SAFOTIBANT

Details

Stereochemistry	ACHIRAL
Molecular Formula	C25H34N4O5S
Molecular Weight	502.626
Optical Activity	NONE
Defined Stereocenters	0 / 0
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

COC1=CC(C)=C(C(C)=C1)S(=O)(=O)N(C)CCOCC(=O)N(C)CC2=CC=C(C=C2)C3=NCCN3

InChI

InChIKey=AMTQCENHQIDBHQ-UHFFFAOYSA-N

InChI=1S/C25H34N4O5S/c1-18-14-22(33-5)15-19(2)24(18)35(31,32)29(4)12-13-34-17-23(30)28(3)16-20-6-8-21(9-7-20)25-26-10-11-27-25/h6-9,14-15H,10-13,16-17H2,1-5H3,(H,26,27)

HIDE SMILES / InChI

Molecular Formula	C25H34N4O5S
Molecular Weight	502.626
Charge	0
Count

Stereochemistry	ACHIRAL
Additional Stereochemistry	No
Defined Stereocenters	0 / 0
E/Z Centers	0
Optical Activity	NONE

Description
Sources: https://www.ncbi.nlm.nih.gov/pubmed/22470485 | https://adisinsight.springer.com/drugs/800031927

Safotibant (previously known as LF22-0542) was developed as an antagonist at bradykinin B1 receptor for the topical treatment of diabetic macular edema. This drug participated in phase II clinical trials in Australia, in Belgium and in the Czech Republic. However, further, development was discontinued.

Approval Year

PubMed

Title	Date	PubMed
Ocular application of the kinin B1 receptor antagonist LF22-0542 inhibits retinal inflammation and oxidative stress in streptozotocin-diabetic rats.	2012	22470485
Role of kinin B1 and B2 receptors in a rat model of neuropathic pain.	2008-02	18182225
Antinociceptive pharmacology of N-[[4-(4,5-dihydro-1H-imidazol-2-yl)phenyl]methyl]-2-[2-[[(4-methoxy-2,6-dimethylphenyl) sulfonyl]methylamino]ethoxy]-N-methylacetamide, fumarate (LF22-0542), a novel nonpeptidic bradykinin B1 receptor antagonist.	2006-07	16565167

Patents

Substance Class	Chemical Created by `admin` on `Mon Mar 31 20:17:24 GMT 2025` Edited by `admin` on `Mon Mar 31 20:17:24 GMT 2025`
Record UNII	02HU8HWP7U
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

SAFOTIBANT

Official Name

English

LF22-0542

Preferred Name

English

ACETAMIDE, N-((4-(4,5-DIHYDRO-1H-IMIDAZOL-2-YL)PHENYL)METHYL)-2-(2-(((4-METHOXY-2,6-DIMETHYLPHENYL)SULFONYL)METHYLAMINO)ETHOXY)-N-METHYL-

Systematic Name

English

FOV-2304 FREE BASE

Code

English

Safotibant [WHO-DD]

Common Name

English

N-((4-(4,5-DIHYDRO-1H-IMIDAZOL-2-YL)PHENYL)METHYL)-2-(2-(((4-METHOXY-2,6-DIMETHYLPHENYL)SULFONYL)METHYLAMINO)ETHOXY)-N-METHYLACETAMIDE

Systematic Name

English

safotibant [INN]

Common Name

English

LF-22-0542

Common Name

English

N-((4-(4,5-DIHYDRO-1H-IMIDAZOL-2-YL)PHENYL)METHYL)-2-(2-((4-METHOXY-2,6-DIMETHYLBENZENESULFONYL)(METHYL)AMINO)ETHOXY)-N-METHYLACETAMIDE

Systematic Name

English

LF 22-0542

Common Name

English

FOV2304 FREE BASE

Common Name

English

Classification Tree Code System Code

NCI_THESAURUS

C257