Size | Price | Stock | Qty |
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5mg |
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10mg |
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25mg |
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50mg |
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100mg |
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250mg |
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Other Sizes |
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ln Vitro |
NIH 3T3 cells exhibit stable expression of the KFERQ-PS-Dendra reporter gene as a result of CA77.1's dose- and time-dependent activation of CMA (0-30 μM; 16 hours). The average of the fluorescence spots within each cell was used to calculate CMA activity [1]. LC3-II expression and autophagic flux in NIH 3T3 cells are unaffected by CA77.1 (20 μM; 6 hours) [1].
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ln Vivo |
CA-77.1 (10 mg/kg; single dose; oral gavage) exhibits good pharmacokinetics and brain penetration. Cmax, AUClast, Tmax, and T1/2 are, in that order, 3534 ng/g, 8338 h*ng/g, 1 hour, and 1.89 hours [1]. In PS19 mice, previously reported hyperkinesia was normalized to control levels by CA77.1 (oral gavage; 30 mg/kg; 6 months). In the hippocampus, amygdala, and piriform cortex, it also decreased the quantity and percentage of neurons with pathogenic tau conformations. Vehicle-treated PS19 mice showed a decrease in the number of large Iba1-positive cells with rod-dystrophic morphology and an increase in microglia following CA77.1 treatment [1].
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Animal Protocol |
Animal/Disease Models: 9-month-old CTR or PS19 mice [1]
Doses: 30 mg/kg Route of Administration: po (oral gavage); 30 mg/kg; 6-month Experimental Results: Behavior of frontotemporal dementia-related protein toxicity mouse model and neuropathology improved. |
References |
[1]. Mathieu Bourdenx, et al. Chaperone-mediated autophagy prevents collapse of the neuronal metastable proteome.Cell. 2021 May 13;184(10):2696-2714.e25.
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Molecular Formula |
C16H12CLN3O
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Molecular Weight |
297.7390
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CAS # |
2412270-22-3
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SMILES |
ClC1C([H])=C([H])C2C(C=1[H])=NC([H])=C(C1C([H])=C([H])C(=C([H])C=1[H])N([H])C(C([H])([H])[H])=O)N=2
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
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 : ~5 mg/mL (~16.79 mM)
Ethanol : ~1 mg/mL (~3.36 mM) |
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Solubility (In Vivo) |
Solubility in Formulation 1: 2 mg/mL (6.72 mM) in 45% PEG300 +5% Tween-80 + 50% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.  (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 3.3586 mL | 16.7932 mL | 33.5864 mL | |
5 mM | 0.6717 mL | 3.3586 mL | 6.7173 mL | |
10 mM | 0.3359 mL | 1.6793 mL | 3.3586 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.