inflammatory markers, growth factors, histamine, and specific IgE, while increasing the expression of ErbB3A/HER3A. Olopatadine hydrochloride can be used in research related to seasonal pollinosis, chronic rhinitis, urticaria, allergic conjunctivitis, alopecia areata, and atopic dermatitis[1][2][3].

IC50 & Target

H1 Receptor

 

CXCR3

 

In Vitro

Olopatadine hydrochloride (1×10-6-1×10-5 M; 8 h) significantly inhibits the CXCL10-mediated chemotactic migration speed of CD4+ and CD8+ T cells isolated from patients with acute alopecia areata, with a stronger inhibitory effect at high concentrations than at low concentrations[2].
Olopatadine hydrochloride (1×10-6-1×10-5 M) significantly reduces the CXCR3 expression level and F-actin polymerization on the surface of CD4+ and CD8+ T cells isolated from patients with acute alopecia areata[2].
Olopatadine hydrochloride (1×10-6-1×10-5 M) significantly inhibits CXCL10-induced intracellular calcium influx in PBMCs isolated from one patient with acute alopecia areata, with a stronger inhibitory effect observed at the high concentration than at the low concentration[2].

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

Olopatadine hydrochloride Related Antibodies

Western Blot Analysis[2]

Cell Line: CD4+ and CD8+ T cells isolated from acute phase alopecia areata patients
Concentration: 1×10-5 M
Incubation Time: /
Result: Significantly inhibited F-actin polymerization and CXCR3 surface expression in CD4+ and CD8+ T cells isolated from acute phase alopecia areata patients.
In Vivo

Olopatadine hydrochloride (3-10 mg/kg/day; p.o.; daily; 14 days) administered orally to Dermatophagoides farinae body (Dfb)-induced atopic dermatitis NC/Nga mice significantly reduces scratching behavior, intraepidermal neurite outgrowth, skin inflammatory markers, and Dfb-specific IgE, with the 10 mg/kg/day dose additionally improving dermatitis scores, reducing epidermal thickness, increasing epidermal sema3A expression, and producing a higher scratching inhibition ratio (86.5%)[3].

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

Animal Model: NC/Nga Tnd (female, 10 weeks of age, atopic dermatitis induced by Dermatophagoides farinae body ointment + SDS skin barrier disruption)[3]
Dosage: 3 mg/kg/day; 10 mg/kg/day
Administration: p.o.; daily; 14 days (days 14-28)
Result: Significantly reduced dermatitis scores starting at day 21, with a significant improvement by day 28 (10 mg/kg/day dose).
Reduced epidermal thickness (acanthosis) significantly (10 mg/kg/day dose).
Inhibited scratching behavior with an 86.5% inhibition ratio (10 mg/kg/day dose).
Inhibited scratching behavior with a 66.7% inhibition ratio (3 mg/kg/day dose).
Reduced skin histamine levels significantly (both doses).
Reduced intraepidermal neurite outgrowth significantly (both doses).
Reduced skin nerve growth factor (NGF) protein and mRNA expression significantly (both doses).
Reduced skin amphiregulin protein expression significantly (both doses).
Increased epidermal semaphorin 3A (sema3A) mRNA expression significantly (10 mg/kg/day dose).
Reduced skin levels of IL-1β, TNF-α, IL-6, GM-CSF, and E-selectin significantly (10 mg/kg/day dose).
Reduced skin levels of IL-1β, TNF-α, GM-CSF, and E-selectin significantly (3 mg/kg/day dose).
Reduced total serum IgE by 31.9% (not statistically significant, 10 mg/kg/day dose).
Reduced total serum IgE by 6.4% (not statistically significant, 3 mg/kg/day dose).
Reduced serum Dfb-specific IgE titer significantly (10 mg/kg/day dose).
Reduced serum Dfb-specific IgE titer significantly compared to control (3 mg/kg/day dose).
Clinical Trial
Molecular Weight

373.87

Formula

C21H24ClNO3
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(O)CC1=CC=C(C/2=C1)OCC3=CC=CC=C3C2=C\CCN(C)C.Cl
Structure Classification
Initial Source
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: 

DMSO : 50 mg/mL (133.74 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : 6.67 mg/mL (17.84 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 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
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.

  • Molarity Calculator

  • 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: ≥ 2.5 mg/mL (6.69 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: ≥ 2.5 mg/mL (6.69 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.

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: 17.14 mg/mL (45.84 mM); Clear solution; Need ultrasonic

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.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

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

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).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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
H2O / DMSO 1 mM 2.6747 mL 13.3736 mL 26.7473 mL 66.8682 mL
5 mM 0.5349 mL 2.6747 mL 5.3495 mL 13.3736 mL
10 mM 0.2675 mL 1.3374 mL 2.6747 mL 6.6868 mL
15 mM 0.1783 mL 0.8916 mL 1.7832 mL 4.4579 mL
DMSO 20 mM 0.1337 mL 0.6687 mL 1.3374 mL 3.3434 mL
25 mM 0.1070 mL 0.5349 mL 1.0699 mL 2.6747 mL
30 mM 0.0892 mL 0.4458 mL 0.8916 mL 2.2289 mL
40 mM 0.0669 mL 0.3343 mL 0.6687 mL 1.6717 mL
50 mM 0.0535 mL 0.2675 mL 0.5349 mL 1.3374 mL
60 mM 0.0446 mL 0.2229 mL 0.4458 mL 1.1145 mL
80 mM 0.0334 mL 0.1672 mL 0.3343 mL 0.8359 mL
100 mM 0.0267 mL 0.1337 mL 0.2675 mL 0.6687 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.

  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.

Olopatadine hydrochloride 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:

Olopatadine140462-76-6ALO4943A KW4679KW4679KW 4679KW-4679Histamine ReceptorCXCRCXC chemokine receptorsC-X-C motif chemokine receptorsCD4+ T cellsmast cellCXCL10CD8+ T cellsCXCR3allergic conjunctivitisalopecia areatasemaphorin 3Aatopic dermatitishistamine H1 receptorInhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

  

Requested Quantity *

Applicant Name *

 

Salutation

Email Address *

 

Phone Number *

Department

 

Organization Name *

City

State

Country or Region *

      

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
Olopatadine hydrochloride
Cat. No.:
HY-B0426A
Quantity:
MCE Japan Authorized Agent:

Customer Review

Thank You for Your Feedback!

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

Product Name

  

Lot #

Applicant Name *

 

Email Address *

Phone Number

 

Department *

Organization Name *

 

Country or Region *

Remarks

SAFETY DATA SHEET (SDS)

English - EN (623 KB) Français - FR (623 KB) Deutsch - DE (623 KB) Norwegian - NO (623 KB) Español - ES (623 KB) Swedish - SV (623 KB) Italian - IT (623 KB) Korean - KR (623 KB) Portuguese - PT (623 KB)

Request for HNMR Report

We have received your request and will respond to you as soon as possible.