566203-88-1 Usage
Description
AZD2098, also known as 566203-88-1, is a potent and selective agonist of the CCR4 chemokine receptor. It is an orally bioavailable compound with IC50 values ranging from 10 to 25 nM across different species. AZD2098 is particularly effective in targeting the CCR4 receptor, which plays a crucial role in the activation and migration of Th2 lymphocytes to the lungs in response to allergens. AZD2098 is inactive at other receptors such as CXCR1/2, CCR1, CCR2b, CCR5, CCR7, and CCR8, even at a concentration of 10 μM.
Uses
Used in Pharmaceutical Industry:
AZD2098 is used as a therapeutic agent for treating allergic conditions and asthma. AZD2098's ability to activate the CCR4 receptor helps in modulating the immune response and reducing inflammation in the lungs, particularly in sensitized rats.
Used in Research Applications:
AZD2098 is used as a research tool for studying the role of CCR4 in various biological processes, including immune cell trafficking, inflammation, and allergic reactions. Its high selectivity for the CCR4 receptor makes it a valuable compound for investigating the molecular mechanisms underlying these processes and for identifying potential therapeutic targets for related conditions.
Used in Drug Development:
AZD2098 serves as a lead compound in the development of new drugs targeting the CCR4 receptor. Its potent and selective agonist activity, along with its oral bioavailability, make it an attractive candidate for further optimization and development into a more effective and safer drug for treating allergic diseases and asthma.
Biochem/physiol Actions
AZD-2098 is an orally active, potent and selective CCR4 antagonist (pIC50 = 7.8/8.0/8.0/7.6 against CCL22 binding to human/mouse/rat/dog CCR4; inactive toward CXCR1/2 & CCR1/2b/5/7/8 at 10 μM) with little or no activity toward a panel of ～120 receptors/enzymes. AZD-2098 effectively inhibits chemokine-induced cellular responses in vitro (pIC50 = 7.5 against CCL22-induced calcium influx in hCCR4-expressing CHO cells; pIC50 = 6.3 against CCL17- or CCL22-induced chemotaxis of primary human Th2 cells) and exhibits efficacy against antigen-induced inflammatory response among ovalbumin-sensitized rats in vivo (Emax = 7.5 μmol/kg p.o.; 1 h before and every 12 h after antigen challenge).
References
Kindon et al. (2017), Discovery of AZD-2098 and AZD-1678, Two Potent and Bioavailable CCR4 Receptor Antagonists; ACS Med. Chem. Lett. 8 981
Check Digit Verification of cas no
The CAS Registry Mumber 566203-88-1 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 5,6,6,2,0 and 3 respectively; the second part has 2 digits, 8 and 8 respectively.
Calculate Digit Verification of CAS Registry Number 566203-88:
(8*5)+(7*6)+(6*6)+(5*2)+(4*0)+(3*3)+(2*8)+(1*8)=161
161 % 10 = 1
So 566203-88-1 is a valid CAS Registry Number.
566203-88-1Relevant articles and documents
Discovery of AZD-2098 and AZD-1678, Two Potent and Bioavailable CCR4 Receptor Antagonists
Kindon, Nicholas,Andrews, Glen,Baxter, Andrew,Cheshire, David,Hemsley, Paul,Johnson, Timothy,Liu, Yu-Zhen,McGinnity, Dermot,McHale, Mark,Mete, Antonio,Reuberson, James,Roberts, Bryan,Steele, John,Teobald, Barry,Unitt, John,Vaughan, Deborah,Walters, Iain,Stocks, Michael J.
supporting information, p. 981 - 986 (2017/09/22)
N-(5-Bromo-3-methoxypyrazin-2-yl)-5-chlorothiophene-2-sulfonamide 1 was identified as a hit in a CCR4 receptor antagonist high-throughput screen (HTS) of a subset of the AstraZeneca compound bank. As a hit with a lead-like profile, it was an excellent sta
