SB-699551 free base

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SB-699551 free base is a selective and brain penetrant 5-HT5A receptor antagonist with a pK_i 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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SB-699551 free base Chemical Structure

CAS No. : 791789-61-2

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SB-699551

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1 Publications Citing Use of MCE SB-699551 free base

•Mol Cancer Ther. 2024 Oct 1;23(10):1404-1417. [Abstract]

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•Related Small Molecules:

•Related Proteins:

View All 5-HT Receptor Isoform Specific Products:

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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

Biological Activity
Purity & Documentation
References
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Description

IC₅₀ & Target^[1]

5-HT_5A Receptor

8.2 (pKi)

5-HT_1A Receptor

6.3 (pKi)

5-HT_1B Receptor

6.5 (pKi)

5-HT_1D Receptor

6.4 (pKi)

5-HT_2A Receptor

6.1 (pKi)

5-HT_2B Receptor

6.0 (pKi)

5-HT_2C Receptor

6.4 (pKi)

5-HT₆ Receptor

5.4 (pKi)

5-HT₇ Receptor

5.4 (pKi)

In Vitro

SB-699551 free base potently binds to human 5-HT_5A receptors expressed in CHO cells with a pK_i 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-HT_5A receptors expressed in HEK 293 cells, with an apparent pK_B 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 Gα_i/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.

In Vivo

SB-699551 (3-30 mg/kg; i.p.; once) free base exhibits dose-dependent sedative effects on motor behavior in healthy rats in the open field and forced swim tests (FST)^[2].
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.

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.

Molecular Weight

511.74

Formula

C₃₄H₄₅N₃O

CAS No.

791789-61-2

SMILES

O=C(N(CCN(C)C)CC1=CC=C(C2=CC=C(CNCCC3=CC=CC=C3)C=C2)C=C1)CCC4CCCC4

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Purity & Documentation

Handling Instructions (2659 KB)

References

[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-HT_5A receptor blockade on amnesia or forgetting. Behav Brain Res. 2019;357-358:98-103. [Content Brief]