2. GPCR/G Protein Neuronal Signaling Immunology/Inflammation Autophagy
  3. Histamine Receptor Autophagy
  4. Rupatadine

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

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

Rupatadine Chemical Structure

Rupatadine Chemical Structure

CAS No. : 158876-82-5

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Based on 2 publication(s) in Google Scholar

Other Forms of Rupatadine:

Rupatadine Related Antibodies

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  • Biological Activity

  • Purity & Documentation

  • References

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Description

Rupatadine (UR-12592) is a potent, orally active and long-lasting dual PAF/H1 antagonist, with Kis of 0.55 μM and 0.1 μM, respectively. Rupatadine can be used for the research of allergic rhinitis and urticaria[1][2][3].

IC50 & Target[1]

H1 Receptor

0.1 μM (Ki)

PAF

0.55 μM (Ki)

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.

Rupatadine Related Antibodies
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
Molecular Weight

415.96

Formula

C26H26ClN3
CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

CC1=CN=CC(CN2CC/C(CC2)=C3C4=CC=C(Cl)C=C4CCC5=CC=CN=C5\3)=C1
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 : 125 mg/mL (300.51 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.4041 mL 12.0204 mL 24.0408 mL
5 mM 0.4808 mL 2.4041 mL 4.8082 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.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
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Concentration
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Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

=
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C2

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V2

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.
Calculation results:
Working solution concentration: mg/mL
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
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
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Rupatadine 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:

Rupatadine158876-82-5UR-12592UR12592UR 12592Histamine ReceptorAutophagyPAFH1allergicrhinitisurticariaInhibitorinhibitorinhibit

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