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| Targets |
Nuclear factor of activated T cells (NFAT), a family of transcription factors involved in immune responses, neuronal function, and aging. Q134R is a neuro-protective hydroxyquinoline analogue that inhibits NFAT signaling. By inhibiting NFAT, the compound may modulate the expression of genes involved in inflammation, neurodegeneration, and cellular senescence. Q134R can cross the blood-brain barrier (BBB), making it suitable for central nervous system applications.
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| ln Vitro |
Q134R (1-10 μM) inhibits calcineurin activity but reduces NFAT signaling. In primary rat astrocytes, Q134R partially reduces NFAT activity, but neither in vivo nor in vitro, it stops calcineurin-mediated dephosphorylation of a non-NFAT target[1].
In vitro, Q134R inhibits NFAT signaling. NFAT is a transcription factor that plays important roles in immune responses, neuronal function, and aging. By inhibiting NFAT, Q134R may reduce the expression of pro-inflammatory genes and modulate pathways involved in neurodegeneration and cellular senescence. The compound's neuro-protective properties make it a potential candidate for Alzheimer's disease research. |
| ln Vivo |
In mouse models of AD-like disease, Q134R (4 mg/kg; oral gavage; twice daily; for 7 days) therapy improves cognitive function[1].
In vivo, Q134R can cross the blood-brain barrier (BBB) and may be utilized in the study of Alzheimer's disease and aging-related disorders. The compound's ability to penetrate the CNS and inhibit NFAT signaling suggests potential therapeutic applications in neurodegenerative diseases. However, detailed in vivo efficacy data in animal models of Alzheimer's disease are limited in the available literature. |
| Enzyme Assay |
The in vitro enzyme/receptor binding (cell-free) assay for Q134R is not a typical enzyme inhibition assay, as NFAT is a transcription factor rather than an enzyme. Instead, the compound's activity is assessed in cell-based assays measuring NFAT transcriptional activity. The binding of Q134R to its molecular target could potentially be assessed using biophysical techniques, but such assays are not described in the available literature.
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| Cell Assay |
In vitro cellular assays for Q134R are performed using cells that express NFAT, such as immune cells or neuronal cells. Cells are treated with varying concentrations of Q134R, and NFAT transcriptional activity is assessed using a luciferase reporter assay or by measuring the expression of NFAT target genes by qPCR or Western blotting. The compound's ability to inhibit NFAT signaling is evaluated, and the IC50 is determined from dose-response curves.
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| Animal Protocol |
Animal/Disease Models: APP/PS1 mice (12‐month‐old) injected with oligomeric Aβ (oAβ) peptides[1]
Doses: 4 mg/kg Route of Administration: Orally gavage; twice per day; for 7 days Experimental Results: Led to improved Y maze performance. In vivo animal experiments for Q134R would typically be conducted in rodent models of Alzheimer's disease, such as APP/PS1 transgenic mice or aged animals. The compound would be administered via oral gavage or intraperitoneal injection. Pharmacodynamic endpoints would include the measurement of NFAT target gene expression in brain tissue, assessment of neuroinflammation markers, evaluation of amyloid plaque burden, and behavioral testing to assess cognitive function. |
| ADME/Pharmacokinetics |
Pharmacokinetic data for Q134R are limited. Q134R can cross the blood-brain barrier (BBB), suggesting good CNS penetration. As a small molecule with a molecular weight of 410.39 g/mol and a molecular formula of C22H17F3N4O, the compound is expected to have moderate oral bioavailability and tissue distribution. However, detailed pharmacokinetic parameters such as half-life, Cmax, AUC, and clearance have not been extensively reported.
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| Toxicity/Toxicokinetics |
Toxicology data for Q134R are limited. The compound is used for research purposes only and is not approved for human use. No significant toxicities have been reported in the available literature. As an NFAT inhibitor, the compound may have immunomodulatory effects that could impact immune function. Careful evaluation of safety and potential off-target effects would be required for therapeutic development.
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| References | |
| Additional Infomation |
Q134R (CAS: 2022949-46-6) has a molecular formula of C22H17F3N4O and a molecular weight of 410.39. It is a neuro-protective hydroxyquinoline analogue that inhibits NFAT signaling, can cross the BBB, and may be utilized in the study of Alzheimer's disease and aging-related disorders. The compound is not approved for human use and is intended for research purposes only.
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| Molecular Formula |
C22H17F3N4O
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| Molecular Weight |
410.391794919968
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| Exact Mass |
410.135
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| CAS # |
2022949-46-6
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| PubChem CID |
122604490
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| Appearance |
White to off-white solid powder
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| LogP |
4.9
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
30
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| Complexity |
555
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| Defined Atom Stereocenter Count |
1
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| SMILES |
N1C2C(=CC=C([C@H](NC3=NC=CC(C)=N3)C3=CC=C(C(F)(F)F)C=C3)C=2O)C=CC=1
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| InChi Key |
PFCKQDHXCWWBSM-GOSISDBHSA-N
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| InChi Code |
InChI=1S/C22H17F3N4O/c1-13-10-12-27-21(28-13)29-18(15-4-7-16(8-5-15)22(23,24)25)17-9-6-14-3-2-11-26-19(14)20(17)30/h2-12,18,30H,1H3,(H,27,28,29)/t18-/m1/s1
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| Chemical Name |
7-[(R)-[(4-methylpyrimidin-2-yl)amino]-[4-(trifluoromethyl)phenyl]methyl]quinolin-8-ol
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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) |
DMSO: 100 mg/mL (243.67 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.07 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 2.08 mg/mL (5.07 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (5.07 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.4367 mL | 12.1835 mL | 24.3671 mL | |
| 5 mM | 0.4873 mL | 2.4367 mL | 4.8734 mL | |
| 10 mM | 0.2437 mL | 1.2184 mL | 2.4367 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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