2. GPCR/G Protein Neuronal Signaling Epigenetics PI3K/Akt/mTOR MAPK/ERK Pathway Metabolic Enzyme/Protease
  3. 5-HT Receptor Epigenetic Reader Domain Akt Ribosomal S6 Kinase (RSK) FOXO
  4. SB-699551

SB-699551 is a selective and brain penetrant 5-HT5A receptor antagonist with a pKi of 8.2 nM. SB-699551 shows high selectivity over most other 5-HT receptor subtypes, dopamine receptors, and α1B adrenoceptor. SB-699551 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 can be used for the research of anxiety, breast cancer, and Alzheimer's disease.

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SB-699551

SB-699551 Chemical Structure

CAS No. : 864741-95-7

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Based on 1 publication(s) in Google Scholar

Other Forms of SB-699551:

SB-699551 Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE SB-699551

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

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p70S6K RSK2 RSK3 RSK4

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FOXO1 FOXO3

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

SB-699551 is a selective and brain penetrant 5-HT5A receptor antagonist with a pKi of 8.2 nM. SB-699551 shows high selectivity over most other 5-HT receptor subtypes, dopamine receptors, and α1B adrenoceptor. SB-699551 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 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

 

5-HT5A Receptor

8.2 (pKi)

In Vitro

SB-699551 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 (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 (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 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.

SB-699551 Related Antibodies
In Vivo

SB-699551 (3-30 mg/kg; i.p.; once) 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) 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) 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) 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) 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.) prevents forgetting induced by a 216-hour interruption of autoshaping training in rats[5].
SB-699551 (0.3 mg/kg; s.c.) 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, 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: 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: 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

584.66

Formula

C34H47Cl2N3O
CAS No.
Appearance

Solid

Color

White to light yellow

SMILES

O=C(N(CCN(C)C)CC1=CC=C(C2=CC=C(CNCCC3=CC=CC=C3)C=C2)C=C1)CCC4CCCC4.[H]Cl.[H]Cl
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (171.04 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : 1 mg/mL (1.71 mM; ultrasonic and warming and heat to 60°C)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.7104 mL 8.5520 mL 17.1040 mL
5 mM 0.3421 mL 1.7104 mL 3.4208 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: 2.5 mg/mL (4.28 mM); Clear solution; Need ultrasonic

    This protocol yields a clear solution of 2.5 mg/mL.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: 2.5 mg/mL (4.28 mM); Clear solution; Need ultrasonic

    This protocol yields a clear solution of 2.5 mg/mL.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.53%

SDS (393 KB)

COA (246 KB) HNMR (145 KB) RP-HPLC (169 KB) LCMS (392 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
H2O / DMSO 1 mM 1.7104 mL 8.5520 mL 17.1040 mL 42.7599 mL
DMSO 5 mM 0.3421 mL 1.7104 mL 3.4208 mL 8.5520 mL
10 mM 0.1710 mL 0.8552 mL 1.7104 mL 4.2760 mL
15 mM 0.1140 mL 0.5701 mL 1.1403 mL 2.8507 mL
20 mM 0.0855 mL 0.4276 mL 0.8552 mL 2.1380 mL
25 mM 0.0684 mL 0.3421 mL 0.6842 mL 1.7104 mL
30 mM 0.0570 mL 0.2851 mL 0.5701 mL 1.4253 mL
40 mM 0.0428 mL 0.2138 mL 0.4276 mL 1.0690 mL
50 mM 0.0342 mL 0.1710 mL 0.3421 mL 0.8552 mL
60 mM 0.0285 mL 0.1425 mL 0.2851 mL 0.7127 mL
80 mM 0.0214 mL 0.1069 mL 0.2138 mL 0.5345 mL
100 mM 0.0171 mL 0.0855 mL 0.1710 mL 0.4276 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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  • 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:

SB-699551864741-95-7SB699551SB 6995515-HT ReceptorEpigenetic Reader DomainAktRibosomal S6 Kinase (RSK)FOXOSerotonin Receptor5-hydroxytryptamine ReceptorPKBProtein kinase BS6KForkhead box OHCC1954MCF-7WNK1PRAS40anticancerbreast tumorInhibitorinhibitorinhibit

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