SB-699551 free base
Based on 1 publication(s) in Google Scholar
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.
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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。
- CAS 番号: 791789-61-2
- 分子式: C34H45N3O
- 分子量:511.74
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
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生物活性
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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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MedChemExpress（MCE）の使用を引用している文献 SB-699551 free base
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生物活性
製品説明
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) |
体外実験
SB-699551 free base potently binds to human 5-HT5A receptors expressed in CHO cells with a pKi of 8.2 and exhibits ≥100-fold selectivity against most other 5-HT receptor subtypes[1].
SB-699551 free base (1 μM) acts as a competitive antagonist at human 5-HT5A receptors expressed in HEK 293 cells, with an apparent pKB of 8.0[1].
SB-699551 free base (72 h) inhibits tumorsphere formation and cell viability in HCC1954 and MCF-7 human breast tumor cell lines with IC50 values ranging from 0.2 to 0.3 μM[3].
SB-699551 free base inhibits tumorsphere formation in PDX-derived human breast tumor cell lines (PDX 81, PDX 18, PDX 12) with IC50 values ranging from 470 nM to 775 nM, independent of subtype[3].
SB-699551 (4 μM, 30 min; 4 μM, 5-60 min; 3-5 μM, 24 h) modulates signaling via the Gαi/o pathway and the PI3K/AKT/mTOR axis in MCF-7 and MDA-MB-157 human breast tumor cell lines, with increased CREB phosphorylation and reduced phosphorylation of AKT and downstream targets[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
体内実験
SB-699551 (3-60 mg/kg; i.p.; once) free base shows anxiolytic-like effects in the foot-shock-induced USV model with an ED50 of 25.4 mg/kg[2].
SB-699551-A (3-30 mg/kg; i.p.; three times: 23.5, 5, and 1 h before test) free base does not exhibit antidepressant-like effects in the forced swim test[2].
SB-699551 (25 mg/kg; i.p.; 5 days a week; 3 weeks) free base reduces human breast tumor xenograft growth in NOD/SCID mice[3].
SB-699551 (0.1-3.0 mg/kg; s.c.; single injection post-first autoshaping session) free base impairs short-term memory at 0.3 mg/kg and long-term memory at 0.3, 1.0, and 3.0 mg/kg in male Wistar rats in an autoshaping associative learning task[4].
SB-699551 (0.3-3.0 mg/kg; s.c.) free base prevents forgetting induced by a 216-hour interruption of autoshaping training in rats[5].
SB-699551 (0.3 mg/kg; s.c.) free base alone induces amnesia-like effects in rats, with co-administration with Dizocilpine (HY-15084B) reversing these effects in 48-hour long-term memory and co-administration with Scopolamine (HY-N0296) reversing effects in 1.5-hour short-term and 24- and 48-hour long-term memory[5].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Hannover Wistar (male, 240-290 g and 160-210 g)[2]
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Dosage:3, 10, 30 mg/kg
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Administration:i.p.
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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.
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Animal Model:Hannover Wistar (male, 225-360 g, 8-12 animals/group)[2]
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Dosage:3, 10, 30, 60 mg/kg
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Administration:i.p.
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Result:Dose-dependently decreased ultrasonic vocalization, with a significant effect at 30 mg/kg and an ED50 value of 25.4 mg/kg.
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Animal Model:NOD/SCID (female, 6-8-week old) injected with HCC1954 cells[3]
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Dosage:25 mg/kg
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Administration:i.p.; 5 days a week; 3 weeks
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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.
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Animal Model:Wistar (male, 12 weeks-old, body weight reduced to 85% of ad libitum weight)[4]
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Dosage:0.1, 0.3, 1.0, 3.0 mg/kg
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Administration:s.c.; single injection post-first autoshaping session
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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.
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Animal Model:Wistar rats (adult male)[5]
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Dosage:0.3, 3.0 mg/kg
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Administration:s.c.
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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.
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Animal Model:Wistar rats (adult male)[5]
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Dosage:0.3 mg/kg
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Administration:s.c.
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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.
化学情報
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CAS 番号 791789-61-2
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分子量 511.74
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分子式 C34H45N3O
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SMILES
O=C(N(CCN(C)C)CC1=CC=C(C2=CC=C(CNCCC3=CC=CC=C3)C=C2)C=C1)CCC4CCCC4
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (1)
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Journal Impact Factor
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Most Recent
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Mol Cancer Ther
AKT Inhibition Sensitizes to Polo-Like Kinase 1 Inhibitor Onvansertib in Prostate Cancer. [Abstract]2024 Oct 1;23(10):1404-1417. PMID: 38894678
純度とドキュメンテーション
参考文献
[1]. Corbett DF, et al. Discovery of a potent and selective 5-ht5A receptor antagonist by high-throughput chemistry. Bioorg Med Chem Lett. 2005;15(18):4014-4018. [Content Brief]
[2]. Kassai F, et al. Effect of 5-HT5A antagonists in animal models of schizophrenia, anxiety and depression. Behav Pharmacol. 2012;23(4):397-406. [Content Brief]
[3]. Gwynne WD, et al. Antagonists of the serotonin receptor 5A target human breast tumor initiating cells. BMC Cancer. 2020;20(1):724. Published 2020 Aug 5. [Content Brief]
[4]. Gonzalez R, et al. Role of 5-HT5A receptors in the consolidation of memory. Behav Brain Res. 2013 Sep 1;252:246-51. [Content Brief]
[5]. Aparicio-Nava L, et al. Effects of 5-HT5A receptor blockade on amnesia or forgetting. Behav Brain Res. 2019;357-358:98-103. [Content Brief]
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
SB-699551 free base 関連分類
HY-136700 関連分類
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