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Merck
CN

SML0119

Acrivastine

≥98% (HPLC)

Synonym(s):

(E)-6-((E)-3-(1-Pyrrolidinyl)-1-p-tolylpropenyl)-2-pyridineacrylic acid

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About This Item

Empirical Formula (Hill Notation):
C22H24N2O2
CAS Number:
87848-99-5
Molecular Weight:
348.44
NACRES:
NA.77
PubChem Substance ID:
329825170
UNSPSC Code:
12352200
MDL number:
MFCD00869830
Assay:
≥98% (HPLC)
Form:
powder
Quality level:
100
Storage condition:
desiccated

Key Documents

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Product Name

Acrivastine, ≥98% (HPLC)

InChI

1S/C22H24N2O2/c1-17-7-9-18(10-8-17)20(13-16-24-14-2-3-15-24)21-6-4-5-19(23-21)11-12-22(25)26/h4-13H,2-3,14-16H2,1H3,(H,25,26)/b12-11+,20-13+

SMILES string

Cc1ccc(cc1)\C(=C/CN2CCCC2)c3cccc(\C=C\C(O)=O)n3

InChI key

PWACSDKDOHSSQD-IUTFFREVSA-N

assay

≥98% (HPLC)

form

powder

storage condition

desiccated

color

white to beige

solubility

DMSO: >2 mg/mL (warmed)

storage temp.

2-8°C

Quality Level

100

Gene Information

human ... HRH1(3269)

Application

Acrivastine has been used as an antihistamine to investigate the relation between the increased residence time of antihistamine at the histamine H1 receptor (H1R) and the duration of effective target-inhibition by this antagonist.

Biochem/physiol Actions

Acrivastine is a second-generation H1-receptor antagonist.
Acrivastine is a second-generation antihistamine, an H1-receptor antagonist.
Acrivastine is a second-generation antihistamine. It is a derivative of first-generation compound triprolidine. Acrivastine is effectively used for treating allergic diseases including cholinergic urticaria and histamine-medicated dermatoses.

Storage Class

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

Regulatory Information

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Certificates of Analysis (COA)

Lot/Batch Number
0000321748
0000321748
052M4713V
0000040978
0000040979

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M J Mattila et al.
European journal of clinical pharmacology, 55(2), 85-93 (1999-05-21)
Most of the modern non-sedating H1 receptor antagonists (antihistamines) penetrate the brain poorly, allowing the use of doses large enough to counteract allergic processes in peripheral tissues without important central effects. The antihistamines reviewed here are acrivastine, astemizole, cetirizine, ebastine
A Reimers et al.
Clinical and experimental allergy : journal of the British Society for Allergy and Clinical Immunology, 32(12), 1763-1768 (2003-03-26)
Leukotriene receptor antagonists have shown some efficacy in t he treatment of asthma. Injection of LTC4, LTD4 and LTE4 into the skin leads to a weal-and-flare reaction, suggesting an involvement of leukotrienes in the pathogenesis of urticaria. Indeed, various reports
R D Mann et al.
BMJ (Clinical research ed.), 320(7243), 1184-1186 (2000-04-28)
To investigate the frequency with which sedation was reported in post-marketing surveillance studies of four second generation antihistamines: loratadine, cetirizine, fexofenadine, and acrivastine. Prescription-event monitoring studies. Prescriptions were obtained for each cohort in the immediate post-marketing period. Event data were
R N Brogden et al.
Drugs, 41(6), 927-940 (1991-06-01)
Acrivastine is a short acting histamine H1-receptor antagonist with a rapid onset of action. Double-blind clinical trials have shown acrivastine (usually 8mg three times daily) to be an effective and well tolerated antihistamine in the treatment of chronic urticaria and
Ilari Paakkari
Toxicology letters, 127(1-3), 279-284 (2002-06-08)
Although the new second-generation nonsedative antihistamines terfenadine and astemizole were launched as highly selective and specific H(1)-receptor antagonists, they were later found to cause prolongation of the QT-interval and severe cardiac arrhythmias. The prolongation of the QT-interval is caused by
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