Cat. No.: HY-B0426A

Olopatadine hydrochloride

(Synonyms: ALO4943A; KW4679)

Customer Review

Based on 1 Customer Validation

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.

Purity: 99.83%
CAS No.: 140462-76-6
Formula: C₂₁H₂₄ClNO₃
Molecular Weight:373.87

Storage:

4°C, sealed storage, away from moisture

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

Olopatadine hydrochloride Chemical Structure

CAS No.: 140462-76-6

Size

Price

Stock

Quantity

Amount: USD 0.00

* Please select Quantity before adding items.

Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Solvent & Solubility
- In Vitro
- In Vivo
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target

H₁ Receptor

CXCR3

All Histamine Receptor Isoforms :

All CXCR Isoforms :

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.

Western Blot Analysis^[2]

Cell Line:

CD4⁺ and CD8⁺ T cells isolated from acute phase alopecia areata patients
Concentration:

1×10^-5M
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

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

Chemical Information

CAS No. 140462-76-6
Appearance Solid
Molecular Weight 373.87
Formula C₂₁H₂₄ClNO₃
Color White to off-white
SMILES

O=C(O)CC1=CC=C(C/2=C1)OCC3=CC=CC=C3C2=C\CCN(C)C.Cl
Synonyms

ALO4943A; KW4679
Structure Classification
- Alkaloids
- Other Alkaloids
- Ketones, Aldehydes, Acids
Initial Source
- Endogenous metabolite
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)

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

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

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

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

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: ≥ 2.5 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.

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.

Protocol 3

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

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

This protocol yields a clear solution of ≥ 2.5 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 (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

Working Solution

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 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.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (284 KB)
SDS (623 KB)
- 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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
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)
Handling Instructions (2659 KB)

References

[1]. Baba A, et al. Olopatadine inhibits exocytosis in rat peritoneal mast cells by counteracting membrane surface deformation. Cell Physiol Biochem. 2015;35(1):386-396. [Content Brief]

[2]. Ito T, et al. Antihistaminic drug olopatadine downmodulates T cell chemotaxis toward CXCL10 by reducing CXCR3 expression, F-actin polymerization and calcium influx in patients with alopecia areata[J]. Journal of Dermatological Science, 2013, 72(1): 68-71.

[3]. Murota H, et al. Olopatadine hydrochloride improves dermatitis score and inhibits scratch behavior in NC/Nga mice. Int Arch Allergy Immunol. 2010;153(2):121-132. [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
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.

Product Name:
Cat. No.:
Quantity:
MCE Japan Authorized Agent:

Product Name:
CAS No.:
Species:
Purity:
Quantity:

Olopatadine hydrochloride

Bioactive Compound Library Max

Bioactive Compound Library

Anti-Infection Compound Library

GPCR/G Protein Compound Library

Immunology/Inflammation Compound Library

Neuronal Signaling Compound Library

FDA-Approved Drug Library

Small Molecule Immuno-Oncology Compound Library

Drug Repurposing Compound Library

Anti-COVID-19 Compound Library

NMPA-Approved Drug Library

Orally Active Compound Library

Neurotransmitter Receptor Compound Library

FDA Approved & Pharmacopeial Drug Library

Alkaloids Library

Anti-Parkinson's Disease Compound Library

Neurodegenerative Disease-related Compound Library

Anti-Obesity Compound Library

Protein-protein Interaction Inhibitor Library

EMA-Approved Drug Library

Human Metabolite Library

Anti-Pulmonary Fibrosis Compound Library

Non-steroidal Anti-Inflammatory Compound Library

Chemokine Compound Library

Coagulation and Anti-coagulation Compound Library

Off-patent Drug Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Inhibitors Library

Cytokine Inhibitors Library

Multi-Target Compound Library

Radioprotector Library

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

FDA-Approved Drug Library Plus

FDA-Approved Drug Library Mini

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

RO5 Drug-like Natural Product Library

High-Throughput Bioactive Compound Library

Anti-Rheumatic Arthritis Compound Library

Mass Spectrometry Human Metabolite Library

Natural Product Diversity Scaffold Library

Lactylation Compound Library

All Histamine Receptor Isoforms

All CXCR Isoforms

Biological Activity

Chemical Information

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Olopatadine hydrochloride Related Classifications

HY-B0426A Related Classifications