JNJ-64326067
JNJ-64326067 is an aggregated tau-binding agent with blood-brain barrier permeability, with a Ki of 2.4 nM. JNJ-64326067 selectively binds to aggregated tau protein but does not bind to aggregated β-amyloid protein, and shows no significant off-target binding to the tested receptors, ion channels, transporters, kinases or monoamine oxidases. JNJ-64326067 is applicable to the research of Alzheimer's disease.
For research use only. We do not sell to patients.
- CAS No.: 2173357-28-1
- Formula: C15H12FN3
- Molecular Weight:253.28
-
Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biological Activity
-
Chemical Information
- Purity & Documentation
- References
-
Help & FAQs
Biological Activity
[3H]JNJ-64326067 and [18F]JNJ-64326067 specifically bind to tau pathologies in post-mortem human AD brain sections, but do not bind to pathologies with only Aβ present, and this binding can be selectively blocked by non-radioactive JNJ-64326067[1].
JNJ-64326067 possesses physicochemical properties suitable for central nervous system penetration, exhibits no significant MDR1-mediated efflux, has a low free fraction in plasma and brain tissue, and shows high intrinsic clearance in rat, monkey and human liver microsomes as well as hepatocytes[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| Species | Dose | Route | CL | T1/2 | AUC | Vdss |
|---|---|---|---|---|---|---|
| Rat[1] | 0.03 mg/kg | i.v. | 228 mL/min/kg | 0.08 h | 2.2 ng·h/mL | 1.6 L/kg |
JNJ-64326067 (1-10 mg/kg; s.c.; i.v.; single dose) shows high initial brain uptake, rapid washout, and no detectable off-target binding in healthy female Wistar rats, with bone uptake indicating in vivo defluorination[1].
JNJ-64326067 (1 mg/kg; i.v.; single dose; simultaneous with [18F]9 injection) exhibits high brain uptake, rapid washout, homogeneous brain distribution, and no bone uptake in healthy male rhesus monkeys, with a blocking study showing increased peak uptake due to enhanced tracer availability for brain entry[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:Sprague-Dawley (male)[1]
-
Dosage:0.03 mg/kg
-
Administration:i.v.; single dose
-
Result:Exhibited a plasma clearance of 228 mL/min/kg.
Showed a plasma half-life of 0.08 h.
Reached a plasma AUC of 2.2 ng·h/mL.
Reached a cortex AUC of 8.72 ng·h/mL.
Had a volume of distribution at steady state (Vd,ss) of 1.6 L/kg.
Achieved a cortex-to-plasma ratio (Kp) of 4.0.
Had an estimated unbound brain-to-plasma ratio (Kp,uu) of 1.1.
-
Animal Model:Wistar (female)[1]
-
Dosage:10 mg/kg (pretreatment); 1 mg/kg (displacement)
-
Administration:s.c.; single dose, 60 minutes pre [18F]9 injection; i.v.; single dose, 30 minutes post [18F]9 injection
-
Result:Showed high initial brain uptake (SUV of 2.4 at 1 minute post-injection).
Underwent rapid brain washout (SUV of 0.2 at 60 minutes post-injection).
Did not reduce time-activity curve intensity with pretreatment and displacement, indicating no reversible or irreversible off-target specific binding.
Caused bone uptake at later time points, suggesting in vivo defluorination.
-
Animal Model:male[1]
-
Dosage:1 mg/kg
-
Administration:i.v.; single dose; simultaneous with [18F]9 injection
-
Result:Showed high brain uptake (SUV of 5.4 in whole brain, time to peak uptake: 4.5 minutes) with rapid washout.
Had homogeneous distribution across brain regions, with lower uptake in the corpus callosum and skull.
Showed no bone uptake up to 120 minutes post-injection.
Had a higher peak whole brain SUV of 7.5 in blocking study, with shorter time to peak (3.5 minutes) and slightly faster washout, and no pronounced blocking effect was observed.
Chemical Information
-
CAS No. 2173357-28-1
-
Molecular Weight 253.28
-
Formula C15H12FN3
-
SMILES
FC1=CC(=NC=C1C)NC=2C=CC=3C=NC=CC3C2
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
JNJ-64326067 Related Classifications
HY-W569115 Related Classifications
Powered by Bioz