Art. -Nr.: HY-13511

Rupatadine

(Synonyms: UR-12592)

2 Cited Publications

Kundenbewertung

Based on 2 publication(s) in Google Scholar

Rupatadine (UR-12592) is a potent, orally active and long-lasting dual PAF/H1 antagonist, with K_is of 0.55 μM and 0.1 μM, respectively. Rupatadine can be used for the research of allergic rhinitis and urticaria.

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Reinheit: 99.96%
CAS. Nr.: 158876-82-5
Formel: C₂₆H₂₆ClN₃
Molecular Weight:415.96

Speicherung:

-20°C, sealed storage, away from moisture

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

Rupatadine Chemical Structure

CAS. Nr.: 158876-82-5

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (2)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

H₁ Receptor

0.1 μM (Ki)

PAF

0.55 μM (Ki)

Alle Histamine Receptor Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
HEK293	IC₅₀	>40 μM Compound: Rupatadine	Inhibition of eGFP-tagged human B0AT2 expressed in HEK293 cells measured within 10 mins by [3H]proline uptake assay Inhibition of eGFP-tagged human B0AT2 expressed in HEK293 cells measured within 10 mins by [3H]proline uptake assay	[PMID: 25318072]

In Vitro

Rupatadine competitively inhibits histamine-induced guinea pig ileum contraction (pA₂=9.29) without affecting contraction induced by ACh, serotonin or leukotriene D4 (LTD4)^[1].
Rupatadine competitively inhibits PAF-induced platelet aggregation in washed rabbit platelets (WRP) (pA₂=6.68) and in human platelet-rich plasma (HPRP) (IC₅₀=0.68 μM), while not affecting ADP- or arachidonic acid-induced platelet aggregation^[1].
Rupatadine (0.1-30 μM) inhibits TNF-α secretion in a concentration-dependent manner, with maximum values of 92.5%^[2].

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

In Vivo

Rupatadine blocks histamine- and PAF-induced effects in vivo, such as hypotension in rats (ID₅₀=1.4 and 0.44 mg/kg i.v., respectively) and bronchoconstriction in guinea pigs (ID₅₀=113 and 9.6 μg/kg i.v.)^[1].
Rupatadine potently inhibits PAF-induced mortality in mice (ID₅₀=0.31 and 3.0 mg/kg i.v. and p.o., respectively) and endotoxin-induced mortality in mice and rats (ID₅₀=1.6 and 0.66 mg/kg i.v.)^[1].
Rupatadine (6 mg/kg) promotes the absorption of the lesions and decreased the density of lungs^[3].

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

Animal Model:

Male C57BL/6J mice (18 g, 6-8 wk)^[3]
Dosage:

1.5, 3, 6 mg/kg
Administration:

Oral gavage once a day
Result:

Markedly decreased the BLM-enhanced inflammatory scores and lung index.

Clinical Trial

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

Chemical Information

CAS. Nr. 158876-82-5
Appearance Solid
Molecular Weight 415.96
Formel C₂₆H₂₆ClN₃
Color Off-white to light yellow
SMILES

CC1=CN=CC(CN2CC/C(CC2)=C3C4=CC=C(Cl)C=C4CCC5=CC=CN=C5\3)=C1
Synonyms

UR-12592
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

-20°C, sealed storage, away from moisture

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

Publications (2)

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Journal Impact Factor

Biomed Pharmacother

Rupatadine inhibits colorectal cancer cell proliferation through the PIP5K1A/Akt/CDK2 pathway. [Abstract]

2024 Jun 4:176:116826. PMID: 38838507
Pharmaceutics

Elucidation of Inverse Agonist Activity of Bilastine. [Abstract]

2020 Jun 8;12(6):525. PMID: 32521742

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (240.41 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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

2.4041 mL

12.0204 mL

24.0408 mL

5 mM

0.4808 mL

2.4041 mL

4.8082 mL

10 mM

0.2404 mL

1.2020 mL

2.4041 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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

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 (6.01 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 (6.01 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 (6.01 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.

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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (280 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 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)

Verweise

[1]. Merlos M, et al. Rupatadine, a new potent, orally active dual antagonist of histamine and platelet-activating factor (PAF). J Pharmacol Exp Ther. 1997 Jan;280(1):114-21. [Content Brief]

[2]. Queralt M, et al. In vitro inhibitory effect of rupatadine on histamine and TNF-alpha release from dispersed canine skin mast cells and the human mast cell line HMC-1. Inflamm Res. 2000 Jul;49(7):355-60. [Content Brief]

[3]. Lv XX, et al. Rupatadine protects against pulmonary fibrosis by attenuating PAF-mediated senescence in rodents. PLoS One. 2013 Jul 15;8(7):e68631. [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
DMSO	1 mM	2.4041 mL	12.0204 mL	24.0408 mL	60.1019 mL
	5 mM	0.4808 mL	2.4041 mL	4.8082 mL	12.0204 mL
	10 mM	0.2404 mL	1.2020 mL	2.4041 mL	6.0102 mL
	15 mM	0.1603 mL	0.8014 mL	1.6027 mL	4.0068 mL
	20 mM	0.1202 mL	0.6010 mL	1.2020 mL	3.0051 mL
	25 mM	0.0962 mL	0.4808 mL	0.9616 mL	2.4041 mL
	30 mM	0.0801 mL	0.4007 mL	0.8014 mL	2.0034 mL
	40 mM	0.0601 mL	0.3005 mL	0.6010 mL	1.5025 mL
	50 mM	0.0481 mL	0.2404 mL	0.4808 mL	1.2020 mL
	60 mM	0.0401 mL	0.2003 mL	0.4007 mL	1.0017 mL
	80 mM	0.0301 mL	0.1503 mL	0.3005 mL	0.7513 mL
	100 mM	0.0240 mL	0.1202 mL	0.2404 mL	0.6010 mL

Keywords

Rupatadine

2 Cited Publications

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Publications Citing Use of MedChemExpress (MCE) Rupatadine

Alle Histamine Receptor Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (2)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Rupatadine Related Classifications

HY-13511 Related Classifications