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Rupatadine

Name: Rupatadine
Brand: TargetMol
SKU: T36618
Price: 30 USD
Availability: InStock
Rating: 5 (10 reviews)

🥰Excellent

Catalog No. T36618Cas No. 158876-82-5

Alias UR-12592, UR12592

Rupatadine (UR-12592, rupatadine) is a potent and orally available dual antagonist of PAF and histamine H1 receptors with Ki values of 0.55 μM and 0.1 μM, respectively, which provides relief of allergic symptoms and anti-inflammatory properties, and is used in allergic rhinitis and chronic urticaria.

Rupatadine

🥰Excellent

Purity: 99.87%

Catalog No. T36618Alias UR-12592, UR12592Cas No. 158876-82-5

Pack Size	Price	USA Warehouse	Global Warehouse
10 mg	$30	In Stock	In Stock
25 mg	$52	In Stock	In Stock
50 mg	$87	In Stock	In Stock
100 mg	$135	In Stock	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

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Purity:99.87%

Appearance:Solid

Color:White

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COA LCMS HNMR

Product Introduction

Bioactivity

Description	Rupatadine (UR-12592, rupatadine) is a potent and orally available dual antagonist of PAF and histamine H1 receptors with Ki values of 0.55 μM and 0.1 μM, respectively, which provides relief of allergic symptoms and anti-inflammatory properties, and is used in allergic rhinitis and chronic urticaria.
Targets&IC50	H1 Receptor:0.1 μM (Ki), PAF-induced platelet aggregation (human plasma):0.68 μM, PAF:0.55 μM (Ki)
In vitro	Rupatadine acts as a dual H1 and PAF receptor antagonist. Rupatadine has a Ki of 0.10 μM for H1 and 0.55 μM for PAF receptors. Rupatadine competitively inhibits histamine-induced guinea pig ileum contraction (pA₂ = 9.29), and PAF-induced platelet aggregation in rabbit platelets (pA₂ = 6.68) and human plasma (IC₅₀ = 0.68 μM), without affecting ACh, 5-HT, or LTD₄ responses[1].
In vivo	Rupatadine blocks histamine- and PAF-induced hypotension (ID₅₀ = 1.4 and 0.44 mg/kg i.v.) and bronchoconstriction (113 and 9.6 μg/kg i.v.). Rupatadine protects mice from PAF- and endotoxin-induced death (ID₅₀ = 0.31-3.0 mg/kg). In dogs, 1 mg/kg p.o. still inhibited vascular permeability >26 h. No sedation was observed at 100 mg/kg[1].
Synonyms	UR-12592, UR12592

Chemical Properties

Molecular Weight	415.96
Formula	C₂₆H₂₆ClN₃
Cas No.	158876-82-5
Smiles	ClC=1C=CC2=C(C1)CCC=3C=CC=NC3C2=C4CCN(CC=5C=NC=C(C5)C)CC4

Storage & Solubility Information

Storage

keep away from moisture | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 100 mg/mL (240.41 mM), Sonication is recommended.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.4041 mL	12.0204 mL	24.0408 mL	120.2039 mL
5 mM	0.4808 mL	2.4041 mL	4.8082 mL	24.0408 mL
10 mM	0.2404 mL	1.2020 mL	2.4041 mL	12.0204 mL
20 mM	0.1202 mL	0.6010 mL	1.2020 mL	6.0102 mL
50 mM	0.0481 mL	0.2404 mL	0.4808 mL	2.4041 mL
100 mM	0.0240 mL	0.1202 mL	0.2404 mL	1.2020 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc