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Rupatadine

CAS No.
158876-82-5
Chemical Name:
Rupatadine
Synonyms
Rupax;Rupafi;Rupafin;Pafinur;Rinialer;UR-12592;RUPATADINE;ROPATADINE;Rupatidine;Alergoliber
CBNumber:
CB1346639
Molecular Formula:
C26H26ClN3
Molecular Weight:
415.96
MDL Number:
MFCD09039284
MOL File:
158876-82-5.mol
Last updated:2023-08-14 13:33:12

Rupatadine Properties

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)
FDA UNII 2AE8M83G3E

SAFETY

Risk and Safety Statements

Symbol(GHS)  GHS hazard pictograms
GHS07
Signal word  Warning
Hazard statements  H302-H413
Precautionary statements  P301+P312+P330

Rupatadine price More Price(6)

Manufacturer Product number Product description CAS number Packaging Price Updated Buy
Matrix Scientific 093670 8-Chloro-11-(1-((5-methylpyridin-3-yl)methyl)piperidin-4-ylidene)-6,11-dihydro-5H-benzo[5,6]cyclohepta[1,2-b]pyridine 95+% 158876-82-5 250mg $120 2021-12-16 Buy
Matrix Scientific 093670 8-Chloro-11-(1-((5-methylpyridin-3-yl)methyl)piperidin-4-ylidene)-6,11-dihydro-5H-benzo[5,6]cyclohepta[1,2-b]pyridine 95+% 158876-82-5 1g $299 2021-12-16 Buy
American Custom Chemicals Corporation API0004113 RUPATADINE 95.00% 158876-82-5 1G $975.45 2021-12-16 Buy
American Custom Chemicals Corporation API0004113 RUPATADINE 95.00% 158876-82-5 2.5G $2277.8 2021-12-16 Buy
American Custom Chemicals Corporation API0004113 RUPATADINE 95.00% 158876-82-5 5G $4305 2021-12-16 Buy
Product number Packaging Price Buy
093670 250mg $120 Buy
093670 1g $299 Buy
API0004113 1G $975.45 Buy
API0004113 2.5G $2277.8 Buy
API0004113 5G $4305 Buy

Rupatadine Chemical Properties,Uses,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

Global( 165)Suppliers
Supplier Tel Email Country ProdList Advantage
Henan Bao Enluo International TradeCo.,LTD
+86-17331933971 +86-17331933971 deasea125996@gmail.com China 2472 58
Henan Tianfu Chemical Co.,Ltd.
+86-0371-55170693 +86-19937530512 info@tianfuchem.com China 21634 55
Chembon Pharmaceutical Co., Ltd.
+86-28-8425-2981 CHINA 722 55
career henan chemical co
+86-0371-86658258 +8613203830695 sales@coreychem.com China 29880 58
Hubei Jusheng Technology Co.,Ltd.
18871490254 linda@hubeijusheng.com CHINA 28172 58
Hebei Jimi Trading Co., Ltd.
+86 319 5273535 bestoneforyou@sina.com CHINA 287 58
Chongqing Chemdad Co., Ltd
+86-023-6139-8061 +86-86-13650506873 sales@chemdad.com China 39894 58
Alchem Pharmtech,Inc.
8485655694 sales@alchempharmtech.com United States 63687 58
CONIER CHEM AND PHARMA LIMITED
+8618523575427 sales@conier.com China 49374 58
Nanjing Shizhou Biotechnology Co., Ltd
+86-15850508050 +86-15850508050 sean.lv@synzest.com China 323 58

View Lastest Price from Rupatadine manufacturers

Image Update time Product Price Min. Order Purity Supply Ability Manufacturer
Rupatadine pictures 2023-08-14 Rupatadine
158876-82-5
US $100.00 / kg 1kg 99% 1000tons Henan Bao Enluo International TradeCo.,LTD
Rupatadine fumarate pictures 2019-07-06 Rupatadine fumarate
158876-82-5
US $100.00 / KG 1KG 98% 10KG,20KG Career Henan Chemical Co
Rupatadine fumarate pictures 2019-05-22 Rupatadine fumarate
158876-82-5
US $1.00 / Kg 1 kg/barrel 99% 500KG Hebei Jimi Trading Co., Ltd.
  • Rupatadine pictures
  • Rupatadine
    158876-82-5
  • US $100.00 / kg
  • 99%
  • Henan Bao Enluo International TradeCo.,LTD
8-chloro-6,11-dihydro-11-[1-[(5-methyl-3-pyridyl)methyl]-4-piperidylidene]-5h-benzo[5,6]cyclohepta[1,2-b]pyridine 8-Chloro-6,11-dihydro-11-[1-[(5-methyl-3-pyridinyl)methyl]-4-piperidinylidene]- 5H-benzo[5,6]cyclohepta[1,2-b]pyridine (2E)-2-Butenedioate Rupafi RUPATADINEFUMARATE(FORR&DONLY) RUPATADINE FREE BASE 8-Chloro-6,11-dihydro-11-[1-[(5-methyl-3-pyridinyl)methyl]-4-piperidinylidene]- 5H-benzo[5,6]cyclohepta[1,2-β]pyridine (2E)-2-Butenedioate Rupafin Rupatadine fumarate 5H-Benzo(5,6)cyclohepta(1,2-B)pyridine, 8-chloro-6,11-dihydro-11-(1-((5-methyl-3-pyridinyl)methyl)-4-piperidinylidene)- Unii-2ae8m83G3e Rupatidine FuMerate Alergoliber Pafinur Rinialer Rupax 8-Chloro-11-(1-((5-methylpyridin-3-yl)methyl)piperidin-4-ylidene)-6,11-dihydro-5H-benzo[5,6]cyclo Rupatadine fuMerate 8-Chloro-11-(1-((5-Methylpyridin-3-yl)Methyl)piperidin-4-ylidene)-6,11-dihydro-5H-benzo[5,6]cyclohepta[1,2-b]pyridine UR-12592 8-Chloro-11-(1-((5-methylpyridin-3-yl)methyl)piperidin-4-ylidene)-6,11-dihydro-5H-benzo[5,6]cy RUPATADINE 8-chloro-11-[1-[(5-methylpyridin-3-yl)methyl]piperidin-4-ylidene]-5,6-dihydrobenzo[1,2]cyclohepta[2,4-b]pyridine 8-Chloro-6,11-dihydro-11-[1-[(5-methyl-3-pyridinyl)methyl]-4-piperidinylidene]-5H-benzo[5,6]cyclohepta[1,2-b]pyridine ROPATADINE Rupatidine Rupatadine (UR-12592) Lupatadine in methanol 158876-82-5 C30H30ClN3O4 C26H26ClN3C4H4O4 API Heterocyclic Compounds Heterocycles Intermediates & Fine Chemicals Pharmaceuticals Rupatadine Pharmaceutical material and intermeidates APIs