[CAS NO. 1707147-26-9] THK5351

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PRODUCTS SPECIFICATIONS [1707147-26-9]

Catalog

AS968604

Brand

Arctom Scientific

CAS

1707147-26-9

DESCRIPTION [1707147-26-9]

Overview

MDL	-
Molecular Weight	327.35
Molecular Formula	C18H18FN3O2
SMILES	O[C@@H](COC1=CC=C2N=C(C3=CC=C(NC)N=C3)C=CC2=C1)CF

For research use only. We do not sell to patients.

Summary

THK5351 can be radiolabeled and used as a radiotracer for in vivo imaging of tau pathology in the brain.

In Vitro

Aggregated tau protein is a major neuropathological substrate central to the pathophysiology of neurodegenerative diseases such as Alzheimer's disease (AD). ¹⁸ F-THK5351 binds to Alzheimer disease hippocampal homogenates with high affinity (K _d =2.9 nM; maximum number of binding sites=368.3 pmol/g tissue). It has fast dissociation from white-matter tissue. The THK5351 binding amount correlates with the amount of tau deposits in tissue ^[1] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

THK5351 exhibits favorable pharmacokinetics and no defluorination in mice. ¹⁸ F-THK5351 enters the brain immediately after intravenous injection and shows a fast washout from the brain. At 0.1 and 1 mg/kg, no animals died and no treatment-related changes in any animal are noted in clinical observations, body weight measurement, and pathologic examination ^[1] . Autoradiography in the brain sections of patients with PSP demonstrates [ ³ H]THK-5351 binding to tau deposits with a high selectivity. Although patients with PSP exhibits no remarkable [ ¹⁸ F]THK-5351 retention in the temporal cortex, significantly higher tracer retention is observed in the globus pallidus and midbrain ^[2] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase
NCT04318626	Chang Gung Memorial Hospital	Post-stroke Cognitive Impairment\|Neuroinflammation	November 1, 2020	Phase 2
NCT03430869	Chang Gung Memorial Hospital	Major Depressive Disorder	March 23, 2018	Phase 2
NCT02884492	William Charles Kreisl\|National Institute on Aging (NIA)\|Columbia University	Alzheimer´s Disease	July 2016	Phase 2
NCT04588649	Chang Gung Memorial Hospital	Post-stroke Dementia\|Vascular Mild Cognitive Impairment	January 4, 2016	Phase 2
NCT02686216	Chang Gung Memorial Hospital	Alzheimer´s Disease	December 2015	Phase 1
NCT03024944	Columbia University\|National Institute on Aging (NIA)	Diabetes Mellitus\|Alzheimer Dementia	December 2017	Phase 2

Appearance

Solid

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : 50 mg/mL ( 152.74 mM ; Need ultrasonic)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	3.0548 mL	15.2742 mL	30.5483 mL
5 mM	0.6110 mL	3.0548 mL	6.1097 mL
10 mM	0.3055 mL	1.5274 mL	3.0548 mL

* Please refer to the solubility information to select the appropriate solvent.

In Vivo:

1.

Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

Solubility: ≥ 2.5 mg/mL (7.64 mM); Clear solution
2.

Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)

Solubility: ≥ 2.5 mg/mL (7.64 mM); Clear solution
3.

Add each solvent one by one: 10% DMSO >> 90% corn oil

Solubility: ≥ 2.5 mg/mL (7.64 mM); Clear solution

* All of the co-solvents are available by MCE.