Art. -Nr.: HY-18596

SB-215505

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SB-215505 is an orally active and subtype-selective 5-HT_2B receptor antagonist with pK_i values of 8.3, 6.77, 7.66 for 5-HT_2B, 5-HT_2A, 5-HT_2C, respectively. SB-215505 increases wakefulness and motor activity in rats.

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Reinheit: 98.91%
CAS. Nr.: 162100-15-4
Formel: C₁₉H₁₆ClN₃O
Molecular Weight:337.80

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

SB-215505 Chemical Structure

CAS. Nr.: 162100-15-4

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

SB-215505 is an orally active and subtype-selective 5-HT_2B receptor antagonist with pK_i values of 8.3, 6.77, 7.66 for 5-HT_2B, 5-HT_2A, 5-HT_2C, respectively^[1]. SB-215505 increases wakefulness and motor activity in rats^[2].

IC₅₀ & Target^[1]

5-HT_2A Receptor

5-HT_2B Receptor

5-HT_2C Receptor

5-HT_2B Receptor

8.3 (pKi)

5-HT_2A Receptor

6.77 (pKi)

5-HT_2C Receptor

7.66 (pKi)

Alle 5-HT Receptor Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
CHO-K1	IC₅₀	13 nM Compound: SB-215505	Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay	[PMID: 19307114]
CHO-K1	IC₅₀	64 nM Compound: SB-215505	Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albumin Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albumin	[PMID: 19307114]

In Vitro

SB-215505 is 30 fold selective for the 5-HT_2B over the 5-HT_2A receptor, and only marginally selective over the 5-HT_2C receptor^[1].

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

In Vivo

SB-215505 (0.1-1.0 mg/kg; i.p.; two doses) dose-dependently increases wakefulness (W) and decreases IS, PS, SWS-2 in rats^[2].

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

Animal Model:

Male Sprague-Dawley rats weighing 230-260 g^[2]
Dosage:

0.1, 0.3 and 1.0 mg/kg
Administration:

IP; two doses (4 days between two doses)
Result:

Dose-dependently increased wakefulness (W) and decreased intermediate stage of sleep (IS), paradoxical sleep (PS), SWS-2.

Chemical Information

CAS. Nr. 162100-15-4
Appearance Solid
Molecular Weight 337.80
Formel C₁₉H₁₆ClN₃O
Color Off-white to light brown
SMILES

O=C(N1CCC2=C1C=C(Cl)C(C)=C2)NC3=C4C=CC=NC4=CC=C3
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 25 mg/mL (74.01 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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

2.9603 mL

14.8017 mL

29.6033 mL

5 mM

0.5921 mL

2.9603 mL

5.9207 mL

10 mM

0.2960 mL

1.4802 mL

2.9603 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (276 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)

Verweise

[1]. C Reavill, et al. Attenuation of haloperidol-induced catalepsy by a 5-HT2C receptor antagonist. Br J Pharmacol. 1999 Feb;126(3):572-4. [Content Brief]

[2]. Sandor Kantor, et al. Increased wakefulness, motor activity and decreased theta activity after blockade of the 5-HT2B receptor by the subtype-selective antagonist SB-215505. J Pharmacol. 2004 Aug;142(8):1332-42. [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

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. 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
DMSO	1 mM	2.9603 mL	14.8017 mL	29.6033 mL	74.0083 mL
	5 mM	0.5921 mL	2.9603 mL	5.9207 mL	14.8017 mL
	10 mM	0.2960 mL	1.4802 mL	2.9603 mL	7.4008 mL
	15 mM	0.1974 mL	0.9868 mL	1.9736 mL	4.9339 mL
	20 mM	0.1480 mL	0.7401 mL	1.4802 mL	3.7004 mL
	25 mM	0.1184 mL	0.5921 mL	1.1841 mL	2.9603 mL
	30 mM	0.0987 mL	0.4934 mL	0.9868 mL	2.4669 mL
	40 mM	0.0740 mL	0.3700 mL	0.7401 mL	1.8502 mL
	50 mM	0.0592 mL	0.2960 mL	0.5921 mL	1.4802 mL
	60 mM	0.0493 mL	0.2467 mL	0.4934 mL	1.2335 mL

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SB-215505

GPCR/G Protein Compound Library

Neuronal Signaling Compound Library

Orally Active Compound Library

Neurotransmitter Receptor Compound Library

Anti-Alzheimer's Disease Compound Library

Anti-Parkinson's Disease Compound Library

Neurodegenerative Disease-related Compound Library

5-HT Receptor Compound Library

Human Metabolite Library

Coagulation and Anti-coagulation Compound Library

Heterocyclic Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Inhibitors Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

Lactylation Compound Library

Alle 5-HT Receptor Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

SB-215505

GPCR/G Protein Compound Library

Neuronal Signaling Compound Library

Orally Active Compound Library

Neurotransmitter Receptor Compound Library

Anti-Alzheimer's Disease Compound Library

Anti-Parkinson's Disease Compound Library

Neurodegenerative Disease-related Compound Library

5-HT Receptor Compound Library

Human Metabolite Library

Coagulation and Anti-coagulation Compound Library

Heterocyclic Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Inhibitors Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

Lactylation Compound Library

Alle 5-HT Receptor Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

SB-215505 Related Classifications

HY-18596 Related Classifications