1. GPCR/G Protein Neuronal Signaling
  2. 5-HT Receptor
  3. SB 242084

SB 242084 

Cat. No.: HY-13409 Purity: 99.76%
COA Handling Instructions

SB 242084 is a selective, competitive and high-affinity (pKi=9.0) 5-HT2C receptor antagonist (crosses the blood-brain barrier). SB 242084 increases basal activity of dopaminergic neurons in the ventral tegmental area (VTA) of the midbrain and dopamine release in the vomeronasal nucleus. SB 242084 also increases mitochondrial gene expression and oxidative metabolism via 5-HT2A receptor. SB 242084 has good research potential in the negative symptoms of anxiety, depression and schizophrenia, as well as in acute organ damage.

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

SB 242084 Chemical Structure

SB 242084 Chemical Structure

CAS No. : 181632-25-7

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Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 113 In-stock
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10 mM * 1 mL in DMSO USD 113 In-stock
Solid
5 mg USD 103 In-stock
10 mg USD 144 In-stock
50 mg USD 660 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

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Top Publications Citing Use of Products

1 Publications Citing Use of MCE SB 242084

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

SB 242084 is a selective, competitive and high-affinity (pKi=9.0) 5-HT2C receptor antagonist (crosses the blood-brain barrier). SB 242084 increases basal activity of dopaminergic neurons in the ventral tegmental area (VTA) of the midbrain and dopamine release in the vomeronasal nucleus. SB 242084 also increases mitochondrial gene expression and oxidative metabolism via 5-HT2A receptor. SB 242084 has good research potential in the negative symptoms of anxiety, depression and schizophrenia, as well as in acute organ damage[1][2][3].

IC50 & Target

5-HT2C Receptor

9.0 (pKi)

In Vitro

SB 242084 (100 nM; 45 min) exhibits antagonism of the 5-HT stimulated increase in phosphatidylinositol hydrolysis at the human 5-HT2C receptor in SH-SY5Y cells[1].
SB 242084 (1-100 Nm; 24 h) increases RPTC respiration and PGC-1α mRNA expression in RPTC[2].

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

Cell Viability Assay[1]

Cell Line: SH-SY5Y cells
Concentration: 100 nM
Incubation Time: 45 min
Result: Antagonized 5-HT induced concentration-related increase in PI hydrolysis.

RT-PCR[2]

Cell Line: RPTC cells
Concentration: 1-100 nM
Incubation Time: 24 h
Result: Increased FCCP-uncoupled respiration and PGC-1α mRNA expression.
In Vivo

SB 242084 (0.1-1 mg/kg; i.p.; single; 20 min pre-test) improves the behavior of rats in social interaction tests[1].
SB 242084 (5 mg/kg; i.p.; single; 20 min pre-test) improves mCPP-induced hypophagia in rats[1].
SB 242084 (5, 10 mg/kg; i.p.; single) increases the levels of basal dialysate dopamine (DA) and dihydroxyphenylacetic acid (DOPAC) in the nucleus accumbens of rats[3].
SB 242084 (160-640 µg/kg; i.v.; single) dose-dependently and significantly increases the basal firing rate of VTA (ventral tegmental area) dopaminergic neurons, and the bursting activity is also enhanced in the same area, in vivo[3].

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

Animal Model: Male Sprague-Dawley (CD) rats[1].
Dosage: 0.1-1 mg/kg
Administration: Intraperitoneal injection; single; 20 min pre-test
Result: Significantly increased the amount of time rats spent in social interaction over 15 min under brightly lit conditions and in an unfamiliartest box.
Animal Model: Male Sprague-Dawley (CD) rats(mCPP-induced hypophagia model)[1].
Dosage: 5 mg/kg
Administration: Intraperitoneal injection; single; 20 min pre-test
Result: Significantly reduced the amount of food consumed by 23 h food-deprivedrats over a 1hr test period from the time of food presentation.
Animal Model: Rats[2].
Dosage: 5, 10 mg/kg
Administration: Intraperitoneal injection; single
Result: Significantly increased basal dialysate dopamine (DA) and dihydroxyphenylacetic acid (DOPAC) in the nucleus accumbens.
Molecular Weight

394.85

Formula

C21H19ClN4O2

CAS No.
Appearance

Solid

Color

Off-white to pink

SMILES

O=C(N1CCC2=C1C=C(Cl)C(C)=C2)NC3=CC=C(OC4=CC=CN=C4C)N=C3

Shipping

Room temperature in continental US; may vary elsewhere.

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

DMSO : ≥ 44 mg/mL (111.43 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.5326 mL 12.6630 mL 25.3261 mL
5 mM 0.5065 mL 2.5326 mL 5.0652 mL
10 mM 0.2533 mL 1.2663 mL 2.5326 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 (6.33 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (6.33 mM); Clear solution

*All of the co-solvents are available by MedChemExpress (MCE).
Purity & Documentation

Purity: 99.76%

References
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SB 242084 Related Classifications

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 242084
Cat. No.:
HY-13409
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