Olopatadine hydrochloride
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)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biological Activity
-
Chemical Information
-
Solvent & Solubility
- Protocols
- Purity & Documentation
- References
-
Help & FAQs
-
HY-B0426AR
Olopatadine hydrochloride (Standard)Histamine Receptor Blocker -
HY-B0083
LeflunomideDHODH Inhibitor -
HY-17042A
Cetirizine dihydrochlorideH1-receptor Antagonist -
HY-B0157A
Ketotifen fumarateHistamine 1 Receptor Blocker -
HY-B0577
LatanoprostProstaglandin Receptor Agonist -
HY-B0191
BimatoprostProstaglandin Analog -
HY-B0640A
Epinastine hydrochlorideHistamine H1 Receptor Antagonist -
HY-B0600
TafluprostProstaglandin Receptor Agonist -
HY-113756A
Latanoprost acidFP Agonist -
HY-B0781
Promethazine hydrochlorideHistamine Receptor Antagonist -
HY-B0170A
Azatadine dimaleateHistamine H1 Receptor Inhibitor -
HY-A0128A
Buclizine dihydrochlorideAntihistamine Agent
All Histamine Receptor Isoforms
More
Biological Activity
Description
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. Further protocols information, click here.
-
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
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
|
|---|---|---|---|---|
| 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
-
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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.
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.
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:
-
-
-
-
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
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)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Protocols
-
PC12 NGF-Induced Neuronal Differentiation Culture
PC12 cells are a rat adrenal pheochromocytoma clonal line that responds to NGF by stopping proliferation and extending branching neurite-like processes; after longer NGF exposure, cells develop long processes and neuronal-like ultrastructural and functional features. NGF-induced differentiation is read out mainly by neurite outgrowth, reduced proliferation, microtubule assembly, and neuronal differentiation-associated proteins such as MAPs, tau, GAP-43, and synapsin-1.
-
RNA extraction experimental
By lysing cells, releasing RNA, and removing impurities such as proteins and DNA, high-purity RNA products are finally obtained. The commonly used traditional method is the guanidine isothiocyanate/phenol/chloroform method (Trizol), which is suitable for a variety of animal materials including animal tissues, microorganisms, cultured cells, etc., and most plant materials.
-
SH-SY5Y Neuronal Differentiation Culture
SH-SY5Y neuronal differentiation culture uses sequential exposure to retinoic acid and neurotrophic factors to reduce proliferative neuroblastoma-like behavior and induce neuron-like morphology, including neurite extension, neuronal marker expression, and, in RA/BDNF protocols, greater synaptic-marker expression than undifferentiated culture. Retinoic acid is commonly used as the initiating differentiation cue, while BDNF in serum-reduced or serum-free medium supports later maturation and neurotrophic-factor-dependent neuron-like survival.
-
TPA/Croton Oil Ear Edema and Dermatitis
The TPA (12-O-tetradecanoylphorbol-13-acetate) and croton oil-induced mouse ear edema model is a well-established acute cutaneous inflammation system used to evaluate topical anti-inflammatory activity by measuring edema formation, neutrophil infiltration, vascular permeability, and cytokine-mediated skin responses in vivo. The inflammatory response is triggered by topical application of phorbol esters (TPA) or croton oil constituents, leading to rapid activation of protein kinase C signaling, leukocyte recruitment, and increased vascular permeability, which can be quantified by ear thickness, weight, dye extravasation, and biochemical markers such as myeloperoxidase (MPO) activity and pro-inflammatory mediators in ear tissue homogenates. This model is widely used for screening anti-inflammatory agents, where reductions in edema and inflammatory biomarkers reflect suppression of acute dermal inflammation and immune cell infiltration. Histological evaluation typically confirms epidermal
-
SH-SY5Y neuronal-like differentiation
SH-SY5Y neuronal-like differentiation uses defined culture conditions to shift proliferative human neuroblastoma cells toward a neuron-like state, mainly assessed by reduced proliferation, neurite extension, neuronal-marker expression, and, in some protocols, increased dependence on neurotrophic support. Retinoic acid (RA) is commonly used for the first differentiation phase, and sequential RA followed by brain-derived neurotrophic factor (BDNF) in serum-free medium is a well-characterized approach for generating neuron-like SH-SY5Y cultures with extensive neurite outgrowth. The primary readouts are morphology-based neurite outgrowth and marker-based confirmation using proteins such as βIII-tubulin, MAP2, GAP43, synaptophysin, NeuN, NSE, TH, or related neuronal/synaptic markers, depending on the study endpoint.
-
Cell differentiation
Cell differentiation refers to the process in which cells of the same origin gradually produce cell groups with different morphological structure and functional characteristics.
-
Ca2+ Staining Technique
Ca2+ staining is an experimental technique that utilizes specific fluorescent probes (such as Fluo-4 AM, Fura-2, etc.) to qualitatively or quantitatively detect dynamic changes in intracellular Ca2+ concentrations; this is achieved by monitoring the changes in fluorescent signals generated when these probes bind to free intracellular calcium ions. The underlying principle relies primarily on the presence of chelating groups within the probe's molecular structure that possess high affinity for calcium ions.
-
PC12 NGF-induced neuronal-like differentiation
PC12 cells are a rat adrenal pheochromocytoma-derived clonal cell line that responds to nerve growth factor by stopping proliferation and extending neurites, producing a sympathetic neuron-like phenotype used to study neuronal differentiation and neurite outgrowth. NGF acts through TrkA-dependent signaling, and neurite outgrowth is associated with ERK/Akt signaling, microtubule organization, neuronal-marker expression, and increased electrophysiological neuronal features such as sodium-channel density. The main assay readout is morphological differentiation, usually measured as the percentage of neurite-bearing cells, neurite length, neurite number, or total neurite length per cell. Additional readouts include GAP-43, tyrosine hydroxylase, βIII-tubulin, neurofilament, synapsin I, synaptophysin, ERK phosphorylation, Akt phosphorylation, and sodium-channel current density.
-
Research Protocol for Cancer Immunology
Cancer immunology studies how the immune system recognizes, suppresses, edits, or fails to eliminate malignant cells through tumor antigen release, antigen presentation, T-cell priming, immune trafficking, tumor-cell killing, and feedback inhibition in the tumor microenvironment. The cancer-immunity cycle links tumor antigenicity, dendritic-cell priming, CD8+ T-cell infiltration, cytotoxic function, and immune-checkpoint regulation to tumor rejection or immune escape. Immune-checkpoint pathways such as PD-1/PD-L1 and CTLA-4 suppress antitumor T-cell activity and can be therapeutically blocked, but many tumors remain resistant because of poor antigen presentation, weak T-cell infiltration, suppressive myeloid cells, regulatory T cells, and tumor-intrinsic immune-exclusion programs. Unresolved questions include which immune-cell states predict response, how tumor-intrinsic pathways exclude immune cells, how myeloid suppression limits checkpoint blockade, and which combination strategies
-
Phalloidin F-actin cytoskeleton staining
Phalloidin F-actin staining detects polymerized filamentous actin in fixed and permeabilized specimens by using fluorescent phalloidin or phalloidin-derived phallotoxins that bind actin filaments and generate a fluorescence microscopy readout corresponding to F-actin organization, including stress fibers, cortical actin, filament bundles, and tissue-specific actin networks. Phalloidin stabilizes F-actin by reducing actin subunit dissociation from filament ends, and fluorescent phallotoxins were established as tools for visualizing actin-containing structures in eukaryotic cells.
Purity & Documentation
-
Data Sheet (297 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)
-
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]
[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]
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.
Olopatadine hydrochloride Related Classifications
HY-B0426A Related Classifications
Powered by Bioz