SB 242084 dihydrochloride

Cat. No.: HY-13409A Purity: 99.10%: FAQs
Data Sheet SDS COA Handling Instructions

SB 242084 dihydrochloride is a selective, competitive and high-affinity (pK_i=9.0) 5-HT_2C receptor antagonist (crosses the blood-brain barrier). SB 242084 dihydrochloride increases basal activity of dopaminergic neurons in the ventral tegmental area (VTA) of the midbrain and dopamine release in the vomeronasal nucleus. SB 242084 dihydrochloride also increases mitochondrial gene expression and oxidative metabolism via 5-HT_2A receptor. SB 242084 dihydrochloride 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 dihydrochloride Chemical Structure

CAS No. : 1049747-87-6

Size	Price	Stock	Quantity
Solution
10 mM * 1 mL in DMSO	USD 124	In-stock	Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL ready for reconstitution	USD 124	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 113	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 158	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 726	In-stock	Estimated Time of Arrival: December 31
100 mg		Get quote
200 mg		Get quote

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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of SB 242084 dihydrochloride:

SB 242084 In-stock

1 Publications Citing Use of MCE SB 242084 dihydrochloride

•Authorea. September 19, 2022.

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Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

5-HT_2C Receptor

9.0 (pKi)

In Vitro

SB 242084 dihydrochloride (100 nM; 45 min) exhibits antagonism of the 5-HT stimulated increase in phosphatidylinositol hydrolysis at the human 5-HT_2C receptor in SH-SY5Y cells^[1].
SB 242084 dihydrochloride (1-100 nM; 24 h) increases RPTC respiration and PGC-1α mRNA expression in RPTC^[2].

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 dihydrochloride (0.1-1 mg/kg; i.p.; single; 20 min pre-test) improves the behavior of rats in social interaction tests^[1].
SB 242084 dihydrochloride (5 mg/kg; i.p.; single; 20 min pre-test) improves mCPP-induced hypophagia in rats^[1].
SB 242084 dihydrochloride (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 dihydrochloride (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].

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

467.78

Appearance

Solid

Formula

C₂₁H₂₁Cl₃N₄O₂

CAS No.

1049747-87-6

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

-20°C, stored under nitrogen, away from moisture

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

Solvent & Solubility

In Vitro:

DMSO : ≥ 125.5 mg/mL (268.29 mM)

H₂O : < 0.1 mg/mL (ultrasonic) (insoluble)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.1378 mL	10.6888 mL	21.3776 mL
5 mM	0.4276 mL	2.1378 mL	4.2755 mL
10 mM	0.2138 mL	1.0689 mL	2.1378 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: ≥ 5 mg/mL (10.69 mM); Clear solution
2.

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 5 mg/mL (10.69 mM); Clear solution
3.

Add each solvent one by one: 10% DMSO 90% corn oil
Solubility: ≥ 5 mg/mL (10.69 mM); Clear solution

*All of the co-solvents are available by MCE.

Purity & Documentation

Purity: 99.10%

Select Batch:

Data Sheet (285 KB) SDS (393 KB)

COA (258 KB) HNMR (141 KB) RP-HPLC (138 KB) LCMS (383 KB)

Handling Instructions (2659 KB)

References

[1]. Kennett GA, et al. SB 242084, a selective and brain penetrant 5-HT2C receptor antagonist. Neuropharmacology. 1997 Apr-May;36(4-5):609-20. [Content Brief]

[2]. Harmon JL, et al. 5-HT2 Receptor Regulation of Mitochondrial Genes: Unexpected Pharmacological Effects of Agonists and Antagonists. J Pharmacol Exp Ther. 2016 Apr;357(1):1-9. [Content Brief]