1. GPCR/G Protein
    Neuronal Signaling
  2. 5-HT Receptor
  3. SB-224289 hydrochloride

SB-224289 hydrochloride (Synonyms: SB-224289A)

Cat. No.: HY-101105A Purity: >99.0%
Handling Instructions

SB-224289 hydrochloride is a selective 5-HT1B receptor antagonist, with anxiolytic effect.

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

SB-224289 hydrochloride Chemical Structure

SB-224289 hydrochloride Chemical Structure

CAS No. : 180084-26-8

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 118 In-stock
Estimated Time of Arrival: December 31
5 mg USD 96 In-stock
Estimated Time of Arrival: December 31
10 mg USD 168 In-stock
Estimated Time of Arrival: December 31
50 mg   Get quote  
100 mg   Get quote  

* Please select Quantity before adding items.

Customer Review

Based on 1 publication(s) in Google Scholar

Top Publications Citing Use of Products
  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

SB-224289 hydrochloride is a selective 5-HT1B receptor antagonist, with anxiolytic effect.

IC50 & Target

5-HT1B Receptor

 

In Vitro

SB-224289 has specific toxin-blocking ability and does not inhibit Cho1p. SB-224289 (100 μM-25 μM) shows consistent efficacy at producing Pap-A resistance. SB-224289 does not directly inhibit the PS synthase enzyme in this in vitro assay. Moreover, SB-224289 specifically blocks the activity of papuamides and not other membrane disruptors. SB-224289 is unable to protect wild-type cells against KF, but it is able to provide protection against TPap-A[1]. SB-224289 has a pKi of 8 at human cloned 5-HT1B receptors and displays more than 80 fold selectivity over the closely related 5-HT1D receptor and a range of other receptors. SB-224289 is a potent antagonist with pEC50 of 7.9±0.1. SB-224289 evokes a parallel rightward shift in the 5-HT concentration response curve with pA2 of 8.4±0.2. SB-224289 (100 nM and 1 μM) also significantly increases [3H]-5HT release in electrically stimulated guinea-pig brain cortex slices[3].

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

In Vivo

SB-224289 (SB 224289) alone or in combination with cocaine, increases anxiety-like behavior. SB 224289 significantly reduces the amount of locomotor activity in the cocaine-treated rats. SB 224289-treated animals spend a significantly longer time in the corners than those treated with vehicle[2]. SB 224289 is a potent antagonist with an ED50 of 3.6 mg/kg, p.o in SK&F-99101-induced hypothermia in the guinea-pig. SB 224289 (4 mg/kg, p.o) reverses sumatriptan-induced inhibition of 5-HT release showing that it is also a potent terminal 5-HT autoreceptor antagonist in vivo. SB 224289 (2-16 mg/kg, p.o) does not increase 5-HT levels in the fuinea-pig frontal cortex. However, SB 224289 (4 mg/kg, p.o) causes a significantly increase in levels of 5-HT in the fuinea-pig dentate gyrus[3].

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

Molecular Weight

557.08

Formula

C₃₂H₃₃ClN₄O₃

CAS No.

180084-26-8

SMILES

O=C(C1=CC=C(C2=CC=C(C3=NOC(C)=N3)C=C2C)C=C1)N4CCC5=C4C=C6C(OCC67CCN(C)CC7)=C5.Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

-20°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

Solvent & Solubility
In Vitro: 

DMSO : 14.29 mg/mL (25.65 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.7951 mL 8.9754 mL 17.9507 mL
5 mM 0.3590 mL 1.7951 mL 3.5901 mL
10 mM 0.1795 mL 0.8975 mL 1.7951 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

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

    Solubility: ≥ 1.43 mg/mL (2.57 mM); Clear solution

  • 2.

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

    Solubility: ≥ 1.43 mg/mL (2.57 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 1.43 mg/mL (2.57 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
Animal Administration
[2]

Ninety minutes before each animal is tested, it receives an ip injection of either 5 mg/kg SB 224289 in a vehicle of 10% Trappsol in sterile water or vehicle alone (total volume 1 mL/kg). This dosage of this drug is effective as a pharmacological agent. The rat is put back in its home cage until just before it is to be tested.

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

References

Purity: >99.0%

  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.
  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

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

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

Keywords:

SB-224289SB-224289ASB224289SB 2242895-HT ReceptorSerotonin Receptor5-hydroxytryptamine ReceptorInhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

 

Salutation

Applicant Name *

 

Email address *

Phone number *

 

Organization name *

Department *

 

Requested quantity *

Country or Region *

     

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
SB-224289 hydrochloride
Cat. No.:
HY-101105A
Quantity:
MCE Japan Authorized Agent: