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

Rupatadine Fumarate (Synonyms: UR-12592 Fumarate)

Cat. No.: HY-13511A Purity: 99.93%
Handling Instructions

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

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

Rupatadine Fumarate Chemical Structure

Rupatadine Fumarate Chemical Structure

CAS No. : 182349-12-8

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10 mM * 1 mL in DMSO USD 106 In-stock
Estimated Time of Arrival: December 31
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ready for reconstitution
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Estimated Time of Arrival: December 31
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Estimated Time of Arrival: December 31
500 mg USD 198 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of Rupatadine Fumarate:

Top Publications Citing Use of Products

1 Publications Citing Use of MCE Rupatadine Fumarate

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  • Customer Review

Description

Rupatadine (UR-12592) Fumarate is a potent, orally active and long-lasting dual PAF/H1 antagonist, with Kis of 0.55 μM and 0.1 μM, respectively. Rupatadine Fumarate 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)

In Vitro

Rupatadine Fumarate competitively inhibits histamine-induced guinea pig ileum contraction (pA2=9.29) without affecting contraction induced by ACh, serotonin or leukotriene D4 (LTD4)[1].
Rupatadine Fumarate 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) Fumarate inhibits TNF-α secretion in a concentration-dependent manner, with maximum values of 92.5%[2].

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

In Vivo

Rupatadine Fumarate 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 Fumarate 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) Fumarate promotes the absorption of the lesions and decreased the density of lungs[3].

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

532.03

Formula

C₃₀H₃₀ClN₃O₄

CAS No.
Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 30 mg/mL (56.39 mM; Need ultrasonic and warming)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.8796 mL 9.3980 mL 18.7959 mL
5 mM 0.3759 mL 1.8796 mL 3.7592 mL
10 mM 0.1880 mL 0.9398 mL 1.8796 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (3.91 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (3.91 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (3.91 mM); Clear solution

*All of the co-solvents are provided by MCE.
References

Purity: 99.93%

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Rupatadine Fumarate
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