Size | Price | Stock | Qty |
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5mg |
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10mg |
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Other Sizes |
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Targets |
mTORC1[1].
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ln Vivo |
When administered intravenously and orally to rats, NV-5138 hydrochloride has nearly 100% oral bioavailability and a plasma elimination half-life of roughly three hours[1]. In PFC synaptosome preparations, NV-5138 hydrochloride (160 mg/kg, oral, single dose) substantially raises levels of phosphorylated mTOR and downstream targets phosphorylated p70S6K1 and phosphorylated 4EB-P1[2]. The antidepressant effects of NV-5138 hydrochloride (80 mg/kg, PO, daily for 7 days) are also observed[2].
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Animal Protocol |
Animal/Disease Models: Male SD (Sprague-Dawley) rats weighing 250-260 g[2].
Doses: 40, 80, 160 mg/kg. Route of Administration: PO, single dose (160 mg/kg) or daily for a total of 7 days (40 , 80 mg/kg). Experimental Results: Produced antidepressant effects. Animal/Disease Models: Male SD (Sprague-Dawley) rats weighed 250-400 g[1]. Doses: 1 mg/kg, 5 mg/kg (pharmacokinetic/PK Design). Route of Administration: IV at 1 mg/kg and PO at 5 mg/kg. Experimental Results: Essentially 100% orally bioavailable with an elimination half-life in plasma of ~ 3 h. |
References |
[1]. Sengupta S, et al. Discovery of NV-5138, the first selective Brain mTORC1 activator. Sci Rep. 2019 Mar 11;9(1):4107.
[2]. Kato T, et al. Sestrin modulator NV-5138 produces rapid antidepressant effects via direct mTORC1 activation. J Clin Invest. 2019 Apr 16;129(6):2542-2554. |
Molecular Formula |
C7H14CLF2NO2
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Molecular Weight |
217.64
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CAS # |
2639392-70-2
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Related CAS # |
NV-5138;2095886-80-7
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SMILES |
Cl.FC(C(C)(C)C[C@@H](C(=O)O)N)F
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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: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
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: 250 mg/mL (1148.69 mM)
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (9.56 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 (9.56 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in 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 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 (9.56 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 | 4.5947 mL | 22.9737 mL | 45.9474 mL | |
5 mM | 0.9189 mL | 4.5947 mL | 9.1895 mL | |
10 mM | 0.4595 mL | 2.2974 mL | 4.5947 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.