AC-264613

Name: AC-264613
Brand: MedChemExpress
SKU: HY-14351
Rating: 4.5 (1 reviews)

Cat. No.: HY-14351 Purity: 98.3%: FAQs
Data Sheet SDS COA Handling Instructions

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AC-264613 is a potent and selective protease-activated receptor (PAR-2) agonist with a pEC₅₀ of 7.5.

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

AC-264613 Chemical Structure

CAS No. : 1051487-82-1

Size	Price	Stock	Quantity
1 mg	USD 105	In-stock	Estimated Time of Arrival: December 31
5 mg	USD 290	In-stock	Estimated Time of Arrival: December 31
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50 mg		Get quote

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Customer Review

Based on 1 publication(s) in Google Scholar

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Biological Activity
Purity & Documentation
References
Customer Review

Description

AC-264613 is a potent and selective protease-activated receptor (PAR-2) agonist with a pEC₅₀ of 7.5^[1].

IC₅₀ & Target

pEC50: 7.5 (PAR-2)^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
HEK-293T	EC₅₀	30 nM Compound: 12, AC-264613	Agonist activity at human PAR2 expressed in HEK293T cells assessed as stimulation of phosphatidylinositol hydrolysis after 45 mins by scintillation counting analysis Agonist activity at human PAR2 expressed in HEK293T cells assessed as stimulation of phosphatidylinositol hydrolysis after 45 mins by scintillation counting analysis	[PMID: 23895492]
HEK-293T	EC₅₀	30 nM Compound: 12, AC-264613	Agonist activity at human PAR2 expressed in HEK293T cells assessed as stimulation of cell proliferation after 5 days by beta-galactosidase assay Agonist activity at human PAR2 expressed in HEK293T cells assessed as stimulation of cell proliferation after 5 days by beta-galactosidase assay	[PMID: 23895492]
HEK-293T	EC₅₀	30 nM Compound: 12, AC-264613	Agonist activity at human PAR2 expressed in HEK293T cells assessed as increase in intracellular calcium level by bioluminescence assay Agonist activity at human PAR2 expressed in HEK293T cells assessed as increase in intracellular calcium level by bioluminescence assay	[PMID: 23895492]

In Vitro

AC-264613 (10 μM; for 6 hours) causes a decrease of IRF5 expression and also significantly reduces p53 protein expression in macrophages^[2].

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

Western Blot Analysis^[2]

Cell Line:	Granulocyte-macrophage colony-stimulating factor (GM-CSF)-dependent macrophages
Concentration:	10 μM
Incubation Time:	6 hours
Result:	Significantly decreased IRF5 expression and reduced p53 protein levels.

In Vivo

AC-264613 exhibits moderate elimination half-live (T_1/2=2.5±2.0 h) following i.p. administration (10 mg/kg) in male Sprague-Dawley rats^[3].

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

Molecular Weight

400.27

Formula

C₁₉H₁₈BrN₃O₂

CAS No.

1051487-82-1

Appearance

Solid

Color

White to off-white

SMILES

O=C(N/N=C(C1=CC=CC(Br)=C1)\C)[C@H]2[C@@H](CNC2=O)C3=CC=CC=C3

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

-20°C, sealed storage, away from moisture

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

Solvent & Solubility

In Vitro:

DMSO : ≥ 40 mg/mL (99.93 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.4983 mL	12.4916 mL	24.9831 mL
5 mM	0.4997 mL	2.4983 mL	4.9966 mL
10 mM	0.2498 mL	1.2492 mL	2.4983 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

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(per animal)

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Calculation results:

Working solution concentration: mg/mL

Purity & Documentation

Purity: 98.3%

Select Batch:

Data Sheet (275 KB) SDS (251 KB)

COA (252 KB) Elemental Analysis Report (110 KB)

Handling Instructions (2659 KB)

References

[1]. Jimmi Gerner Seitzberg, et al. Discovery of potent and selective small-molecule PAR-2 agonists. J Med Chem. 2008 Sep 25;51(18):5490-3. [Content Brief]

[2]. Rui Yamaguchi, et al. A protease-activated receptor 2 agonist (AC-264613) suppresses interferon regulatory factor 5 and decreases interleukin-12p40 production by lipopolysaccharide-stimulated macrophages: Role of p53. Cell Biol Int. 2016 Jun;40(6):629-41 [Content Brief]

[3]. Luis R Gardell, et al. Identification and characterization of novel small-molecule protease-activated receptor 2 agonists. J Pharmacol Exp Ther. 2008 Dec;327(3):799-808. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.4983 mL	12.4916 mL	24.9831 mL	62.4578 mL
	5 mM	0.4997 mL	2.4983 mL	4.9966 mL	12.4916 mL
	10 mM	0.2498 mL	1.2492 mL	2.4983 mL	6.2458 mL
	15 mM	0.1666 mL	0.8328 mL	1.6655 mL	4.1639 mL
	20 mM	0.1249 mL	0.6246 mL	1.2492 mL	3.1229 mL
	25 mM	0.0999 mL	0.4997 mL	0.9993 mL	2.4983 mL
	30 mM	0.0833 mL	0.4164 mL	0.8328 mL	2.0819 mL
	40 mM	0.0625 mL	0.3123 mL	0.6246 mL	1.5614 mL
	50 mM	0.0500 mL	0.2498 mL	0.4997 mL	1.2492 mL
	60 mM	0.0416 mL	0.2082 mL	0.4164 mL	1.0410 mL
	80 mM	0.0312 mL	0.1561 mL	0.3123 mL	0.7807 mL

AC-264613 Related Classifications

Inflammation/Immunology

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.

Keywords:

AC-2646131051487-82-1AC264613AC 264613Protease Activated Receptor (PAR)Thrombin receptorsInhibitorinhibitorinhibit

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AC-264613

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Complete Stock Solution Preparation Table

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