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| ln Vitro |
[3H]JNJ-64326067 and [18F]JNJ-64326067 can specifically bind to tau protein lesions in post-mortem human Alzheimer's disease (AD) brain tissue sections, but cannot bind to lesions containing only Aβ, and this binding can be selectively blocked by non-radioactive JNJ-64326067 [1]. JNJ-64326067 has physicochemical properties suitable for central nervous system penetration, no obvious MDR1-mediated efflux, low free concentrations in plasma and brain tissue, and high intrinsic clearance rates in rat, monkey, and human liver microsomes and hepatocytes [1].
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| ln Vivo |
JNJ-64326067 (0.03 mg/kg; intravenous; single dose) showed rapid plasma clearance, short plasma half-life and good brain exposure in healthy male Sprague-Dawley rats with a cortex/plasma ratio of 4.0[1]. JNJ-64326067 (1–10 mg/kg; subcutaneous; intravenous; single dose) showed high initial brain uptake, rapid clearance and no off-target binding in healthy female Wistar rats, with bone uptake indicating defluorination in vivo[1]. JNJ-64326067 (1 mg/kg; intravenous; single dose; co-administered with [18F]9) showed high brain uptake, rapid clearance and uniform brain distribution in healthy male rhesus monkeys, with no bone uptake, and blocking studies showed increased peak uptake due to enhanced availability of the tracer into brain tissue[1].
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| Animal Protocol |
Animal/Disease Models:Sprague-Dawley mice (male) [1]
Doses: 0.03 mg/kg Route of Administration: Intravenous injection; single dose Experimental Results: Plasma clearance was 228 mL/min/kg. Plasma half-life was 0.08 h. Plasma AUC was 2.2 ng·h/mL. Cortical AUC was 8.72 ng·h/mL. Steady-state volume of distribution (Vd, ss) was 1.6 L/kg. Cortical/plasma ratio (Kp) was 4.0. Estimated free brain/plasma ratio (Kp, uu) was 1.1. Animal/Disease Models:Wistar (female) [1] Doses: 10 mg/kg (pretreatment); 1 mg/kg (replacement) Route of Administration: Subcutaneous injection; single dose, 60 minutes before injection of [18F]9; intravenous injection; single dose, 30 minutes after injection of [18F]9 Experimental Results: High initial brain uptake (SUV 2.4 1 minute after injection). Rapid clearance of the drug from the brain (SUV 0.2 60 minutes after injection). Neither pretreatment nor replacement reduced the intensity of the time-activity curve, indicating no reversible or irreversible off-target specific binding. Bone uptake was induced at later time points, suggesting the presence of defluorination in vivo. Animal/Disease Models:Male [1] Doses: 1 mg/kg< Route of Administration: Intravenous injection; single dose; simultaneous injection with [18F]9 Experimental Results: High brain uptake was observed (whole-brain SUV 5.4, time to peak: 4.5 min), and rapid clearance was observed. The drug was evenly distributed in the brain regions, with lower uptake in the corpus callosum and skull. No bone uptake was observed within 120 minutes after injection. In the blocking experiment, the whole-brain SUV peak was higher (7.5), the time to peak was shorter (3.5 min), the clearance rate was slightly faster, and no obvious blocking effect was observed. |
| References |
| Molecular Formula |
C15H12FN3
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|---|---|
| Molecular Weight |
253.28
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| CAS # |
2173357-28-1
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| Appearance |
Typically exists as solids at room temperature
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| SMILES |
FC1=CC(=NC=C1C)NC=2C=CC=3C=NC=CC3C2
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.9482 mL | 19.7410 mL | 39.4820 mL | |
| 5 mM | 0.7896 mL | 3.9482 mL | 7.8964 mL | |
| 10 mM | 0.3948 mL | 1.9741 mL | 3.9482 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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