Size | Price | Stock | Qty |
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1mg |
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5mg |
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10mg |
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Other Sizes |
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Targets |
IC50: 0.58 nM (SERT)[1]
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ln Vivo |
In rats and dogs, SERT-IN-2 (DH4) (2.5 mg/kg, 5 mg/kg; intravenous or oral; single dosage) has high oral bioavailability and plasma exposure [1]. The blood-brain barrier can be crossed by SERT-IN-2 (10 mg/kg; intraperitoneal injection; single dosage) in SD rats [1]. In the rat hypothalamus, SERT-IN-2 (1–10 mg/kg; i.p.; single dosage) effectively counteracts p-chloroamphetamine (PCA)-induced serotonin depletion by inhibiting serotonin uptake [1]. Rats treated with SERT-IN-2 (1–10 mg/kg; intravenous injection; three times prior to the test) exhibit antidepressant effects, and the number of immobilities in the forced swim test (FST) decreases dose-dependently [1]. Pharmacokinetic analysis[1] Rat IV 1 193 1340 7.53 6.41 11.6 / PO 2.5 180 2790 7.28 / 83.28 Dog IV 1 520 2820 4.39 3.4 5.14 / PO 5 794 7540 16.4 / / 53.5 Route Dose (mg/kg) Cmax (ng/mL) AUC(0-t) (ng·h/mL) T1/2 (h) Vss (L/kg) Cl (L/h/kg) F (%)
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References |
[1]. Wang ZZ, et al. Deciphering Nonbioavailable Substructures Improves the Bioavailability of Antidepressants by Serotonin Transporter. J Med Chem. 2023 Jan 12;66(1):371-383.
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Molecular Formula |
C26H24F2N6
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Molecular Weight |
458.51
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CAS # |
2055228-33-4
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SMILES |
N1C2=C(C=C(C#N)C=C2)C(CCCN2CCN(C3=NC=C(C4=CC=C(F)C=C4F)C=N3)CC2)=C1
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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: 200 mg/mL (436.20 mM)
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 5 mg/mL (10.90 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 50.0 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: ≥ 5 mg/mL (10.90 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 50.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.  (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.1810 mL | 10.9049 mL | 21.8098 mL | |
5 mM | 0.4362 mL | 2.1810 mL | 4.3620 mL | |
10 mM | 0.2181 mL | 1.0905 mL | 2.1810 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.