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製品番号: HY-182244

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SERT/NET-IN-1

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.

商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。

分子式: C₁₆H₂₀N₂OS
分子量:288.41

保管条件:

Please store the product under the recommended conditions in the Certificate of Analysis.

SERT/NET-IN-1 構造式

価格（税別）

Amount: USD 0.00

* アイテムを追加する前、数量をご選択ください

Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

生物活性

製品説明

5-HT Receptor アイソフォーム固有の製品をすべて表示 :

体外実験

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.

Cell Cytotoxicity Assay^[1]

Cell Line:

HEK293, HepG2 cell
Concentration:

0-100 μM
Incubation Time:

48 h
Result:

Showed no obvious cytotoxicity in either HEK293 or HepG2 cells, with an IC₅₀ of > 100 μM in both cell lines.

体内実験

SERT/NET-IN-1 (compound 7) (2.5 mg/kg, intravenous injection; 5 mg/kg, i.p.; 10 mg/kg, p.o.; single administration) exhibits the pharmacokinetic properties of rapid absorption (T_max=1.0 h) and moderate elimination (T_1/2=2.8 h) in Wistar rats. Its oral bioavailability reaches 61.60%, with an AUC_0-t of 1347.05 ng?h/mL; the brain concentration reaches 143 ng/g at 0.5 h post-administration, with a brain/plasma ratio of 0.45; the brain concentration reaches 152.33 ng/g at 4 h post-administration, with the brain/plasma ratio increasing to 1.96, indicating favorable blood-brain barrier penetration ability^[1].
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.

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]
Dosage:

10 mg/kg and 20 mg/kg
Administration:

intraperitoneal injection 15 min before testing
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.

化学情報

分子量 288.41
分子式 C₁₆H₂₀N₂OS
SMILES

CCC(N(C1CCNCC1)C2=C3C=CSC3=CC=C2)=O
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件

Please store the product under the recommended conditions in the Certificate of Analysis.

純度とドキュメンテーション

取扱説明書 (2659 KB)

参考文献

[1]. Cui W, et al. N-aryl-N-acyl diamine derivatives as novel selective serotonin/norepinephrine transporter inhibitors for the treatment of premature ejaculation. Eur J Med Chem. Published online March 20, 2026. [Content Brief]

Calculators

モル濃度計算機

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

濃度濃度

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分子量分子量

希釈計算機

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濃度 _(開始) 濃度 _(開始)

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濃度 _(終了) 濃度 _(終了)

体積 _(終了) 体積 _(終了)

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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MOQ

Minimum order quantity

100 mg

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生物活性
- 製品説明
- 体外実験
- 体内実験
化学情報
純度とドキュメンテーション
参考文献

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SERT/NET-IN-1

5-HT Receptor アイソフォーム固有の製品をすべて表示