2. Neuronal Signaling GPCR/G Protein Membrane Transporter/Ion Channel
  3. Cholinesterase (ChE) Serotonin Transporter 5-HT Receptor Calcium Channel Sodium Channel Sigma Receptor
  4. BGC-201259

BGC-201259 (RS-1259) 是一种口服有效的同时靶向乙酰胆碱酯酶 (AChE) (IC50 = 101 nM) 和血清素转运蛋白 (SERT) (IC50 = 42 nM) 的抑制剂。BGC-20125 抑制 5-HT 受体，IC50 值为 90 nM。BGC-20125 对 NA 转运体 (NA transporter) (IC50 = 7.7 μM)、L 型钙通道 (L-type calcium channel) (IC50 = 3.6 μM)、σ 受体 (σ receptor) (IC50 = 2 μM) 和钠通道 (sodium channel) (IC50 = 5.1 μM) 有微弱活性。BGC-201259 通过均衡抑制两种靶点，在改善认知和情绪症状方面展现出协同潜力。BGC-201259 可用于研究阿尔茨海默症。

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BGC-201259

BGC-201259 Chemical Structure

CAS No. : 444667-97-4

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BGC-201259 相关抗体

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AChE BChE

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5-HT Receptor 5-HT1 Receptor 5-HT2 Receptor 5-HT3 Receptor 5-HT4 Receptor 5-HT5 Receptor 5-HT6 Receptor 5-HT7 Receptor

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N-type calcium channel L-type calcium channel P/Q-type calcium channel T-type calcium channel Calcium Channel

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Sigma 1 Receptor Sigma 2 Receptor

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

BGC-201259 (RS-1259) is an orally active inhibitor that simultaneously targets acetylcholinesterase (AChE) (IC50 = 101 nM) and serotonin transporter (SERT) (IC50 = 42 nM). BGC-201259 inhibits 5-HT receptor with an IC50 of 90 nM. BGC-201259 exhibits strong weak activity against the NA transporter (IC50 = 7.7 μM), L-type calcium channel (IC50 = 3.6 μM), σ receptor (IC50 = 2 μM), and sodium channel (IC50 = 5.1 μM). BGC-201259 demonstrates synergistic potential in improving cognitive and emotional symptoms by balancing the inhibition of these two targets. BGC-201259 can be used in research on Alzheimer's disease[1][2].

体内研究
(In Vivo)

BGC-201259 (1 和 10 mL/kg，口服，单次给药) 分别抑制小鼠 (AChE ED50 = 13 mg/kg；SERT ED50 = 2.4 mg/kg) 和大鼠 (AChE ED50 = 43 mg/kg) 脑内的乙酰胆碱酯酶 (AChE) 和血清素转运蛋白 (SERT) 活性[1][2]。
BGC-201259 (64 mg/kg，口服，单次给药) 可同时增强活体大鼠脑内的胆碱能和血清素能神经传递[1][2]。
BGC-201259 (4-16 mg/kg，口服，单次给药) 在小鼠模型中可显著增强 5-羟色氨酸 (5-HTP) 诱导的运动活性，并表现出抗抑郁样活性[1][2]。
BGC-201259 (0.5-1 mg/kg，口服，单次给药) 可显著改善老年大鼠的空间短期记忆障碍[1][2]。
BGC-201259 (1-4 mg/kg，口服，单次给药) 呈剂量依赖性地延长大鼠清醒时间并减少睡眠[1][2]。

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

Animal Model: 5-HTP enhancement experiment established in male ddY mice (4 weeks old)[1][2]
Dosage: 4, 8, 16 mg/kg
Administration: Oral administration (p.o.), single dose
Result: Significantly enhanced 5-HTP-induced motor activity, exhibiting a bell-shaped dose-response curve.
Animal Model: Water maze test established in aged F344 rats (24-25 months old)[1][2]
Dosage: 0.5, 1 and 2 mg/kg
Administration: Oral administration (p.o.), single dose
Result: Significantly improved spatial short-term memory deficits in aged rats.
Animal Model: Electroencephalogram (EEG) monitoring of consciousness level established in rats[1][2]
Dosage: 1 and 4 mg/kg
Administration: Oral administration (p.o.), single dose
Result: Effectively enhanced the overall level of brain arousal.
分子量

862.88

Formula

C42H50N6O14
CAS 号
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

BGC-201259 相关分类

  • 摩尔计算器

  • 稀释计算器

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  • Do most proteins show cross-species activity?

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Keywords:

BGC-201259444667-97-4RS-1259BGC201259BGC 201259RS1259RS 1259Cholinesterase (ChE)Serotonin Transporter5-HT ReceptorCalcium ChannelSodium ChannelSigma Receptor5-HTTSERTSLC6A4Serotonin Receptor5-hydroxytryptamine ReceptorCa2+ channelsCa channelsNa channelsNa+ channelsacetylcholinesteraseserotonin transportercerebral activationAlzheimer’s diseaserodentInhibitorinhibitorinhibit

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