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Rupatadine

Product Name
Rupatadine
CAS No.
158876-82-5
Chemical Name
Rupatadine
Synonyms
Rupax;Rupafi;Rupafin;Pafinur;Rinialer;UR-12592;ROPATADINE;Rupatidine;RUPATADINE;Alergoliber
CBNumber
CB1346639
Molecular Formula
C26H26ClN3
Formula Weight
415.96
MOL File
158876-82-5.mol
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Rupatadine Property

Melting point:
58-61°C
Boiling point:
586.4±50.0 °C(Predicted)
Density 
1.233±0.06 g/cm3(Predicted)
storage temp. 
Store at -20°C
solubility 
Dichloromethane; Ethyl Acetate
form 
Oil
pka
6.95±0.20(Predicted)
CAS DataBase Reference
158876-82-5(CAS DataBase Reference)
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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Warning
Hazard statements

H302Harmful if swallowed

H413May cause long lasting harmful effects to aquatic life

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N-Bromosuccinimide Price

Matrix Scientific
Product number
093670
Product name
8-Chloro-11-(1-((5-methylpyridin-3-yl)methyl)piperidin-4-ylidene)-6,11-dihydro-5H-benzo[5,6]cyclohepta[1,2-b]pyridine
Purity
95+%
Packaging
250mg
Price
$120
Updated
2021/12/16
Matrix Scientific
Product number
093670
Product name
8-Chloro-11-(1-((5-methylpyridin-3-yl)methyl)piperidin-4-ylidene)-6,11-dihydro-5H-benzo[5,6]cyclohepta[1,2-b]pyridine
Purity
95+%
Packaging
1g
Price
$299
Updated
2021/12/16
American Custom Chemicals Corporation
Product number
API0004113
Product name
RUPATADINE
Purity
95.00%
Packaging
1G
Price
$975.45
Updated
2021/12/16
American Custom Chemicals Corporation
Product number
API0004113
Product name
RUPATADINE
Purity
95.00%
Packaging
2.5G
Price
$2277.8
Updated
2021/12/16
American Custom Chemicals Corporation
Product number
API0004113
Product name
RUPATADINE
Purity
95.00%
Packaging
5G
Price
$4305
Updated
2021/12/16
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Rupatadine Chemical Properties,Usage,Production

Chemical Properties

Rupatadine is off white to pinkish crystalline powder. It is soluble in methanol and ethanol slightly soluble in Chloroform and insoluble inwater.

Uses

Rupatadine Fumarate is a dual antagonist of histamine H1 and platelet-activating factor receptors. Rupatadine fumarate has been approved for the treatment of allergic rhinitis and chronic urticaria in adults and children over 12 years.

Uses

Rupatadine is an intermediate in the synthesis of Rupatadine (5-Methyl-3-pyridinyl)methyl)pyridinium Chloride (M326740). (5-Methy-3-pyridinyl)methyl-Rupatadine is an impurity of Rupatadine (R701650), a dual antagonist of histamine H1 and platelet-activating factor receptors

Definition

ChEBI: Rupatadine is a benzocycloheptapyridine.

Biological Activity

Rupatadine is an antagonist of histamine H1 and platelet-activating factor (PAF) receptors. It binds to rabbit platelet membranes and guinea pig cerebellum membranes with apparent Ki values of 0.55 and 0.1 μM, respectively, in radioligand binding assays. It inhibits contraction of isolated guinea pig ileum induced by histamine (pA2 = 9.29) and platelet aggregation induced by PAF in washed rabbit platelets (pA2 = 6.68). Rupatadine prevents histamine- or PAF-induced hypotension in rats (ID50s = 1.4 and 0.44 mg/kg, respectively) and reverses histamine- or PAF-induced bronchoconstriction in guinea pigs (ID50s = 113 and 9.6 mg/kg, respectively). It does not reduce locomotor activity or potentiate sleep induced by barbiturates in mice, indicating a lack of sedative effects.

Pharmacokinetics

Rupatadine was rapidly absorbed after oral administration, with a time taken to reach the maximum plasma concentration (Tmax) of 1 hour (median value). The maximum plasma concentration (Cmax) obtained after single and repeated doses of 10 mg rupatadine were from 1.54 to 4.03 ng/mL and from 1.99 to 4.74 ng/mL respectively. Steady state was reached by the fifth day of therapy without extensive accumulation and the plasma concentration-time curve during a time dose interval (AUCτ) ranged from 8.37 to 16.2 ng.h/mL. Pharmacokinetics of rupatadine was linear for a dose between 10 and 20 mg after single and repeated doses. The plasma concentration followed a bi-exponential drop-off with a mean elimination half-life after a single dose of 6.1 hours.

Side effects

Common side effects (may affect up to 1 in 10 people):
Sleepiness, headache, dizziness, dry mouth, sensation of weakness and fatigue.
Uncommon side effects (may affect up to 1 in 100 people):
Increased appetite, irritability, difficulty concentrating, nosebleed, nasal dryness, sore throat, cough, dry throat, rhinitis, nausea, abdominal pain, diarrhoea, indigestion, vomiting, constipation, rash, back pain, joint pain, muscle pain, thirst, general discomfort, fever, abnormal liver function test and increased weight.

Mode of action

Rupatadine is a second generation, non-sedating, long-acting histamine antagonist with selective peripheral H1receptor antagonist activity. It further blocks the receptors of the platelet-activating factor (PAF) according to in vitro and in vivo studies.
Rupatadine possesses anti-allergic properties such as the inhibition of the degranulation of mast cells induced by immunological and non-immunological stimuli, and inhibition of the release of cytokines, particularly of the tumor necrosis factors (TNF) in human mast cells and monocytes.

Rupatadine Preparation Products And Raw materials

Raw materials

Preparation Products

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Rupatadine Suppliers

CARBONE SCIENTIFIC CO.,LTD
Tel
--
Fax
--
Email
sales@carbonesci.com
Country
United Kingdom
ProdList
6666
Advantage
30
Sequoia Research Products Ltd.
Tel
--
Fax
--
Email
sales@seqchem.com
Country
United Kingdom
ProdList
3113
Advantage
69
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View Lastest Price from Rupatadine manufacturers

Henan Bao Enluo International TradeCo.,LTD
Product
Rupatadine 158876-82-5
Price
US $100.00/kg
Min. Order
1kg
Purity
99%
Supply Ability
1000tons
Release date
2023-08-14
Career Henan Chemical Co
Product
Rupatadine fumarate 158876-82-5
Price
US $100.00/KG
Min. Order
1KG
Purity
98%
Supply Ability
10KG,20KG
Release date
2018-07-25
Hebei Jimi Trading Co., Ltd.
Product
Rupatadine fumarate 158876-82-5
Price
US $1.00/Kg
Min. Order
1 kg/barrel
Purity
99%
Supply Ability
500KG
Release date
2019-04-15

158876-82-5, RupatadineRelated Search:


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