THK5351 free base · Synonyms: THK-5351 · THK 5351
THK5351 can be radiolabeled and used as a radiotracer for in vivo imaging of tau pathology in the brain.
For research use only. Not for human or veterinary use.
THK5351 structure
CAS No.: 1707147-26-9
Pack sizes & pricing
| Size | Price | SKU | Stock | |
|---|---|---|---|---|
| 50 mg | USD 620.00 | BP-00013-50mg | In stock | Get quote |
| 100 mg | USD 980.00 | BP-00013-100mg | In stock | Get quote |
| 250 mg | USD 1,980.00 | BP-00013-250mg | In stock | Get quote |
| 500 mg | USD 3,150.00 | BP-00013-500mg | In stock | Get quote |
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Description
THK5351 can be radiolabeled and used as a radiotracer for in vivo imaging of tau pathology in the brain.
Biological activity
In Vitro Aggregated tau protein is a major neuropathological substrate central to the pathophysiology of neurodegenerative diseases such as Alzheimer's disease (AD). 18F-THK5351 binds to Alzheimer disease hippocampal homogenates with high affinity (Kd=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. In Vivo THK5351 exhibits favorable pharmacokinetics and no defluorination in mice. 18F-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 [3H]THK-5351 binding to tau deposits with a high selectivity. Although patients with PSP exhibits no remarkable [18F]THK-5351 retention in the temporal cortex, significantly higher tracer retention is observed in the globus pallidus and midbrain.
Identifiers
- SMILES
-
O(C[C@@H](CF)O)C1=CC2=C(N=C(C=C2)C=3C=CC(NC)=NC3)C=C1 - InChIKey
-
DLVXFZWSPCOWSN-CQSZACIVSA-N
Specifications
- MW (average)
- 327.3528
- Formula
- C18H18FN3O2
- CAS No.
- 1707147-26-9
- Physical state
- Solid
- Color
- Light yellow to yellow
- Shipping
- Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
- Storage
- Powder -20°C, 3 years , 4°C, 2 years; In solvent -20℃ 1 month;
Solubility
Soluble in DMSO : 50 mg/mL