SB-215505

Name: SB-215505
Brand: MedChemExpress
SKU: HY-18596
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Cat. No.: HY-18596 Pureza: 98.91%: Ficha de datos
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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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SB-215505 Estructura química

No. CAS : 162100-15-4

Tamaño	Stock	Cantidad
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	En stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	En stock	Estimated Time of Arrival: December 31
Solid
5 mg	En stock	Estimated Time of Arrival: December 31
10 mg	En stock	Estimated Time of Arrival: December 31
25 mg	En stock	Estimated Time of Arrival: December 31
50 mg	En stock	Estimated Time of Arrival: December 31
100 mg	En stock	Estimated Time of Arrival: December 31
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500 mg	Obtener un presupuesto

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Based on 1 Customer Validation

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Ver todos los productos específicos de isoformas 5-HT Receptor:

Ver todas las isoformas

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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Descripciòn

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)

Cellular Effect

Cell Line	Type	Value	Description	References
CHO-K1	IC₅₀	13 1 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	13 1 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	13 1 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 1 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]
CHO-K1	IC₅₀	64 1 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]
CHO-K1	IC₅₀	64 1 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.

Peso molecular

337.80

Fòrmula

C₁₉H₁₆ClN₃O

No. CAS

162100-15-4

Appearance

Solid

Color

Off-white to light brown

SMILES

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

Envío

Room temperature in continental US; may vary elsewhere.

Almacenamiento

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

Solvente y solubilidad

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)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

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

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

Calculadora de molaridad
Calculadora de dilución

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

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Volume _(start)

Concentration _(final)

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In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

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

Calculation results:

Working solution concentration: mg/mL

Pureza y Documentación

Purity: 98.91%

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Ficha de datos (276 KB) SDS (393 KB)

COA (253 KB) HNMR (267 KB) LCMS (93 KB)

Instrucciones de manejo (2659 KB)

Referencias

[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]

Complete Stock Solution Preparation Table

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

SB-215505 Related Classifications

Neurological Disease

Help & FAQs

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.

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SB-215505

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SB-215505 Related Antibodies

Recomendaciones destacadas

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

Ver todos los productos específicos de isoformas 5-HT Receptor:

Actividad biológica

Pureza y Documentación

Referencias

Revisión del cliente

SB-215505 Related Antibodies

Calculadora de molaridad

Calculadora de dilución

Complete Stock Solution Preparation Table

SB-215505 Related Classifications

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