SB 243213 hydrochloride

Name: SB 243213 hydrochloride
Brand: MedChemExpress
SKU: HY-103112
Rating: 4.5 (0 reviews)

Cat. No.: HY-103112 Purity: 98.84%: Data Sheet
COA

SDS
Handling Instructions
FAQs
Technical Support

SB 243213 hydrochloride is an orally active, selective and high-affinity 5-HT_2C receptor antagonist with a pK_i of 9.37 and a pK_b of 9.8 for human 5-HT_2C receptor. SB 243213 hydrochloride shows greater than a 100-fold selectivity over a wide range of neurotransmitter receptors, enzymes and ion channels. SB 243213 hydrochloride has improved anxiolytic profile and has the potential for schizophrenia and motor disorders.

For research use only. We do not sell to patients.

SB 243213 hydrochloride Chemical Structure

CAS No. : 200940-23-4

Size	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
25 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	In-stock	Estimated Time of Arrival: December 31
200 mg	Get quote
500 mg	Get quote

or Bulk Inquiry

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 1 Customer Validation

Other Forms of SB 243213 hydrochloride:

SB 243213 In-stock
SB 243213 dihydrochloride Get quote

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All 5-HT Receptor Isoform Specific Products:

View All Isoforms

5-HT Receptor 5-HT₁ Receptor 5-HT₂ Receptor 5-HT₃ Receptor 5-HT₄ Receptor 5-HT₅ Receptor 5-HT₆ Receptor 5-HT₇ Receptor

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[1]

Human 5-HT_2C Receptor

9.37 (pKi)

5-HT_2C Receptor

human 5-HT_1A Receptor

<5.3 (pKi)

human 5-HT_1B Receptor

5.5 (pKi)

human 5-HT_1D Receptor

6.32 (pKi)

human 5-HT_1E Receptor

<5.4 (pKi)

human 5-HT_1F Receptor

5.35 (pKi)

Human 5-HT_2A Receptor

7.01 (pKi)

human 5-HT_2B Receptor

7.2 (pKi)

Human 5-HT₆ Receptor

6.5 (pKi)

Human 5-HT₇ Receptor

5.64 (pKi)

In Vitro

SB 243213 hydrochloride shows little affinity (pK_i<6) for cloned human 5-HT_1A, 5-HT_1B, 5-HT_1E, 5- HT_1F and 5-HT₇ receptors. It shows weak affinity (pK_i<6.5) for the cloned human 5-HT_1D and D3 receptors and moderate affinity (pK_i=6.7) for the cloned human D2 receptor^[1].
SB 243213 hydrochloride shows 100-fold selectivity over a wide range of neurotransmitter receptors, enzymes and ion channels^[1].

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

In Vivo

SB 243213 hydrochloride (0.1-10 mg/kg, p.o. 1 h pre-test) dose-dependently and significantly increases the amount of time rats spent in social interaction over 15 min under brightly lit conditions and in an unfamiliar test box^[1].
SB 243213 hydrochloride (0.3 mg/kg; p.o.; 1 h pre-test) significantly increases time spent in social interaction^[1].

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

Animal Model:	Male Sprague-Dawley experimentally naive rats (220-300 g)^[1]
Dosage:	0.1, 0.3, 1, 3, 10 mg/kg
Administration:	PO; 1 hour pre-test
Result:	Dose-dependently and significantly increased the amount of time rats spent in social interaction over 15 min under brightly lit conditions and in an unfamiliar test box.

Molecular Weight

464.87

Formula

C₂₂H₂₀ClF₃N₄O₂

CAS No.

200940-23-4

Appearance

Solid

Color

Off-white to light yellow

SMILES

O=C(N1CCC2=C1C=C(C(F)(F)F)C(C)=C2)NC3=CC=C(OC4=CC=CN=C4C)N=C3.[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 : 20 mg/mL (43.02 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	2.1511 mL	10.7557 mL	21.5114 mL
5 mM	0.4302 mL	2.1511 mL	4.3023 mL
10 mM	0.2151 mL	1.0756 mL	2.1511 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.

Molarity Calculator
Dilution Calculator

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

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

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 mg/mL (4.30 mM); Clear solution

This protocol yields a clear solution of ≥ 2 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.0 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 mg/mL (4.30 mM); Clear solution

This protocol yields a clear solution of ≥ 2 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.0 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.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2 mg/mL (4.30 mM); Clear solution

This protocol yields a clear solution of ≥ 2 mg/mL (saturation unknown). 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 (20.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

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: 98.84%

Select Batch:

Data Sheet (279 KB) SDS (393 KB)

COA (256 KB) HNMR (391 KB) RP-HPLC (258 KB) LCMS (97 KB)

Handling Instructions (2659 KB)

References

[1]. Wood MD, et al. SB-243213; a selective 5-HT2C receptor inverse agonist with improved anxiolytic profile: lack of tolerance and withdrawal anxiety. Neuropharmacology. 2001 Aug;41(2):186-99. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.1511 mL	10.7557 mL	21.5114 mL	53.7785 mL
	5 mM	0.4302 mL	2.1511 mL	4.3023 mL	10.7557 mL
	10 mM	0.2151 mL	1.0756 mL	2.1511 mL	5.3778 mL
	15 mM	0.1434 mL	0.7170 mL	1.4341 mL	3.5852 mL
	20 mM	0.1076 mL	0.5378 mL	1.0756 mL	2.6889 mL
	25 mM	0.0860 mL	0.4302 mL	0.8605 mL	2.1511 mL
	30 mM	0.0717 mL	0.3585 mL	0.7170 mL	1.7926 mL
	40 mM	0.0538 mL	0.2689 mL	0.5378 mL	1.3445 mL