Home>>ACT-389949

ACT-389949

Catalog No.GC60564

ACT-389949 is a first-in-class, potent and selective and agonist of formyl peptide receptor type 2 (FPR2)/Lipoxin A4 receptor (ALX), with an EC50 of 3 nM for FPR2/ALX internalization into monocytes.

Products are for research use only. Not for human use. We do not sell to patients.

ACT-389949 Chemical Structure

Cas No.: 1258417-54-7

Size Price Stock Qty
5mg
$352.00
In stock
10mg
$510.00
In stock
25mg
$816.00
In stock
50mg
$1,391.00
In stock
100mg
$2,318.00
In stock

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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Background

ACT-389949 is a first-in-class, potent and selective and agonist of formyl peptide receptor type 2 (FPR2)/Lipoxin A4 receptor (ALX), with an EC50 of 3 nM for FPR2/ALX internalization into monocytes. ACT-389949 has potential for the treatment of inflammatory disorders[1][2].

ACT-389949 has well tolerated. Maximum concentrations are reached around 2 hours after dosing, with a mean terminal half-life of 29.3 hours[1]. Administration of ACT-389949 results in a dose-dependent, long-lasting internalization of FPR2/ALX into leukocytes[1].

[1]. Stalder AK,et al. Biomarker-guided clinical development of the first-in-class anti-inflammatory FPR2/ALX agonist ACT-389949. Br J Clin Pharmacol. 2017 Mar;83(3):476-486. [2]. Lind S, et al. Functional and signaling characterization of the neutrophil FPR2 selective agonist Act-389949. Biochem Pharmacol. 2019 Aug;166:163-173.

Chemical Properties

Cas No. 1258417-54-7 SDF
Canonical SMILES O=C(C1=C(C2=CC=CC(C)=C2)OC(C)=N1)NC3=NN(CC4=NC(C(F)(F)C)=CO4)N=C3
Formula C20H18F2N6O3 M.Wt 428.39
Solubility DMSO: 10 mg/mL (23.34 mM; ultrasonic and adjust pH to 1 with HCl) Storage Store at -20°C,unstable in solution, ready to use.
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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1 mg 5 mg 10 mg
1 mM 2.3343 mL 11.6716 mL 23.3432 mL
5 mM 0.4669 mL 2.3343 mL 4.6686 mL
10 mM 0.2334 mL 1.1672 mL 2.3343 mL
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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3. All of the above co-solvents are available for purchase on the GlpBio website.

Reviews

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Average Rating: 5 ★★★★★ (Based on Reviews and 27 reference(s) in Google Scholar.)

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