Apoptosis
MAO
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Product name : AZD-7594
Item : C2475
Price : 100mg, $1750;200mg, $2850;
contact : Send inquiry to: info@acesobio.com
CAS : 1196509-60-0
Molecular Weight : 606.6268
Formula : C32H32F2N4O6
Storage : at -20°C
Additional information : We offer significant discount for bulky quantity order.
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Description of:AZD-7594
AZD-7594(cas:1196509-60-0) is an inhaled selective glucocorticoid receptor (GCCR) modulator. AZD-7594 is in phase II clinical trials by AstraZeneca for the treatment of mild to moderate asthma. It is also in phase I clinical trials for the treatment of chronic obstructive pulmonary disorder (COPD). Quality control data: Quality control by 1H-NMR, 13C-NMR, HPLC and LCMS. Product will be shipped with supporting analytical data. REFERENCES1. J Med Chem. 2017 Oct 26;60(20):8591-8605. doi: 10.1021/acs.jmedchem.7b01215. Epub 2017 Oct 12.Selective Nonsteroidal Glucocorticoid Receptor Modulators for the Inhaled Treatment of Pulmonary Diseases. Hemmerling M(1), Nilsson S(2), Edman K(3), Eirefelt S(2), Russell W(2), Hendrickx R(1), Johnsson E(1), Kärrman Mårdh C(1), Berger M(4), Rehwinkel H(4), Abrahamsson A(1), Dahmén J(2), Eriksson AR(1), Gabos B(2), Henriksson K(2), Hossain N(2), Ivanova S(2), Jansson AH(2), Jensen TJ(1), Jerre A(2), Johansson H(2), Klingstedt T(2), Lepistö M(1), Lindsjö M(5), Mile I(2), Nikitidis G(2), Steele J(1), Tehler U(5), Wissler L(3), Hansson T(1). Author information: (1)Respiratory, Inflammation & Autoimmunity, Innovative Medicines and Early Development Biotech Unit, AstraZeneca , Pepparedsleden 1, Mölndal, SE 43183, Sweden. (2)AstraZeneca R&D Lund , Scheelevägen 1, Lund, SE 22187, Sweden. (3)Discovery Sciences, Innovative Medicines and Early Development Biotech Unit, AstraZeneca , Pepparedsleden 1, Mölndal, SE 43183, Sweden. (4)Medicinal Chemistry Berlin, Drug Discovery, Pharmaceuticals, Bayer AG , Berlin 13353, Germany. (5)Pharmaceutical Sciences, Innovative Medicines and Early Development Biotech Unit, AstraZeneca , Pepparedsleden 1, Mölndal, SE 43183, Sweden. A class of potent, nonsteroidal, selective indazole ether-based glucocorticoid receptor modulators (SGRMs) was developed for the inhaled treatment of respiratory diseases. Starting from an orally available compound with demonstrated anti-inflammatory activity in rat, a soft-drug strategy was implemented to ensure rapid elimination of drug candidates to minimize systemic GR activation. The first clinical candidate 1b (AZD5423) displayed a potent inhibition of lung edema in a rat model of allergic airway inflammation following dry powder inhalation combined with a moderate systemic GR-effect, assessed as thymic involution. Further optimization of inhaled drug properties provided a second, equally potent, candidate, 15m (AZD7594), that demonstrated an improved therapeutic ratio over the benchmark inhaled corticosteroid 3 (fluticasone propionate) and prolonged the inhibition of lung edema, indicating potential for once-daily treatment. |
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