2. Neuronal Signaling GPCR/G Protein
  3. Serotonin Transporter 5-HT Receptor
  4. SERT/NET-IN-1

SERT/NET-IN-1 是一种具有血脑屏障通透性的 SERT 和 NET 抑制剂，对人源 SERT 的 IC50 为 11.2 nM，对人源 NET 的 IC50 为 32.0 nM。SERT/NET-IN-1 可阻断 5-HT 重摄取以增强 5-羟色胺能信号传导。SERT/NET-IN-1 还阻断去甲肾上腺素重摄取以增强中枢去甲肾上腺素能传递，并抑制射精反射。SERT/NET-IN-1 可延长射精潜伏期、减少射精次数并保留性功能。SERT/NET-IN-1 具有跨物种微粒体代谢稳定性，在大鼠中具有可接受的口服脑暴露量，且安全性良好。SERT/NET-IN-1 可用于早泄的相关研究。

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SERT/NET-IN-1

SERT/NET-IN-1 Chemical Structure

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SERT/NET-IN-1 相关抗体

Top Publications Citing Use of Products

查看 5-HT Receptor 亚型特异性产品:

查看所有亚型
5-HT Receptor 5-HT1 Receptor 5-HT2 Receptor 5-HT3 Receptor 5-HT4 Receptor 5-HT5 Receptor 5-HT6 Receptor 5-HT7 Receptor

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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[1].

体外研究
(In Vitro)

SERT/NET-IN-1 (compound 7) (1 μM；0、5、15、30、60 min) 在人、小鼠、大鼠、犬、猴肝微粒体中均表现出优异代谢稳定性，60 min 后剩余原型化合物比例为 86.1% (大鼠) 至 103% (犬)，人肝微粒体中剩余 98.5%[1]。
SERT/NET-IN-1 (100 μM；48 h) 对 HEK293 和 HepG2 细胞均无明显细胞毒性，IC50 均 >100 μM[1]。
SERT/NET-IN-1 (100 μM；48 h) 对 μ-阿片受体几乎无激动活性，EC50>100 μM[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

SERT/NET-IN-1 相关抗体:

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.
体内研究
(In Vivo)

SERT/NET-IN-1 (compound 7) (2.5 mg/kg，静脉注射；5 mg/kg，腹腔注射；10 mg/kg，口服；单次) 在 Wistar 大鼠中药代结果表现出吸收迅速（Tmax=1.0 h)，消除适中 (T1/2=2.8 h) 的特性，口服生物利用度为 61.60%，AUC0-t 为 1347.05 ng・h/mL；给药后 0.5 h 脑浓度达 143 ng/g，脑 / 血浆比为 0.45；4 h 脑浓度达 152.33 ng/g，脑 / 血浆比升至 1.96，具有良好的血脑屏障穿透能力[1]。
SERT/NET-IN-1 (20 mg/kg；腹腔注射；单次给药，给药 15 min 后测试) 在 8-OH-DPAT (HY-112061) 诱导的 Wistar 雄性大鼠早泄模型中，显著延长射精潜伏期 (从 223.3 s 增至 713.2 s)，减少 20 min 内射精次数 (从 2.25 次降至 1.125 次)[1]。

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.
分子量

288.41

Formula

C16H20N2OS
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

SERT/NET-IN-1 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

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

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

SERT/NET-IN-1Serotonin Transporter5-HT Receptor5-HTTSERTSLC6A4Serotonin Receptor5-hydroxytryptamine Receptorserotonin reuptakecentral noradrenergic transmissionnorepinephrine reuptakeserotonergic signalingNETpremature ejaculationratsejaculatory reflexInhibitorinhibitorinhibit

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