2. GPCR/G Protein Neuronal Signaling PI3K/Akt/mTOR
  3. 5-HT Receptor Akt
  4. SB-699551 free base

SB-699551 free base 是一种具有脑穿透性的选择性 5-HT5A 受体拮抗剂，其 pKi 值为 8.2 nM。SB-699551 free base 对大多数其他 5-HT 受体亚型、多巴胺受体和 α1B 肾上腺素受体具有高选择性。SB-699551 free base 可阻断 Gαi/o 偶联信号通路与 PI3K/AKT/mTOR 信号通路，改变乳腺癌细胞中 CREB、ATF1、AKT、PRAS40、S6K 和 FOXO1 的磷酸化水平。SB-699551 free base 可用于焦虑症、乳腺癌和阿尔茨海默病的相关研究。

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SB-699551 free base

SB-699551 free base Chemical Structure

CAS No. : 791789-61-2

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SB-699551 free base 相关抗体

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MCE 顾客使用本产品发表的 1 篇科研文献

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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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Akt Akt1 Akt2 Akt3

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

SB-699551 free base is a selective and brain penetrant 5-HT5A receptor antagonist with a pKi of 8.2 nM. SB-699551 free base shows high selectivity over most other 5-HT receptor subtypes, dopamine receptors, and α1B adrenoceptor. SB-699551 free base disrupts Gαi/o-coupled and PI3K/AKT/mTOR signaling pathways, alters CREB, ATF1, AKT, PRAS40, S6K, and FOXO1 phosphorylation in breast tumor cells. SB-699551 free base can be used for the research of anxiety, breast cancer, and Alzheimer's disease[1][2][3][4][5].

IC50 & Target[1]

5-HT5A Receptor

8.2 (pKi)

5-HT1A Receptor

6.3 (pKi)

5-HT1B Receptor

6.5 (pKi)

5-HT1D Receptor

6.4 (pKi)

5-HT2A Receptor

6.1 (pKi)

5-HT2B Receptor

6.0 (pKi)

5-HT2C Receptor

6.4 (pKi)

5-HT6 Receptor

5.4 (pKi)

5-HT7 Receptor

5.4 (pKi)

体外研究
(In Vitro)

SB-699551 free base 可强效结合于 CHO 细胞中表达的人 5-HT5A 受体，其 pKi 值为 8.2，且对大多数其他 5-HT 受体亚型表现出 ≥100 倍的选择性[1]。
SB-699551 free base (1 μM) 对 HEK 293 细胞中表达的人源 5-HT5A受体发挥竞争性拮抗剂作用，其表观 pKB 值为 8.0[1]。
SB-699551 free base (72 h) 可抑制 HCC1954 和 MCF-7 人乳腺癌细胞系的肿瘤球形成与细胞活力，其 IC50 值范围为 0.2 至 0.3 μM[3]。
SB-699551 free base 可抑制来源于患者源性异种移植 (PDX) 的人乳腺癌细胞系 (PDX 81、PDX 18、PDX 12) 的肿瘤球形成，其 IC50值范围为 470 nM 至 775 nM，且与肿瘤亚型无关[3]。
SB-699551 (4 μM、30 分钟；4 μM、5-60 分钟；3-5 μM、24 小时) 可在人乳腺癌细胞系 MCF-7 和 MDA-MB-157 中调控 Gαi/o通路及 PI3K/AKT/mTOR 轴的信号传导，具体表现为 CREB 磷酸化水平升高，而 AKT 及其下游靶点的磷酸化水平降低[3]。

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

SB-699551 free base 相关抗体:
体内研究
(In Vivo)

SB-699551 (3-30 mg/kg；i.p.；单次) free base 在开放场试验和强迫游泳试验 (FST) 中，对健康大鼠的运动行为表现出剂量依赖性的镇静作用[2]。
SB-699551 (3-60 mg/kg；腹腔注射；单次) free base 在足部电击诱导的超声波发声 (USV) 模型中表现出类抗焦虑作用，其 ED50为 25.4 mg/kg[2]。
SB-699551-A (3-30 mg/kg；腹腔注射；共 3 次：分别于测试前 23.5、5 和 1 小时给药) free base 在强迫游泳试验中未表现出类抗抑郁作用[2]。
SB-699551 (25 mg/kg；腹腔注射；一周 5 次；持续 3 周) free base 可抑制 NOD/SCID 小鼠体内人乳腺癌异种移植物的生长[3]。
SB-699551 (0.1-3.0 mg/kg；皮下注射；首次自塑形训练后单次给药) free base 在雄性 Wistar 大鼠的自塑形联想学习任务中，于 0.3 mg/kg 剂量下会损伤短时记忆，于 0.3、1.0 和 3.0 mg/kg 剂量下会损伤长时记忆[4]。
SB-699551 (0.3-3.0 mg/kg; s.c.) free base 可防止大鼠因自主塑形训练被中断 216 小时而出现的遗忘现象[5]。
SB-699551 (0.3 mg/kg；皮下注射) free base 单独给药会在大鼠中诱导类遗忘效应；与 Dizocilpine (HY-15084B) 联合给药可逆转其对 48 小时长时程记忆的影响，而与 Scopolamine (HY-N0296) 联合给药则可逆转其对 1.5 小时短时程记忆及 24、48 小时长时程记忆的影响[5]。

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

Animal Model: Hannover Wistar (male, 240-290 g and 160-210 g)[2]
Dosage: 3, 10, 30 mg/kg
Administration: i.p.
Result: Showed a dose-dependent tendency to decrease the number of square entries; dose-dependently decreased the number of rearings and groomings, with significant effects at 10 and 30 mg/kg doses, respectively; did not induce writhing behavior.
Animal Model: Hannover Wistar (male, 225-360 g, 8-12 animals/group)[2]
Dosage: 3, 10, 30, 60 mg/kg
Administration: i.p.
Result: Dose-dependently decreased ultrasonic vocalization, with a significant effect at 30 mg/kg and an ED50 value of 25.4 mg/kg.
Animal Model: NOD/SCID (female, 6-8-week old) injected with HCC1954 cells[3]
Dosage: 25 mg/kg
Administration: i.p.; 5 days a week; 3 weeks
Result: Reduced xenograft growth rate compared to vehicle; Induced large fibrotic areas with reduced tumor cell density and a subtle increase in TUNEL-positive cells in xenografts.
Animal Model: Wistar (male, 12 weeks-old, body weight reduced to 85% of ad libitum weight)[4]
Dosage: 0.1, 0.3, 1.0, 3.0 mg/kg
Administration: s.c.; single injection post-first autoshaping session
Result: Decreased conditioned responses (CR%) during both short-term memory (1.5 h) and long-term memory (24 h) at 0.3 mg/kg; decreased CR% during long-term memory (24 h) at 1.0 and 3.0 mg/kg relative to vehicle controls (all effects significant per Tukey test); showed no significant effect at 0.1 mg/kg.
Animal Model: Wistar rats (adult male)[5]
Dosage: 0.3, 3.0 mg/kg
Administration: s.c.
Result: Produced a significant anti-forgetting effect (114% of control-saline group values) at 0.3 mg/kg; produced a slight anti-forgetting effect (82% of control-saline group values) at 3.0 mg/kg following the 216-hour interruption period.
Animal Model: Wistar rats (adult male)[5]
Dosage: 0.3 mg/kg
Administration: s.c.
Result: Induced amnesia-like effects with significant decrements in conditioned responses (CR) at 1.5 hours, 24 hours, and 48 hours; co-administration with dizocilpine reversed these effects in 48-hour long-term memory; co-administration with scopolamine reversed effects in 1.5-hour short-term and 24- and 48-hour long-term memory.
分子量

511.74

Formula

C34H45N3O
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

SB-699551 free base 相关分类

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Keywords:

SB-699551791789-61-2SB699551SB 6995515-HT ReceptorAktSerotonin Receptor5-hydroxytryptamine ReceptorPKBProtein kinase B5-HT5A receptorPI3K/AKT/mTOR signaling pathwaysNOD/SCID micedopamine receptorsblood-brain barrierbreast tumor cellstumor cell apoptosisα1B adrenoceptor5-HT receptor subtypesrat serotonin transportersInhibitorinhibitorinhibit

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