AC-264613 | CAS# 1051487-82-1 | First agonist of the GPCR PAR2

AC-264613
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WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 551012

CAS#: 1051487-82-1

Description: AC-264613 is the first agonist of the G-protein-coupled receptor (GPCR) protease activated receptor 2 (PAR2). AC-264613 suppresses interferon regulatory factor 5 and decreases interleukin-12p40 production by lipopolysaccharide-stimulated macrophages. AC-264613 activated PAR2 signaling in cellular proliferation assays, phosphatidylinositol hydrolysis assays, and Ca(2+) mobilization assays, with potencies ranging from 30 to 100 nM.

Chemical Structure

AC-264613

CAS# 1051487-82-1

Instruction

Theoretical Analysis

MedKoo Cat#: 551012
Name: AC-264613
CAS#: 1051487-82-1
Chemical Formula: C19H18BrN3O2
Exact Mass: 399.06
Molecular Weight: 400.276
Elemental Analysis: C, 57.01; H, 4.53; Br, 19.96; N, 10.50; O, 7.99

Price and Availability

Size	Price	Availability
10mg	USD 260	2 Weeks
25mg	USD 520	2 Weeks
50g	USD 840	2 Weeks
Bulk inquiry Welcome, Customer: Please do not inquire quote if your intended use is for a patient since our products are for research use and for chemical synthesis use, not for human use . For in-stock products, we listed price in the web page. You may inquire prices for which sizes were not listed. If no price is listed, this means the product is not in stock at the moment, which may be available via custom synthesis. For cost-effective reason, minimum order of 1g is requested (typically very expensive). The lead time is usually 2-4 months. Quote of less than 1g will not be provided. MedKoo may not offer quote for below reasons: (1) current available synthetic method appears to be extremely expensive which is obviously not affordable to most customers; (2) Key raw material to make the product is temporally not available; (3) DEA controlled substances; (4) the product is under patent protection in customer’s country.

Synonym: AC-264613; AC 264613; AC264613

IUPAC/Chemical Name: (3R,4S)-rel-2-Oxo-4-phenyl-3-pyrrolidinecarboxylic acid 2-[1-(3-bromophenyl)ethylidene]hydrazide

InChi Key: RQKXQCSEZPQBNZ-CBCLUANDSA-N

InChi Code: InChI=1S/C19H18BrN3O2/c1-12(14-8-5-9-15(20)10-14)22-23-19(25)17-16(11-21-18(17)24)13-6-3-2-4-7-13/h2-10,16-17H,11H2,1H3,(H,21,24)(H,23,25)/b22-12+/t16-,17-/m1/s1

SMILES Code: O=C([C@H]1C(NC[C@@H]1C2=CC=CC=C2)=O)N/N=C(C3=CC=CC(Br)=C3)\C

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

More Info:

Instruction:

View handling instruction

Biological target:
In vitro activity:
In vivo activity:

Preparing Stock Solutions

The following data is based on the product molecular weight 400.28 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

Formulation protocol:
In vitro protocol:
In vivo protocol:

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1: Cosimi E, Saadi J, Wennemers H. Stereoselective Synthesis of α-Fluoro-γ-nitro Thioesters under Organocatalytic Conditions. Org Lett. 2016 Dec 2;18(23):6014-6017. Epub 2016 Nov 11. PubMed PMID: 27934387.

2: Yamaguchi R, Yamamoto T, Sakamoto A, Ishimaru Y, Narahara S, Sugiuchi H, Yamaguchi Y. 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. doi: 10.1002/cbin.10589. Epub 2016 Mar 3. PubMed PMID: 26833899.

3: Ma JN, Burstein ES. The protease activated receptor 2 (PAR2) polymorphic variant F240S constitutively activates PAR2 receptors and potentiates responses to small-molecule PAR2 agonists. J Pharmacol Exp Ther. 2013 Dec;347(3):697-704. doi: 10.1124/jpet.113.208744. Epub 2013 Sep 27. PubMed PMID: 24078870.

4: Gardell LR, Ma JN, Seitzberg JG, Knapp AE, Schiffer HH, Tabatabaei A, Davis CN, Owens M, Clemons B, Wong KK, Lund B, Nash NR, Gao Y, Lameh J, Schmelzer K, Olsson R, Burstein ES. Identification and characterization of novel small-molecule protease-activated receptor 2 agonists. J Pharmacol Exp Ther. 2008 Dec;327(3):799-808. doi: 10.1124/jpet.108.142570. Epub 2008 Sep 3. PubMed PMID: 18768780.

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