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Details

Stereochemistry ACHIRAL
Molecular Formula C12H9N2O3S.Na
Molecular Weight 284.266
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 1
Charge 0

SHOW SMILES / InChI
Structure of TIACRILAST SODIUM ANHYDROUS

SMILES

[Na+].CSC1=CC2=C(C=C1)N=CN(\C=C\C([O-])=O)C2=O

InChI

InChIKey=MVLGDRIPQBDGOO-FXRZFVDSSA-M
InChI=1S/C12H10N2O3S.Na/c1-18-8-2-3-10-9(6-8)12(17)14(7-13-10)5-4-11(15)16;/h2-7H,1H3,(H,15,16);/q;+1/p-1/b5-4+;

HIDE SMILES / InChI
Tiacrilast (also known as Ro 22-3747) is a quinazolinyl-propenoic acid derivative patented by Hoffmann-La Roche, Inc. as an antihypertensive useful for anaphylaxis management. Tiacrilast acts as a potent mast cell degranulation inhibitor in vitro and inhibits of antigen-induced histamine release from passively sensitized rat peritoneal cells in vitro. In preclinical models, Tiacrilast shows marked activity in rat passive cutaneous anaphylaxis assay, rat anaphylactic bronchospasm assay. In vitro studies have confirmed that the mechanism of action of Tiacrilast in the in vivo models is through allergic mediator release inhibition. Clinical evaluations of Tiacrilast in patients with ragweed sensitive allergic asthma, Tiacrilast demonstrates significant inhibitory activity relative to placebo in reducing acute airway responses to inhaled pollen extracts

Approval Year

PubMed

PubMed

TitleDatePubMed
The pharmacological profile and initial clinical evaluation of tiacrilast (Ro 22-3747): a new antiallergic agent.
1986-06
Patents

Patents

Sample Use Guides

350mg/day
Route of Administration: Oral
Name Type Language
TIACRILAST SODIUM ANHYDROUS
Common Name English
2-PROPENOIC ACID, 3-(6-(METHYLTHIO)-4-OXO-3(4H)-QUINAZOLINYL)-, SODIUM SALT (1:1), (2E)-
Preferred Name English
Code System Code Type Description
CAS
875338-33-3
Created by admin on Mon Mar 31 20:34:58 GMT 2025 , Edited by admin on Mon Mar 31 20:34:58 GMT 2025
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PUBCHEM
23665632
Created by admin on Mon Mar 31 20:34:58 GMT 2025 , Edited by admin on Mon Mar 31 20:34:58 GMT 2025
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EPA CompTox
DTXSID50236377
Created by admin on Mon Mar 31 20:34:58 GMT 2025 , Edited by admin on Mon Mar 31 20:34:58 GMT 2025
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FDA UNII
3FU10ZK1QN
Created by admin on Mon Mar 31 20:34:58 GMT 2025 , Edited by admin on Mon Mar 31 20:34:58 GMT 2025
PRIMARY
SMS_ID
300000055355
Created by admin on Mon Mar 31 20:34:58 GMT 2025 , Edited by admin on Mon Mar 31 20:34:58 GMT 2025
PRIMARY