1. GPCR/G Protein
    Neuronal Signaling
  2. 5-HT Receptor
  3. SB 271046 Hydrochloride

SB 271046 Hydrochloride (Synonyms: SB 271046A)

Cat. No.: HY-14336A Purity: 99.06%
Handling Instructions

SB 271046 Hydrochloride (SB 271046A) is a potent, selective and orally active 5-HT6 receptor antagonist with pKi of 9.02, 8.55, and 8.81 for rat, pig and human, respectively. SB 271046 Hydrochloride is over 200 fold selective for the 5-HT6 receptor vs 55 other receptors, binding sites and ion channels. Anticonvulsant activity (EC50=0.16 μM).

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

SB 271046 Hydrochloride Chemical Structure

SB 271046 Hydrochloride Chemical Structure

CAS No. : 209481-24-3

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 152 In-stock
Estimated Time of Arrival: December 31
10 mg USD 138 In-stock
Estimated Time of Arrival: December 31
50 mg USD 528 In-stock
Estimated Time of Arrival: December 31
100 mg   Get quote  
200 mg   Get quote  

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Description

SB 271046 Hydrochloride (SB 271046A) is a potent, selective and orally active 5-HT6 receptor antagonist with pKi of 9.02, 8.55, and 8.81 for rat, pig and human, respectively. SB 271046 Hydrochloride is over 200 fold selective for the 5-HT6 receptor vs 55 other receptors, binding sites and ion channels. Anticonvulsant activity (EC50=0.16 μM)[1].

IC50 & Target

5-HT6 Receptor

8.92-9.02 (pKi)

5-HT1D Receptor

6.55 (pKi)

5-HT1A Receptor

6.35 (pKi)

5-HT1B Receptor

6.05 (pKi)

5-HT1F Receptor

5.95 (pKi)

5-HT2A Receptor

5.62 (pKi)

5-HT2B Receptor

5.41 (pKi)

5-HT7 Receptor

5.39 (pKi)

5-HT4 Receptor

5.27 (pKi)

5-HT1E Receptor

<4.99 (pKi)

Human 5-HT2C Receptor

5.73 (pKi)

In Vitro

SB 271046 Hydrochloride (SB 271046A) shows pKi values of 6.55, 6.35, 6.27, 6.05, 5.95, 5.76, 5.73, 5.62, 5.55, 5.41, 5.39, 5.27 and < 4.99 at 5-HT1D, 5-HT1A, D3, 5-HT1B, 5-HT1F, α1B, 5-HT2C, 5-HT2A, D2, 5-HT2B, 5-HT7, 5-HT4 and 5-HT1E respectively. SB-271046 Hydrochloride competitively antagonizes 5-HT-induced stimulation of adenylyl cyclase activity with a pA2 of 8.71[1].

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

In Vivo

SB 271046 Hydrochloride (10 mg/kg; p.o.) produces an increase in seizure threshold over a wide-dose range in the rat maximal electroshock seizure threshold (MEST) test, with a minimum effective dose of ⩽0.1 mg/kg p.o. and maximum effect at 4 h post-dose[1].

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

Animal Model: Male Sprague Dawley rats[1]
Dosage: 10 mg/kg
Administration: P.o.
Result: Produced an increase in seizure threshold over a wide-dose range in the rat maximal electroshock seizure threshold (MEST) test, with a minimum effective dose of ⩽0.1 mg kg−1 p.o. and maximum effect at 4 h post-dose. The level of anticonvulsant activity achieved correlated well with the blood concentrations of SB-271046 (EC50 of 0.16 μM) and brain concentrations of 0.01-0.04 μM at Cmax.
Molecular Weight

488.45

Formula

C₂₀H₂₃Cl₂N₃O₃S₂

CAS No.

209481-24-3

SMILES

ClC1=CC2=C(C=C1)SC(S(=O)(NC3=CC=C(C(N4CCNCC4)=C3)OC)=O)=C2C.[H]Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (102.36 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.0473 mL 10.2365 mL 20.4729 mL
5 mM 0.4095 mL 2.0473 mL 4.0946 mL
10 mM 0.2047 mL 1.0236 mL 2.0473 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: ≥ 2.5 mg/mL (5.12 mM); Clear solution

  • 2.

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

    Solubility: ≥ 2.5 mg/mL (5.12 mM); Clear solution

  • 3.

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

    Solubility: ≥ 2.5 mg/mL (5.12 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

SB 271046SB 271046ASB271046SB-2710465-HT ReceptorSerotonin Receptor5-hydroxytryptamine ReceptorselectiveoralchannelsanticonvulsantMESTtestInhibitorinhibitorinhibit

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Product Name:
SB 271046 Hydrochloride
Cat. No.:
HY-14336A
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