Arizonin A1
* Please be kindly noted products are not for therapeutic use. We do not sell to patients.
| Category | Antibiotics |
| Catalog number | BBF-00087 |
| CAS | 108890-87-5 |
| Molecular Weight | 330.29 |
| Molecular Formula | C17H14O7 |
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Description
Arizonins are a complex of quinone antibiotics produced by Actinoplanes arizonaensis. Arizonin A1 has anti-Gram-positive bacteria activity.
Specification
| Synonyms | 2H-Furo(3,2-b)naphtho(2,3-d)pyran-2,6,11-trione, 3,3a,5,11b-tetrahydro-8-hydroxy-7-methoxy-5-methyl-, (3aR-(3aalpha,5alpha,11balpha))-; Arizonin-A1 |
| IUPAC Name | (15R)-5-hydroxy-4-methoxy-17-methyl-12,16-dioxatetracyclo[8.7.0.03,8.011,15]heptadeca-1(10),3(8),4,6-tetraene-2,9,13-trione |
| Canonical SMILES | CC1C2=C(C3C(O1)CC(=O)O3)C(=O)C4=C(C2=O)C(=C(C=C4)O)OC |
| InChI | InChI=1S/C17H14O7/c1-6-11-13(17-9(23-6)5-10(19)24-17)14(20)7-3-4-8(18)16(22-2)12(7)15(11)21/h3-4,6,9,17-18H,5H2,1-2H3/t6?,9-,17?/m1/s1 |
| InChI Key | VQAHDQIOJTXEAY-HVLHPAKUSA-N |
Properties
| Antibiotic Activity Spectrum | Gram-positive bacteria |
| Melting Point | 233°C |
Reference Reading
1. The relationship of vancomycin 24-hour AUC and trough concentration
David E Nix, Lisa E Davis, Kathryn R Matthias Am J Health Syst Pharm. 2022 Mar 21;79(7):534-539. doi: 10.1093/ajhp/zxab457.
Purpose: Prior to the 2020 release of a joint consensus guideline on monitoring of vancomycin therapy for serious methicillin-resistant Staphylococcus aureus (MRSA) infections, clinicians had escalated vancomycin doses for 2 decades while targeting trough concentrations of 15 to 20 µg/mL, leading to an increased frequency of nephrotoxicity. For MRSA infections, the 2020 guideline recommends adjusting doses to achieve a 24-hour area under the concentration-time curve (AUC) of 400 to 600 µg · h/mL; however, monitoring of trough concentrations has been entrenched for 3 decades. Calculating dose regimens based on AUC will require obtaining an increased number of vancomycin serum concentrations and, possibly, advanced software. The aim of this investigation was to determine the relationship between AUC and trough concentration and the influence of dosing regimen on goal achievement. Methods: The relationship between trough concentration and AUC was explored through derivation of an equation based on a 1-compartment model and simulations. Results: 24-hour AUC is related to dosing interval divided by half-life in a nonlinear fashion. The target trough concentration can be individualized to achieve a desired AUC range, and limiting use of large doses (>15-20 mg/kg) can protect against excessive 24-hour AUC with trough-only monitoring. Conclusion: After initially determining pharmacokinetic parameters, subsequent monitoring of AUC can be accomplished using trough concentrations only. Trough concentration may be used as a surrogate for AUC, although the acceptable target trough concentration will vary depending on dosing interval and elimination rate constant. This work included development of an AUC-trough equation to establish a patient-specific target for steady-state trough concentration.
2. Examining the policy effects of Arizona's 2016 pre-emption law on firearm suicide rates in the greater Tucson area: an observational study
Evan V Goldstein, Laura C Prater BMJ Open. 2022 May 9;12(5):e058196. doi: 10.1136/bmjopen-2021-058196.
Objective: In 2016, Arizona enacted SB 1487 to nullify Tucson's ordinance permitting the municipality to destroy confiscated and forfeited firearms and instead require the firearms to be resold to the public through an auctioneer. Our objective was to examine whether firearm suicide rates increased in Pima County (greater Tucson area) relative to other Arizona counties following the enactment of Arizona's 2016 pre-emption law. Design: An observational study of a natural policy experiment. We used a difference-in-differences approach to estimate the effects of Arizona enacting SB 1487 on firearm suicide rates in Pima County. Our statistical analyses adjusted for county-level differences in population demographics (age, gender and race) and unemployment rates, as well as a proxy for firearm availability and mental health professional shortage area status. Setting: 9 Arizona counties from 2014 to 2019. Participants: A policy group was constructed using Pima County (Tucson area) observations. A comparison group was created using data from eight other Arizona counties. 54 county-year observations were analysed. Intervention: SB 1487, which pre-empted Tucson law and allowed firearms that were seized/surrendered to law enforcement to be recirculated instead of destroyed. Outcomes and measures: Annual rates of firearm and non-firearm suicides per 100 000 persons extracted from the Centers for Disease Control and Prevention WONDER system. Results: Over the study period, comparison group counties had an average of 14.87 firearm suicides per 100 000 persons per year, compared with 11.56 firearm suicides per 100 000 persons per year in Pima County. A 1.13 increase in Pima County's firearm suicides per 100 000 persons coincided with the enactment of Arizona's 2016 pre-emption law, relative to comparison group counties over the same period. Conclusions: SB 1487 was associated with higher firearm suicide rates in Pima County relative to other areas not targeted by the law, assuming fewer firearms were destroyed and more firearms re-entered the greater Tucson area through 2019.
3. Remembering your A, B, C's: Alzheimer's disease and ABCA1
Cutler T Lewandowski, Megan S Laham, Gregory R J Thatcher Acta Pharm Sin B. 2022 Mar;12(3):995-1018. doi: 10.1016/j.apsb.2022.01.011. Epub 2022 Jan 24.
The function of ATP binding cassette protein A1 (ABCA1) is central to cholesterol mobilization. Reduced ABCA1 expression or activity is implicated in Alzheimer's disease (AD) and other disorders. Therapeutic approaches to boost ABCA1 activity have yet to be translated successfully to the clinic. The risk factors for AD development and progression, including comorbid disorders such as type 2 diabetes and cardiovascular disease, highlight the intersection of cholesterol transport and inflammation. Upregulation of ABCA1 can positively impact APOE lipidation, insulin sensitivity, peripheral vascular and blood-brain barrier integrity, and anti-inflammatory signaling. Various strategies towards ABCA1-boosting compounds have been described, with a bias toward nuclear hormone receptor (NHR) agonists. These agonists display beneficial preclinical effects; however, important side effects have limited development. In particular, ligands that bind liver X receptor (LXR), the primary NHR that controls ABCA1 expression, have shown positive effects in AD mouse models; however, lipogenesis and unwanted increases in triglyceride production are often observed. The longstanding approach, focusing on LXRβ vs. LXRα selectivity, is over-simplistic and has failed. Novel approaches such as phenotypic screening may lead to small molecule NHR modulators that elevate ABCA1 function without inducing lipogenesis and are clinically translatable.
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Bio Calculators
* Our calculator is based on the following equation:
Concentration (start) x Volume (start) = Concentration (final) x Volume (final)
It is commonly abbreviated as: C1V1 = C2V2
* Total Molecular Weight:
g/mol
Tip: Chemical formula is case sensitive. C22H30N4O √ c22h30n40 ╳
