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

Rupatadine Chemical Structure

CAS No. : 158876-82-5

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Customer Review

Based on 2 publication(s) in Google Scholar

Other Forms of Rupatadine:

Rupatadine Related Antibodies

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  • Biological Activity

  • Purity & Documentation

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  • Customer Review

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

-20°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 : 100 mg/mL (240.41 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
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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.

  • 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.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • 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.

    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.
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.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: 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)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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.
Purity & Documentation

Purity: 99.96%

SDS (393 KB)

COA (255 KB) HNMR (337 KB) RP-HPLC (262 KB) MS (71 KB)

Handling Instructions (2659 KB)
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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