Acemetacin - CAS 53164-05-9
Not Intended for Therapeutic Use. For research use only.
Category:
Inhibitor
Product Name:
Acemetacin
Catalog Number:
53164-05-9
Synonyms:
Emflex
CAS Number:
53164-05-9
Description:
COX inhibitor; A non-steroidal anti-inflammatory drug
Molecular Weight:
415.82
Molecular Formula:
C21H18ClNO6
Quantity:
Grams-Kilos
Quality Standard:
In-house
COA:
Inquire
MSDS:
Inquire
Canonical SMILES:
CC1=C(C2=C(N1C(=O)C3=CC=C(C=C3)Cl)C=CC(=C2)OC)CC(=O)OCC(=O)O
InChI:
1S/C21H18ClNO6/c1-12-16(10-20(26)29-11-19(24)25)17-9-15(28-2)7-8-18(17)23(12)21(27)13-3-5-14(22)6-4-13/h3-9H,10-11H2,1-2H3,(H,24,25)
InChIKey:
FSQKKOOTNAMONP-UHFFFAOYSA-N
Targets:
Cox-2 | COX
Chemical Structure
CAS 53164-05-9 Acemetacin

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Reference Reading


1.Aspirin, steroidal and non-steroidal anti-inflammatory drugs for the treatment of Alzheimer's disease.
Jaturapatporn D1, Isaac MG, McCleery J, Tabet N. Cochrane Database Syst Rev. 2012 Feb 15;2:CD006378. doi: 10.1002/14651858.CD006378.pub2.
BACKGROUND: Alzheimer's disease (AD) is the most common form of dementia. The incidence of AD rises exponentially with age and its prevalence will increase significantly worldwide in the next few decades. Inflammatory processes have been suspected in the pathogenesis of the disease.
2.Acemetacin cocrystals and salts: structure solution from powder X-ray data and form selection of the piperazine salt.
Sanphui P1, Bolla G1, Nangia A1, Chernyshev V2. IUCrJ. 2014 Feb 28;1(Pt 2):136-50. doi: 10.1107/S2052252514004229. eCollection 2014.
Acemetacin (ACM) is a non-steroidal anti-inflammatory drug (NSAID), which causes reduced gastric damage compared with indomethacin. However, acemetacin has a tendency to form a less soluble hydrate in the aqueous medium. We noted difficulties in the preparation of cocrystals and salts of acemetacin by mechanochemical methods, because this drug tends to form a hydrate during any kind of solution-based processing. With the objective to discover a solid form of acemetacin that is stable in the aqueous medium, binary adducts were prepared by the melt method to avoid hydration. The coformers/salt formers reported are pyridine carboxamides [nicotinamide (NAM), isonicotinamide (INA), and picolinamide (PAM)], caprolactam (CPR), p-aminobenzoic acid (PABA), and piperazine (PPZ). The structures of an ACM-INA cocrystal and a binary adduct ACM-PABA were solved using single-crystal X-ray diffraction. Other ACM cocrystals, ACM-PAM and ACM-CPR, and the piperazine salt ACM-PPZ were solved from high-resolution powder X-ray diffraction data.
3.Proniosomal oral tablets for controlled delivery and enhanced pharmacokinetic properties of acemetacin.
Shehata TM1, Abdallah MH, Ibrahim MM. AAPS PharmSciTech. 2015 Apr;16(2):375-83. doi: 10.1208/s12249-014-0233-5. Epub 2014 Oct 16.
Free-flowing proniosomal powders of acemetacin (AC) were prepared using the slurry method and maltodextrin as carrier. Positively charged proniosomes composed of 70:20:10 of Span 60/cholesterol (Chol)/stearylamine (SA), respectively, were successively compressed into tablets using direct compression method. The tablets were characterized for weight variability, friability, hardness, drug content uniformity, and dissolution properties. The in vivo evaluation of the prepared proniosomes (powder or tablet forms) after oral administration was investigated by the determination of AC and its active metabolite indomethacin (IND) in the blood of albino rabbits. Results indicated that the increase of Chol from 10% to 20% markedly reduced the efflux of the drug. Further Chol addition from 30% to 50% led to increased AC release rates. The proniosome tablets of AC showed greater hardness and disintegration time and less friability than AC plain tablets.
4.Bilateral sacroiliitis and uveitis comorbidity: brucellosis? Ankylosing spondylitis?
Akyol L1, Aslan K2, Özgen M1, Sayarlioglu M1. BMJ Case Rep. 2015 Sep 22;2015. pii: bcr2015211461. doi: 10.1136/bcr-2015-211461.
We present a rare case of a comorbidity of sacroiliitis and brucellosis infection. A 28-year-old woman received irregular medication due to ongoing backache and hip pain for 5 years. The patient presented to our hospital for evaluation of visual loss and was diagnosed with uveitis. Sacroiliac MRI was performed to investigate the inflammatory backache and hip pain, and the aetiology of the uveitis, revealing the presence of sacroiliitis. The patient's blood test results were as follows: positive brucellosis Rose Bengal test and positive tube agglutination test with a titre of 1/640. The patient was treated with doxycycline and rifampicin for 8 weeks for the brucellosis infection, and with acemetacin for the ankylosing spondylitis. The patient's back and hip pain decreased significantly 8 weeks later; however, the uveitis was not controlled by the treatment. Therefore, anti-tumour necrosis factor (infliximab) treatment was started.