AZD-7594 CAS No.:1196509-60-0

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AZD-7594 CAS No.:1196509-60-0 – A Novel and Selective Antagonist of the TRPV1 Channel

AZD-7594 is a small molecule compound developed by AstraZeneca, a global biopharmaceutical company headquartered in the UK. It belongs to the class of transient receptor potential vanilloid 1 (TRPV1) antagonists, which inhibit the function of the TRPV1 ion channel expressed in sensory neurons. TRPV1 plays a crucial role in mediating pain, inflammation, and thermoregulation in the human body. By blocking TRPV1, AZD-7594 has the potential to relieve multiple types of chronic and acute pain, without causing systemic side effects or addiction. Moreover, AZD-7594 has shown promise in treating other disorders associated with TRPV1 dysfunction, such as cough, itch, and bladder overactivity.

AZD-7594 has undergone extensive preclinical and clinical studies, which have demonstrated its safety, pharmacokinetics, and pharmacodynamics in humans. In 2019, AstraZeneca published the results of a Phase 1 trial of AZD-7594 in healthy volunteers, which showed dose-dependent and reversible effects on cold and heat pain thresholds, as well as no serious adverse events or drug interactions. The study also suggested that AZD-7594 has a favorable oral bioavailability, with a half-life of about 13 hours and an acceptable food effect. These findings support the further development of AZD-7594 as a potential therapy for pain management.

AZD-7594 has several unique features that distinguish it from other TRPV1 antagonists on the market or in development. Firstly, AZD-7594 is highly selective for TRPV1, with minimal activity on other ion channels or receptors. This selectivity enhances the specificity and safety of AZD-7594, as it reduces the risk of off-target effects or interference with physiological functions. Secondly, AZD-7594 has a distinct chemical structure and binding mode to TRPV1, which may confer superior potency and efficacy compared to other TRPV1 antagonists. For example, AZD-7594 has a nanomolar affinity to TRPV1, which is several-fold higher than some other compounds. Thirdly, AZD-7594 may have a novel mechanism of action that involves modulating the voltage-dependent activation of TRPV1, in addition to direct inhibition of the channel pore. This mechanism may provide synergistic effects on pain relief and minimize the risk of tachyphylaxis or tolerance. Fourthly, AZD-7594 may have a longer duration of action than other TRPV1 antagonists, as it accumulates in sensory neurons and remains active even after washout from the plasma.

AZD-7594 has potential applications in various fields of medicine, such as neurology, rheumatology, urology, and dermatology. It may be useful for managing chronic pain syndromes, such as osteoarthritis, neuropathic pain, fibromyalgia, and headache. It may also be effective in reducing acute pain, such as postoperative pain, dental pain, and menstrual pain. Furthermore, AZD-7594 may have a role in treating non-pain symptoms associated with TRPV1 dysfunction, such as cough due to viral or allergic causes, pruritus due to dermatitis or urticaria, and overactive bladder due to neurogenic or idiopathic causes.

As a manufacturer of AZD-7594, we can offer high-quality and low-cost bulk supplies of this compound to merchants worldwide. Our AZD-7594 meets the standards of GMP, FDA, and ISO, and has a purity of over 98%. We provide various forms of AZD-7594, such as powder, granules, capsules, tablets, and solutions, to meet the diverse needs of our customers. We also offer customized packaging, labeling, and shipping options for AZD-7594, to ensure the safe and timely delivery of the product to our clients. We guarantee the confidentiality, integrity, and reliability of our AZD-7594, and welcome inquiries and orders from all interested parties. Please feel free to contact us for more information on AZD-7594 or other products in our portfolio.

Chemical Structure : AZD-7594

CAS No.: 1196509-60-0

 

AZD-7594(AZ-13189620)

Catalog No.: URK-V652 Only Used For Lab.

AZD-7594 (AZ-13189620) is a potent, nonsteroidal, selective glucocorticoid receptor modulator (SGRM) with binding IC50 of 0.9 nM, shows no affinity for AR, PR, MR and ERα/β.

Biological Activity

AZD-7594 (AZ-13189620) is a potent, nonsteroidal, selective glucocorticoid receptor modulator (SGRM) with binding IC50 of 0.9 nM, shows no affinity for AR, PR, MR and ERα/β; demonstrates cell potentcy with IC50 of 55 nM (repression of AP-1 dependent transcription), inhibits LPS-stimulated TNF-α production in human PBMC with IC50 0.43 nM; potently inhibits lung edema in a rat model of allergic airway inflammation with inhaled EC50 of 130 uM/Kg.
Asthma
Phase 2 Clinical

Physicochemical Properties

References

1. Hemmerling M, et al. J Med Chem. 2017 Oct 26;60(20):8591-8605.

URK-V652_COA

URK-V652_SDS

URK-V652_TDS

 

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