FLORTAUCIPIR F-18

Details

Stereochemistry	ACHIRAL
Molecular Formula	C16H10FN3
Molecular Weight	262.2716
Optical Activity	UNSPECIFIED
Defined Stereocenters	0 / 0
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

[18F]C1=CC=C(C=N1)C2=CC=C3C(NC4=C3C=NC=C4)=C2

InChI

InChIKey=GETAAWDSFUCLBS-SJPDSGJFSA-N

InChI=1S/C16H10FN3/c17-16-4-2-11(8-19-16)10-1-3-12-13-9-18-6-5-14(13)20-15(12)7-10/h1-9,20H/i17-1

HIDE SMILES / InChI

Molecular Formula	C16H10FN3
Molecular Weight	262.2716
Charge	0
Count

Stereochemistry	ACHIRAL
Additional Stereochemistry
Defined Stereocenters	0 / 0
E/Z Centers	0
Optical Activity	NONE

Description

Flortaucipir (18F-AV-1451, also known as 18F-T807) is a highly selective positron emission tomography (PET) imaging agent targeting paired helical filament (PHF)-tau in the brain. This tracer is studying for clinical assessment in patients with various tauopathies, including Alzheimer's disease, as well as in healthy subjects.

CNS Activity

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
Microtubule-associated protein tau 4	Binding Agent 965	Alzheimer's Disease	14.6 nM [Kd]

Conditions

Condition	Modality	Targets	Highest Phase	Product
Alzheimer's Disease 149	Diagnostic	Microtubule-associated protein tau	Phase III 636

PubMed

Title	Date	PubMed
[(18)F]T807, a novel tau positron emission tomography imaging agent for Alzheimer's disease.	2013 Nov	23411393
Synthesis and quality control of [(18) F]T807 for tau PET imaging.	2016 Aug	27427174
Kinetics of the Tau PET Tracer 18F-AV-1451 (T807) in Subjects with Normal Cognitive Function, Mild Cognitive Impairment, and Alzheimer Disease.	2016 Oct	27151986
Tau-PET Binding Distinguishes Patients With Early-stage Posterior Cortical Atrophy From Amnestic Alzheimer Disease Dementia.	2017 Apr-Jun	28394771
Quantification of Tau Load Using [¹⁸F]AV1451 PET.	2017 Dec	28374171
Region-Specific Association of Subjective Cognitive Decline With Tauopathy Independent of Global β-Amyloid Burden.	2017 Dec 1	28973551
Tau PET imaging: present and future directions.	2017 Feb 20	28219440
Hierarchical Organization of Tau and Amyloid Deposits in the Cerebral Cortex.	2017 Jul 1	28558094
Relationships between flortaucipir PET tau binding and amyloid burden, clinical diagnosis, age and cognition.	2017 Mar 1	28077397
¹⁸ F-flortaucipir tau positron emission tomography distinguishes established progressive supranuclear palsy from controls and Parkinson disease: A multicenter study.	2017 Oct	28980714
¹⁸F-Flortaucipir PET/MRI Correlations in Nonamnestic and Amnestic Variants of Alzheimer Disease.	2018 Feb	28747523

Patents

Sample Use Guides

In Vivo Use Guide

Flortaucipir PET images were acquired for 20 min, as four 5-min frames, beginning 80 min after injection of 370 MBq flortaucipir. On a separate day, subjects underwent a florbetapir PET scan for 10 min, as two 5-min frames, beginning 50 min after injection of 370 MBq florbetapir F18.

Route of Administration: Parenteral

Substance Class	Chemical Created by `admin` on `Mon Oct 21 22:49:52 UTC 2019` Edited by `admin` on `Mon Oct 21 22:49:52 UTC 2019`
Record UNII	T1JP1KYU9O
Record Status	`Validated (UNII)`
Record Version

Download

Name

Type

Language

FLORTAUCIPIR F-18

Common Name

English

FLORTAUCIPIR F 18

Official Name

English

LY3191748

Code

English

7-(6-(F-18)FLUOROPYRIDIN-3-YL)-5H-PYRIDO(4,3-B)INDOLE

Common Name

English

T807 F-18

Code

English

FLORTAUCIPIR F 18 [USAN]

Common Name

English

(F-18)T807

Code

English

AV-1451 F-18

Code

English

18F-AV-1451

Code

English

FLORTAUCIPIR (18F) [INN]

Common Name

English

T-807 F-18

Code

English

FLORTAUCIPIR (18F) [WHO-DD]

Common Name

English

FLORTAUCIPIR (18F)

Official Name

English

LY-3191748

Code

English

Code System Code Type Description

PUBCHEM

70957463

Created by admin on Mon Oct 21 22:49:52 UTC 2019 , Edited by admin on Mon Oct 21 22:49:52 UTC 2019

PRIMARY

CAS

1522051-90-6

Created by admin on Mon Oct 21 22:49:52 UTC 2019 , Edited by admin on Mon Oct 21 22:49:52 UTC 2019

PRIMARY

INN

10203

Created by admin on Mon Oct 21 22:49:52 UTC 2019 , Edited by admin on Mon Oct 21 22:49:52 UTC 2019

PRIMARY

ChEMBL

CHEMBL3546271

Created by admin on Mon Oct 21 22:49:52 UTC 2019 , Edited by admin on Mon Oct 21 22:49:52 UTC 2019

PRIMARY

Related Record Type Details


					QR9EFE0TG6

MICROTUBULE-ASSOCIATED PROTEIN TAU (PAIRED HELICAL FILAMENTS (PHF))

TARGET->RADIOLIGAND

Comments:

Images aggregates

Related Record Type Details


					T1JP1KYU9O

FLORTAUCIPIR F-18

ACTIVE MOIETY