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Olopatadine hydrochloride

Product Name
Olopatadine hydrochloride
CAS No.
140462-76-6
Chemical Name
Olopatadine hydrochloride
Synonyms
OLOPATADINE HCL;Patanol;Olopatadin HCL;OLAPATADINE HCL;Olopatadine Hydrochlorde;ALO4943A;AL-4943A;Opatanol;OLOPATDINEHYDROCHLORIDE;Olatadine hydrochloride
CBNumber
CB0144403
Molecular Formula
C21H24ClNO3
Formula Weight
373.88
MOL File
140462-76-6.mol
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Olopatadine hydrochloride Property

Melting point:
242-245?C
storage temp. 
Inert atmosphere,Room Temperature
solubility 
H2O: ≥20mg/mL
form 
solid
color 
White to Light yellow
Merck 
14,6840
BCS Class
3(CLogP), 1 (LogP)
InChI
InChI=1S/C21H23NO3.ClH/c1-22(2)11-5-8-18-17-7-4-3-6-16(17)14-25-20-10-9-15(12-19(18)20)13-21(23)24;/h3-4,6-10,12H,5,11,13-14H2,1-2H3,(H,23,24);1H/b18-8-;
InChIKey
HVRLZEKDTUEKQH-NOILCQHBSA-N
SMILES
C(=C1/C2=CC=CC=C2COC2C=CC(CC(=O)O)=CC/1=2)\CCN(C)C.Cl
CAS DataBase Reference
140462-76-6(CAS DataBase Reference)
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Safety

Hazard Codes 
T,N
Risk Statements 
25-50
Safety Statements 
45-61
RIDADR 
UN 2811 6.1 / PGIII
WGK Germany 
3
RTECS 
HQ4135060
HS Code 
29329990
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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Danger
Hazard statements

H301Toxic if swalloed

H400Very toxic to aquatic life

Precautionary statements

P273Avoid release to the environment.

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N-Bromosuccinimide Price

Sigma-Aldrich
Product number
O0391
Product name
Olopatadine hydrochloride
Purity
≥98% (HPLC)
Packaging
10mg
Price
$86
Updated
2024/03/01
Sigma-Aldrich
Product number
1478403
Product name
Olopatadine hydrochloride
Purity
United States Pharmacopeia (USP) Reference Standard
Packaging
150mg
Price
$598
Updated
2024/03/01
TCI Chemical
Product number
O0361
Product name
Olopatadine Hydrochloride
Purity
>98.0%(HPLC)(T)
Packaging
1g
Price
$284
Updated
2024/03/01
Cayman Chemical
Product number
11999
Product name
Olopatadine (hydrochloride)
Purity
≥98%
Packaging
10mg
Price
$37
Updated
2024/03/01
Cayman Chemical
Product number
11999
Product name
Olopatadine (hydrochloride)
Purity
≥98%
Packaging
25mg
Price
$81
Updated
2024/03/01
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Olopatadine hydrochloride Chemical Properties,Usage,Production

Description

Olopatadine hydrochloride is an ophthalmic antihistamine that inhibits release of histamine from mast cells and is a relatively selective histamine H1 antagonist. It inhibits type 1 immediate hypersensitivity reactions. Olopatadine hydrochloride is indicated in the temporary relief of itching caused by allergic conjunctivitis. H1 antagonists have an established and valued place in the symptomatic treatment of various immediate hypersensitivity reactions. In addition, the central properties of some of the series are of therapeutic value for suppressing motion sickness or for sedation.

Chemical Properties

White Solid

Originator

Kyowa Hakko (Japan)

Uses

Dual acting histamine H1-receptor antagonist and mast cell stabilizer. Antiallergic; antihistaminic.

Uses

Olopatadine hydrochloride is a potent, selective antagonist of the H1 histamine receptor (Ki = 16-41.1 nM), with much lower affinities for the H2 and H3 receptors (Ki = 43.4 and 172 μM, respectively). It blocks histamine-induced phosphoinositide turnover in isolated cells (IC50 = 9.5-39.9 nM) and prevents passive cutaneous anaphylaxis in rats (ED50 = 49 μg/kg) and anaphylactic bronchoconstriction in guinea pigs (ID50 = 30 μg/kg). Olopatadine is effective in treating allergic rhinitis and conjunctivitis. It also suppresses itch in patients with well-controlled chronic urticaria. In humans, this antihistamine does not cause cognitive or psychomotor impairment at therapeutic doses.[Cayman Chemical]

Preparation

Olopatadine hydrochloride can be prepared in five steps from the sodium salt of phydroxyphenylacetic acid methyl ester with phthalide.

Definition

ChEBI: Olopatadine hydrochloride is a dibenzooxazepine.

brand name

Patanol (Alcon).

Pharmacokinetics

Olopatadine hydrochloride was launched in the US for use in allergic conjunctivitis. It has a fast onset of action with a long duration of action (due to slow dissociation kinetics) that combines the ability to prevent human conjunctival mast cell mediator release with selective H1-receptor antangonistic activity (greater H3:H1 selectivity than H2:H1 selectivity). In addition, Olopatadine hydrochloride had no inhibition of 5-lipoxygenase, PAF acetyltransferase and thromboxane synthase while interfering with phospholipase A2. It has a presynaptic inhibition of tachykinin release and inhibits bronchial sensory nerves through activation of small conductance calcium activated potassium channels. It was more potent than ketotifen and terfenadine and was effective at inhibition of PAF, LTC4 induced conjunctivitis and TXB2 production. It does not accumulate in the CNS, has a low affinity for H1-receptors in the brain, and significantly inhibits allergen induce sneezing. Olopatadine hydrochloride was more effective in conjuctival than in corneal or the trabecuiar meshwork cells.

Veterinary Drugs and Treatments

Olopatadine HCl is a selective H1 receptor antagonist and inhibitor of histamine release from mast cells. It is marketed for topical use to alleviate symptoms of allergic conjunctivitis in humans and is thought to be safe for use in children three years of age and older. Olopatadine, upon topical application in humans, was shown to have very limited systemic absorption. It was detectable in the milk of nursing rats, after topical application, and like most medications should be avoided in pregnant or nursing animals.

storage

Desiccate at RT

Olopatadine hydrochloride Preparation Products And Raw materials

Raw materials

Preparation Products

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Olopatadine hydrochloride Suppliers

Qingdao Kingway Pharmtech Co.,Ltd.
Tel
0532-87118899 13918827946
Email
m.xiaoyan@kingwaypharm.com
Country
China
ProdList
69
Advantage
58
Cangzhou Weizhidamei Pharmaceutical Co., Ltd.
Tel
13426038769 13426038769
Fax
0317-5486999
Email
askmryu@163.com
Country
China
ProdList
59
Advantage
58
Shandong Mingfeng Pharmaceutical and Technology Co. Ltd
Tel
-1345456643 15315114555
Fax
QQ:1345456643
Email
1345456643@qq.com
Country
China
ProdList
248
Advantage
58
Beijing Lianben Pharm-Chemicals Tech. Co.,Ltd
Tel
010-83386559 18810831598
Fax
010-83386758
Email
sales@lianben.com
Country
China
ProdList
92
Advantage
58
Jinan Lide Pharmaceutical Technology Co., Ltd.
Tel
0531-68654990 18560195202
Fax
053168654990
Email
leadgxm@leadchem.net
Country
China
ProdList
153
Advantage
58
HANGZHOU KELAI BIOMEDICAL TECHNOLOGY Co., Ltd.
Tel
18957050573
Email
752803249@qq.com
Country
China
ProdList
248
Advantage
58
J & K SCIENTIFIC LTD.
Tel
010-82848833 400-666-7788
Fax
86-10-82849933
Email
jkinfo@jkchemical.com
Country
China
ProdList
96815
Advantage
76
Meryer (Shanghai) Chemical Technology Co., Ltd.
Tel
4006608290; 18621169109
Fax
86-21-61259102
Email
market03@meryer.com
Country
China
ProdList
40241
Advantage
62
Chembest Research Laboratories Limited
Tel
021-20908456
Fax
021-58180499
Email
sales@BioChemBest.com
Country
China
ProdList
6013
Advantage
61
TCI (Shanghai) Development Co., Ltd.
Tel
021-67121386
Fax
021-67121385
Email
Sales-CN@TCIchemicals.com
Country
China
ProdList
24539
Advantage
81
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View Lastest Price from Olopatadine hydrochloride manufacturers

Shanghai Affida new material science and technology center
Product
Olopatadine hydrochloride 140462-76-6
Price
US $0.00-0.00/KG
Min. Order
1KG
Purity
99
Supply Ability
10 tons
Release date
2024-03-18
WUHAN CIRCLE POWDER TECHNOLOGY CO.,LTD
Product
Olopatadine hydrochloride 140462-76-6
Price
US $0.00/KG
Min. Order
100g
Purity
98%+
Supply Ability
100kg
Release date
2020-11-24
Hebei Duling International Trade Co. LTD
Product
Olopatadine hydrochloride 140462-76-6
Price
US $50.00/kg
Min. Order
1kg
Purity
99%
Supply Ability
1
Release date
2022-10-18

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