BRL 54443

Cat. No.: HY-13221 Purity: 99.89%: FAQs
Data Sheet SDS COA Handling Instructions

BRL 54443 is a potent 5-HT_1E/1F receptor agonist (K_i values are 1.1 nM and 0.7 nM respectively); displays > 30-fold selectivity over other 5-HT and dopamine receptors.

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

BRL 54443 Chemical Structure

CAS No. : 57477-39-1

Size	Price	Stock	Quantity
Solid + Solvent
10 mM * 1 mL in DMSO ready for reconstitution	USD 69	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 69	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 63	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 101	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 416	In-stock	Estimated Time of Arrival: December 31
100 mg		Get quote
200 mg		Get quote

or Bulk Inquiry

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All 5-HT Receptor Isoform Specific Products:

View All Isoforms

5-HT₁ Receptor 5-HT₂ Receptor 5-HT₃ Receptor 5-HT₄ Receptor 5-HT₅ Receptor 5-HT₆ Receptor 5-HT₇ Receptor 5-HT Receptor

Biological Activity
Purity & Documentation
References
Customer Review

Description

BRL 54443 is a potent 5-HT_1E/1F receptor agonist (K_i values are 1.1 nM and 0.7 nM respectively); displays > 30-fold selectivity over other 5-HT and dopamine receptors^[1].

IC₅₀ & Target^[1]

5-HT_1E Receptor

1.1 nM (Ki)

5-HT_1F Receptor

0.7 nM (Ki)

5-HT_1A Receptor

63 nM (Ki)

5-HT_1B Receptor

126 nM (Ki)

5-HT_1D Receptor

63 nM (Ki)

5-HT_2A Receptor

1259 nM (Ki)

5-HT_2B Receptor

100 nM (Ki)

5-HT_2C Receptor

316 nM (Ki)

5-HT₆ Receptor

>10,000 nM (Ki)

5-HT₇ Receptor

>10,000 nM (Ki)

In Vitro

Despite its low affinity for other receptors [5-HT_1A (63 nM), 5-HT_1B (126 nM), 5-HT_1D (63 nM), 5-HT_2A (1259 nM), 5-HT_2B (100 nM), 5-HT_2C (316 nM), 5-HT₆ (>10,000 nM), 5-HT₇ (>10,000 nM), D₂ (501 nM), D₃ (631 nM), and α_1B-adrenoceptors (1259 nM)], BRL54443 binds with high affinity at 5-HT_1F receptors^[1].
In DG membranes, BRL54443 selectively stimulates 5-HT_1E receptors and potently inhibits forskolin-dependent cAMP production (IC₅₀=14 nM). BRL 54443 also induces contraction (-log EC₅₀=6.52)^[2].

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

In Vivo

Reduction of flinching was considered as antinociception. Ipsilateral, but not contralateral, peripheral administration of BRL54443 (5-HT(1E/1F); 3-300 microg/paw) significantly reduced formalin-induced flinching in rats^[3].

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

Molecular Weight

230.31

Appearance

Solid

Formula

C₁₄H₁₈N₂O

CAS No.

57477-39-1

SMILES

OC1=CC2=C(NC=C2C3CCN(C)CC3)C=C1

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 : ≥ 100 mg/mL (434.20 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	4.3420 mL	21.7099 mL	43.4197 mL
5 mM	0.8684 mL	4.3420 mL	8.6839 mL
10 mM	0.4342 mL	2.1710 mL	4.3420 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 (10.85 mM); Clear solution
2.

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (10.85 mM); Clear solution

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

Purity & Documentation

Purity: 99.89%

Select Batch:

Data Sheet (278 KB) SDS (392 KB)

COA (252 KB) LCMS (266 KB)

Handling Instructions (2659 KB)

References

[1]. Klein MT, et al. Toward selective drug development for the human 5-hydroxytryptamine 1E receptor: a comparison of 5-hydroxytryptamine 1E and 1F receptor structure-affinity relationships. J Pharmacol Exp Ther. 2011 Jun;337(3):860-867. [Content Brief]

[2]. McKune CM, et al. Characterization of the serotonin receptor mediating contraction in the mouse thoracic aorta and signal pathway coupling. J Pharmacol Exp Ther. 2001 Apr;297(1):88-95. [Content Brief]

[3]. Klein MT, et al. Distribution of 5-ht(1E) receptors in the mammalian brain and cerebral vasculature: an immunohistochemical and pharmacological study. Br J Pharmacol. 2012 Jun;166(4):1290-302. [Content Brief]

[4]. Granados-Soto V, et al. The role of peripheral 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E and 5-HT1F serotonergic receptors in the reduction of nociception in rats. Neuroscience. 2010 Jan 20;165(2):561-8. [Content Brief]

BRL 54443 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.

Molarity Calculator
Dilution Calculator

The molarity calculator equation

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

The dilution calculator equation

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Keywords:

BRL 5444357477-39-1BRL54443BRL-544435-HT ReceptorSerotonin Receptor5-hydroxytryptamine ReceptorInhibitorinhibitorinhibit

Your Recently Viewed Products:

Product Name

Salutation

Applicant Name *

Email Address *

Phone Number *

Organization Name *

Department *

Requested quantity *

Country or Region *

Remarks