AZD-5423 - CAS 1034148-04-3
Catalog number: 1034148-04-3
Category: Inhibitor
Please be kindly noted products are not for therapeutic use. We do not sell to patients.
Molecular Formula:
C25H21F4N3O3
Molecular Weight:
487.45
COA:
Inquire
Targets:
Others
Description:
AZD-5423 is a nonsteroidal glucocorticoid. It is used to treat respiratory diseases and in particular chronic obstructive pulmonary disease. It was developed by AstraZeneca.
Purity:
>98 %
Appearance:
Solid powder
Synonyms:
AZD-5423; AZD 5423; AZD5423; UNII-641H0Q518W; 2,2,2-Trifluoro-N-((1R,2S)-1-((1-(4-fluorophenyl)-1H-indazol-5-yl)oxy)-1-(3-methoxyphenyl)-2-propanyl)acetamide
Solubility:
10 mM in DMSO
Storage:
-20°C Freezer
MSDS:
Inquire
Application:
AZD-5423 is used to treat respiratory diseases and in particular chronic obstructive pulmonary disease.
Quality Standard:
In-house standard
Shelf Life:
2 month in rt, long time
Quantity:
Milligrams-Grams
Boiling Point:
573.8±50.0 °C | Condition: Press: 760 Torr
Density:
1.33±0.1 g/cm3 | Condition: Temp: 20 °C Press: 760 Torr
InChIKey:
FCNQMDSJHADDFT-WNSKOXEYSA-N
InChI:
InChI=1S/C25H21F4N3O3/c1-15(31-24(33)25(27,28)29)23(16-4-3-5-20(12-16)34-2)35-21-10-11-22-17(13-21)14-30-32(22)19-8-6-18(26)7-9-19/h3-15,23H,1-2H3,(H,31,33)/t15-,23-/m0/s1
Canonical SMILES:
CC(C(C1=CC(=CC=C1)OC)OC2=CC3=C(C=C2)N(N=C3)C4=CC=C(C=C4)F)NC(=O)C(F)(F)F
Current Developer:
AZD-5423 was developed by AstraZeneca.
1.Efficacy and Tolerability of an Inhaled Selective Glucocorticoid Receptor Modulator - AZD5423 - in Chronic Obstructive Pulmonary Disease Patients: Phase II Study Results.
Kuna P;Aurivillius M;Jorup C;Prothon S;Taib Z;Edsbäcker S Basic Clin Pharmacol Toxicol. 2017 Oct;121(4):279-289. doi: 10.1111/bcpt.12768. Epub 2017 Jul 17.
AZD5423 is a novel, inhaled, selective glucocorticoid receptor modulator (SGRM), which in an allergen challenge model in asthma patients improved lung function and airway hyper-reactivity. In the current trial, AZD5423 was for the first time tested in patients with chronic obstructive pulmonary disease (COPD). In this double-blind, randomized and parallel group study, we examined airway and systemic effects of two doses of AZD5423, inhaled via Turbuhaler for 12 weeks, in 353 symptomatic patients with COPD (average pre-bronchodilator forced expiratory volume in one-second (FEV1) at screening was 50-52% of predicted normal). Pre-bronchodilator FEV1 was primary variable, with other lung function parameters plus symptoms and 24-hr plasma cortisol being secondary variables. Plasma concentrations of AZD5423 were also measured. Effects were compared against placebo and a reference glucocorticoid receptor agonist control. Neither AZD5423, at doses which have shown to be efficacious in allergen-induced asthma, nor the reference control, at double the approved dose, had any clinically meaningful effect in the patient population studied in regard to lung function or markers of inflammation. Both GR modulators were well tolerated and did suppress 24-hr cortisol.
2.Selective Nonsteroidal Glucocorticoid Receptor Modulators for the Inhaled Treatment of Pulmonary Diseases.
Hemmerling M;Nilsson S;Edman K;Eirefelt S;Russell W;Hendrickx R;Johnsson E;Kärrman Mårdh C;Berger M;Rehwinkel H;Abrahamsson A;Dahmén J;Eriksson AR;Gabos B;Henriksson K;Hossain N;Ivanova S;Jansson AH;Jensen TJ;Jerre A;Johansson H;Klingstedt T;Lepistö M;Lindsjö M;Mile I;Nikitidis G;Steele J;Tehler U;Wissler L;Hansson T J Med Chem. 2017 Oct 26;60(20):8591-8605. doi: 10.1021/acs.jmedchem.7b01215. Epub 2017 Oct 12.
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.
3.A nonsteroidal glucocorticoid receptor agonist inhibits allergen-induced late asthmatic responses.
Gauvreau GM;Boulet LP;Leigh R;Cockcroft DW;Killian KJ;Davis BE;Deschesnes F;Watson RM;Swystun V;Mårdh CK;Wessman P;Jorup C;Aurivillius M;O'Byrne PM Am J Respir Crit Care Med. 2015 Jan 15;191(2):161-7. doi: 10.1164/rccm.201404-0623OC.
RATIONALE: ;Effective antiinflammatory therapies are needed for the treatment of asthma, but preferably without the systemic adverse effects of glucocorticosteroids.;OBJECTIVES: ;We evaluated the effect of an inhaled nonsteroidal glucocorticoid receptor agonist, AZD5423, on allergen-induced responses.;METHODS: ;Twenty subjects with mild allergic asthma were randomized to receive 7 days of treatment with nebulized AZD5423 (75 or 300 μg) once daily, budesonide 200 μg twice daily via Turbuhaler, or placebo in a double-blind, four-period, crossover design study. Allergen challenge was performed on Day 6.;MEASUREMENTS AND MAIN RESULTS: ;FEV1 was measured repeatedly for 7 hours after allergen challenge for early and late asthmatic responses. Sputum inflammatory cells was measured before and at 7 and 24 hours after allergen challenge, and methacholine airway responsiveness was measured before and 24 hours after allergen challenge. AZD5423 significantly attenuated the fall in FEV1 during the late asthmatic response (both doses led to an 8.7% fall) versus placebo (14% fall) (P < 0.05) with no effect of budesonide (12.5% fall) versus placebo (P > 0.05). There was no effect on the fall in FEV1 during early asthmatic response.
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