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14976-57-9 (Clemastine (fumarate))

1

Identification

Clemastine (fumarate) Clemastine (fumarate)
Name Clemastine (fumarate)
Formula C25H30ClNO5
MW 459.96
CAS No. 14976-57-9
EINECS 239-055-2
Smiles C[[email protected]](C1=CC=CC=C1)(OCC[[email protected]@H]2N(C)CCC2)C3=CC=C(Cl)C=C3.OC(/C=C/C(O)=O)=O
Synonyms (2R)-2-[2-[(1R)-1-(4-Chlorophenyl)-1-phenylethoxy]ethyl]-1-methylpyrrolidine but-2-enedioic acid; (R)-2-(2-((R)-1-(4-chlorophenyl)-1-phenylethoxy)ethyl)-1-methylpyrrolidine fumarate
InChI InChI=1S/C21H26ClNO.C4H4O4/c1-21(17-7-4-3-5-8-17,18-10-12-19(22)13-11-18)24-16-14-20-9-6-15-23(20)2;5-3(6)1-2-4(7)8/h3-5,7-8,10-13,20H,6,9,14-16H2,1-2H3;1-2H,(H,5,6)(H,7,8)/b;2-1+/t20-,21-;/m1./s1
2

Introduction

Clemastine Fumarate is a selective histamine H1 receptor antagonist with IC50 of 3 nM. Target: Histamine H1 Receptor Clemastine Fumarate inhibits histamine induced rise in [Ca2+]i in HL-60 cells with an IC50 of 3 nM as compared with that of chlorpheniramine or diphenhydramine with IC50 values of 20 nM and 100 nM, respectively [1].

Background Information

Clemastine fumarate, a histamine H1 antagonist used as the hydrogen fumarate in hay fever, rhinitis, allergic skin conditions, and pruritus. It causes drowsiness. Clemastine is a selective histamine H1 antagonist and binds to the histamine H1 receptor. This blocks the action of endogenous histamine, which subsequently leads to temporary relief of the negative symptoms brought on by histamine. ......by AbMole BioScience
Clemastine is a selective histamine H1 antagonist. It binds to the histamine H1 receptor, thus blocking the action of endogenous histamine, which leads to temporary relief of the negative symptoms caused by histamine. ......by AdooQ BioScience, LLC
Clemastine Fumarate (Clemastine) is a selective histamine H1 receptor antagonist with IC50 of 3 nM. ......by BOC Sciences
Clemastine fumarate is a histamine H1 antagonist used as the hydrogen fumarate in hay fever, rhinitis, allergic skin conditions, and pruritus. Clemastine fumarate blocks the H1 histamine receptor and prevents the symptoms that are caused by histamine activity on capillaries, bronchial and gastrointestinal smooth muscles, including vasodilation, increased capillary permeability, bronchoconstriction, and spasmodic contraction of gastrointestinal smooth muscles. It may cause cause drowsiness. This drug also prevents histamine-induced pain and itching of mucous membranes. ......by MedKoo Biosciences, Inc.
Clemastine Fumarate (Clemastine) is a selective histamine H1 receptor antagonist with IC50 of 3 nM. ......by Selleck Chemicals LLC
A histamine H1 antagonist used as the hydrogen fumarate in hay fever, rhinitis, allergic skin conditions, and pruritus. It causes drowsiness. ......by Target Molecule Corp.
H1-receptor antagonist. Clinically-used antihistamine. ......by Tocris Bioscience Inc.
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Protocol(Only for Reference)

Cell Experiment

Animal Experiment

Animal Models Male Wistar rats with paw oedema induced by subplantar injection of zymosan and ear oedema induced by croton oil
Dosage 5-20 mg/kg
Formulation Dissolved in saline
Administration Intraperitoneally
Source Selleck Chemicals LLC
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Physical and Chemical Properties

Appearance:Light yellow to yellow Liquid EBNumber:EB000012573

Storage condition

Store at RT by Tocris Bioscience Inc.

Solubility

DMSO 35 mg/mL; Water <1 mg/mL by MedChemexpress Co., Ltd.
(25°C) * In vitro DMSO 35 mg/mL warming (76.09 mM); Water<1 mg/mL (<1 mM); Ethanol<1 mg/mL (<1 mM); In vivo 30% Propylene glycol, 5% Tween 80, 65% D5W5 mg/mL by Selleck Chemicals LLC
Soluble to 50 mM in DMSO by Tocris Bioscience Inc.
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Mechanism and Indication

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Clinical Information

Product Name Sponsor & Collaborators Indications Start Date End Date Phase
Clemastine (fumarate) - Launched
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Safety Data of Clemastine (fumarate)

RTECS : UY0704600
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Spectral Information

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Suppliers List

Company Price and Availability Country/Region
AbMole BioScience USA
AdooQ BioScience, LLC USA
Apexbio Technology LLC USA
Ark Pharm, Inc. USA
BOC Sciences
Biochempartner Co., Ltd China
CHEMSCENE, LLC 100mg/USD60();200mg/USD96() USA
Cayman Chemical Company USA
Jinan Chuancheng Pharmaceutical Co., Ltd. China
MedChemexpress Co., Ltd. 100mg/USD60();200mg/USD96() USA
MedKoo Biosciences, Inc. USA
Pure Chemistry Scientific Inc. 1g/USD18(In stock) USA
Selleck Chemicals LLC 50mg/USD97(In stock);10mM/1mLIn DMSO/USD130(In stock) USA
Shanghai Haoyuan Chemexpress Co., Ltd. 100mg/USD60();200mg/USD96() China
Target Molecule Corp. 2mg/USD20();10mg/USD86();50mg/USD156();100mg/USD254() USA
Tocris Bioscience Inc. USA
Wuhan Fortuna Chemical Co., Ltd. China
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Related Products

Other Forms of 14976-57-9

Name CAS No Formula MW
Clemastine 15686-51-8 C21H26ClNO 343.89

Recommended Compounds in Histamine Receptor Autophagy

Name CAS No Formula MW
Doxylamine (succinate) 562-10-7 C21H28N2O5 388.46
Ebastine 90729-43-4 C32H39NO2 469.66
Azelastine 58581-89-8 C22H24ClN3O 381.9
Epinastine 80012-43-7 C16H15N3 249.31
Hydroxyzine (dihydrochloride) 2192-20-3 C21H29Cl3N2O2 447.83
Hydroxyzine 68-88-2 C21H27ClN2O2 374.9
Desloratadine 100643-71-8 C19H19ClN2 310.82
Pemirolast (potassium) 100299-08-9 C10H7KN6O 266.3
Betahistine (dihydrochloride) 5579-84-0 C8H14Cl2N2 209.12
Brompheniramine (maleate) 980-71-2 C20H23BrN2O4 435.31
Azelastine (hydrochloride) 79307-93-0 C22H25Cl2N3O 418.36
Olopatadine (hydrochloride) 140462-76-6 C21H24ClNO3 373.87
Famotidine 76824-35-6 C8H15N7O2S3 337.45
Meclizine (dihydrochloride) 1104-22-9 C25H29Cl3N2 463.87
Nizatidine 76963-41-2 C12H21N5O2S2 331.46
Roxatidine (Acetate Hydrochloride) 93793-83-0 C19H29ClN2O4 384.9
Diphenhydramine (hydrochloride) 147-24-0 C17H22ClNO 291.82
Chlorpheniramine (maleate) 113-92-8 C20H23ClN2O4 390.86
Ranitidine (hydrochloride) 66357-59-3 C13H23ClN4O3S 350.86
Mianserin (hydrochloride) 21535-47-7 C18H21ClN2 300.83

Recommended Compounds in Same Indication

Name CAS No Formula MW
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Route of Synthesis

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References

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More Information

Clemastine (fumarate)

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