Cat. No.: HY-103100

SB-699551

1 Cited Publications

고객리뷰

Based on 1 publication(s) in Google Scholar

SB-699551 is a selective and brain penetrant 5-HT5A receptor antagonist with a pK_i 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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Purity: 99.53%
CAS No.: 864741-95-7
화학식: C₃₄H₄₇Cl₂N₃O
분자량:584.66

보관:

4°C, sealed storage, away from moisture

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

SB-699551 Chemical Structure

CAS No.: 864741-95-7

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- 제품 설명
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (1)
용액&용해도
- In Vitro
- In Vivo
순도&문서
References
Help & FAQs
Classifications
Bioz

Biological Activity

제품 설명

IC₅₀ & Target^[1]

5-HT_5A Receptor

8.2 (pKi)

All 5-HT Receptor Isoforms :

All Epigenetic Reader Domain Isoforms :

All Akt Isoforms :

All Ribosomal S6 Kinase (RSK) Isoforms :

All FOXO Isoforms :

FOXO1
FOXO3

In Vitro

SB-699551 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 (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 (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 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) 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.

Chemical Information

CAS No. 864741-95-7
Appearance Solid
분자량 584.66
화학식 C₃₄H₄₇Cl₂N₃O
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
선적

Room temperature in continental US; may vary elsewhere.
보관

4°C, sealed storage, away from moisture

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

Publications (1)

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Journal Impact Factor

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

용액&용해도

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.7104 mL

8.5520 mL

17.1040 mL

5 mM

0.3421 mL

1.7104 mL

3.4208 mL

10 mM

0.1710 mL

0.8552 mL

1.7104 mL

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.

몰농도 계산기

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

농도 희석 계산기

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

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

Stock Solution Working Solution

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.

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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

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

This protocol yields a clear solution of 2.5 mg/mL. If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

순도&문서

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (282 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
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-HT5A receptor blockade on amnesia or forgetting. Behav Brain Res. 2019;357-358:98-103. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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.

Keywords

SB-699551

1 Cited Publications

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SB-699551

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Publications Citing Use of MedChemExpress (MCE) SB-699551

All 5-HT Receptor Isoforms

All Epigenetic Reader Domain Isoforms

All Akt Isoforms

All Ribosomal S6 Kinase (RSK) Isoforms

All FOXO Isoforms

Biological Activity

Chemical Information

Publications (1)

용액&용해도

순도&문서

References

Help & FAQs

Complete Stock Solution Preparation Table

SB-699551 Related Classifications

HY-103100 Related Classifications