SERT/NET-IN-1
Based on 1 Customer Validation
SERT/NET-IN-1 is a blood-brain barrier-permeable SERT and NET inhibitor, with an IC50 of 11.2 nM against human SERT and an IC50 of 32.0 nM against human NET. SERT/NET-IN-1 blocks 5-HT reuptake to enhance serotonergic signaling. SERT/NET-IN-1 also blocks norepinephrine reuptake to enhance central noradrenergic transmission and inhibits the ejaculatory reflex. SERT/NET-IN-1 prolongs ejaculatory latency, reduces ejaculation frequency and preserves sexual function. SERT/NET-IN-1 exhibits cross-species microsomal metabolic stability, shows acceptable oral brain exposure in rats, and has favorable safety profiles. SERT/NET-IN-1 can be used in studies related to premature ejaculation.
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- 화학식: C16H20N2OS
- 분자량:288.41
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
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Biological Activity
제품 설명
In Vitro
SERT/NET-IN-1 (compound 7) (1 μM; 0, 5, 15, 30, 60 min) exhibits excellent metabolic stability in human, mouse, rat, dog and monkey liver microsomes. The proportion of remaining parent compound ranges from 86.1% (rat) to 103% (dog) after 60 min, with 98.5% remaining in human liver microsomes[1].
SERT/NET-IN-1 (100 μM; 48 h) shows no obvious cytotoxicity in either HEK293 or HepG2 cells, with an IC50 of >100 μM in both cell lines[1].
SERT/NET-IN-1 (100 μM; 48 h) exhibits almost no agonistic activity on μ-opioid receptors, with an EC50 > 100 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HEK293, HepG2 cell
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Concentration:0-100 μM
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Incubation Time:48 h
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Result:Showed no obvious cytotoxicity in either HEK293 or HepG2 cells, with an IC50 of > 100 μM in both cell lines.
In Vivo
SERT/NET-IN-1 (20 mg/kg; i.p.; single administration, tested 15 min post-dose) significantly prolongs the ejaculation latency period (from 223.3 s to 713.2 s) and reduces the number of ejaculations within 20 min (from 2.25 to 1.125) in the 8-OH-DPAT-induced premature ejaculation model of male Wistar rats[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male Wistar rats (10 weeks old, trained for 4 weeks to establish stable sexual behavior); premature ejaculation model induced by intraperitoneal injection of 0.4 mg/kg 8-OH-DPAT 1 h before testing[1]
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Dosage:10 mg/kg and 20 mg/kg
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Administration:intraperitoneal injection 15 min before testing
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Result:At 10 mg/kg, showed no significant effect on ejaculation latency or the number of ejaculations.
At 20 mg/kg, significantly increased ejaculation latency from 223.3 s (pre-dose) to 713.2 s (post-dose) (p=0.0281) and reduced the number of ejaculations in 20 min from 2.25 to 1.125 (p=0.0313).
Had no significant effect on mount latency, intromission latency, post-ejaculatory interval, or copulatory rate, indicating no impairment of sexual motivation or erectile function.
Chemical Information
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분자량 288.41
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화학식 C16H20N2OS
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SMILES
CCC(N(C1CCNCC1)C2=C3C=CSC3=CC=C2)=O
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
용액&용해도
In Vitro:
DMSO : 100 mg/mL (346.73 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (8.67 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (8.67 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
순도&문서
References
Complete Stock Solution Preparation Table
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.4673 mL | 17.3364 mL | 34.6729 mL | 86.6822 mL |
| 5 mM | 0.6935 mL | 3.4673 mL | 6.9346 mL | 17.3364 mL | |
| 10 mM | 0.3467 mL | 1.7336 mL | 3.4673 mL | 8.6682 mL | |
| 15 mM | 0.2312 mL | 1.1558 mL | 2.3115 mL | 5.7788 mL | |
| 20 mM | 0.1734 mL | 0.8668 mL | 1.7336 mL | 4.3341 mL | |
| 25 mM | 0.1387 mL | 0.6935 mL | 1.3869 mL | 3.4673 mL | |
| 30 mM | 0.1156 mL | 0.5779 mL | 1.1558 mL | 2.8894 mL | |
| 40 mM | 0.0867 mL | 0.4334 mL | 0.8668 mL | 2.1671 mL | |
| 50 mM | 0.0693 mL | 0.3467 mL | 0.6935 mL | 1.7336 mL | |
| 60 mM | 0.0578 mL | 0.2889 mL | 0.5779 mL | 1.4447 mL | |
| 80 mM | 0.0433 mL | 0.2167 mL | 0.4334 mL | 1.0835 mL | |
| 100 mM | 0.0347 mL | 0.1734 mL | 0.3467 mL | 0.8668 mL |
SERT/NET-IN-1 Related Classifications
HY-182244 Related Classifications
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