1. GPCR/G Protein
    Neuronal Signaling
  2. Dopamine Receptor
    5-HT Receptor
  3. SB-277011 hydrochloride

SB-277011 hydrochloride (Synonyms: SB-277011A hydrochloride)

Cat. No.: HY-10847B Purity: 98.22%
Handling Instructions

SB-277011 hydrochloride (SB-277011A hydrochloride) is a potent, selective, orally bioavailable and brain penetrate dopamine D3 receptor (D3R) antagonist with Ki values of 10.7 nM and 11.2 nM at rodent and human D3R, respectively. SB-277011 hydrochloride displays 80- to 100-fold selectivity over other dopamine receptors with pKis of 8.0, 6.0, <5.2, and 5.9 for D3, D2, 5-HT1B, and 5-HT1D receptors, respectively.

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

SB-277011 hydrochloride Chemical Structure

SB-277011 hydrochloride Chemical Structure

CAS No. : 215804-67-4

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10 mM * 1  mL in DMSO USD 146 In-stock
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10 mg USD 240 In-stock
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50 mg USD 600 In-stock
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100 mg USD 1020 In-stock
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Based on 1 publication(s) in Google Scholar

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Description

SB-277011 hydrochloride (SB-277011A hydrochloride) is a potent, selective, orally bioavailable and brain penetrate dopamine D3 receptor (D3R) antagonist with Ki values of 10.7 nM and 11.2 nM at rodent and human D3R, respectively. SB-277011 hydrochloride displays 80- to 100-fold selectivity over other dopamine receptors with pKis of 8.0, 6.0, <5.2, and 5.9 for D3, D2, 5-HT1B, and 5-HT1D receptors, respectively[1][2].

IC50 & Target[1]

D3 Receptor

10.7-11.2 nM (Ki)

D2 Receptor

 

5-HT1D Receptor

 

5-HT1B Receptor

 

In Vivo

SB-277011 hydrochloride has an excellent pharmacokinetic profile, exhibits oral bioavailability 43%, half-life:2.0 h, plasma clearance 19 mL/min/kg) and to be highly brain-penetrant (brain:blood ratio of 3.6:1), with a clean P450 profile in the rat[1].
SB-277011 hydrochloride (SB 277011; 3 mg/kg, p.o.) completely reverses the effects of quinelorane in the nucleus accumbens, but does not reverse the effects of quinelorane in the striatum at 93 mg/kg in rats[1].
SB-277011 (intraperitoneal injection; 12.5-25 mg/kg) significantly and dose-dependently reduces intravenous cocaine self-administration under both low fixed-ratio and progressive-ratio reinforcement conditions in rats. When it increases to 50 mg/kg, SB-277011 can significantly inhibit basal and cocaine-enhanced locomotion in rats[2].

Molecular Weight

475.02

Formula

C₂₈H₃₁ClN₄O

CAS No.

215804-67-4

SMILES

O=C(C1=CC=NC2=CC=CC=C21)N[[email protected]@H]3CC[[email protected]](CC3)CCN4CC5=C(CC4)C=C(C#N)C=C5.[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 (105.26 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1052 mL 10.5259 mL 21.0517 mL
5 mM 0.4210 mL 2.1052 mL 4.2103 mL
10 mM 0.2105 mL 1.0526 mL 2.1052 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: ≥ 2.08 mg/mL (4.38 mM); Clear solution

  • 2.

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

    Solubility: ≥ 2.08 mg/mL (4.38 mM); Clear solution

  • 3.

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

    Solubility: ≥ 2.08 mg/mL (4.38 mM); Clear solution

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

SB-277011SB-277011ASB277011SB 277011Dopamine Receptor5-HT ReceptorSerotonin Receptor5-hydroxytryptamine ReceptorInhibitorinhibitorinhibit

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SB-277011 hydrochloride
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HY-10847B
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