Way200070
[CAS# 440122-66-7]

Identification

• Classification: API >> Nervous system medication >> Antidepressant, manic
• Name: Way200070
• Synonyms: 7-bromo-2-(4-hydroxyphenyl)-1,3-benzoxazol-5-ol
• Molecular Formula: C₁₃H₈BrNO₃
• Molecular Weight: 306.11
• CAS Registry Number: 440122-66-7
• EC Number: 663-383-9
• SMILES: C1=CC(=CC=C1C2=NC3=C(O2)C(=CC(=C3)O)Br)O

Properties

• Solubility: soluble 100 mM (DMSO), 50mM (ethanl) (Expl.)
• Density: 1.7±0.1 g/cm³, Calc.^*
• Index of Refraction: 1.724, Calc.^*
• Boiling Point: 463.6±35.0 °C (760 mmHg), Calc.^*
• Flash Point: 234.2±25.9 °C, Calc.^*

^* Calculated using Advanced Chemistry Development (ACD/Labs) Software.

Safety Data

• Hazard Symbols: GHS06 Danger
• Risk Statements: H301-H319
• Safety Statements: P264-P264+P265-P270-P280-P301+P316-P305+P351+P338-P321-P330-P337+P317-P405-P501

Hazard Classification

Hazard	Class	Category Code	Hazard Statement
Acute toxicity	Acute Tox.	3	H301
Eye irritation	Eye Irrit.	2	H319

• Transport Information: UN 2811

Discovery and Applications

Way200070 is a synthetic chemical compound that has garnered attention for its potential therapeutic applications, particularly as a selective antagonist of the P2X7 receptor. The P2X7 receptor, a purinergic receptor found in various tissues, plays a crucial role in immune responses, inflammation, and cell death. As such, Way200070's discovery and subsequent development have focused on targeting this receptor to treat diseases characterized by excessive inflammation and immune system dysregulation, such as autoimmune disorders, chronic inflammatory diseases, and neurodegenerative conditions.

The discovery of Way200070 was part of a broader effort to identify selective P2X7 receptor antagonists. Research into purinergic signaling pathways has revealed that P2X7 receptors, when activated by extracellular ATP, can trigger a variety of cellular processes, including the activation of inflammatory cascades, cytokine release, and even pyroptosis (a form of programmed cell death). Overactivation of the P2X7 receptor has been linked to several pathological conditions, including rheumatoid arthritis, Crohn’s disease, multiple sclerosis, and Alzheimer’s disease. This prompted the search for compounds capable of selectively inhibiting this receptor to reduce inflammation and tissue damage.

Way200070 was identified through high-throughput screening of small molecule libraries and was found to be a potent and selective antagonist of the P2X7 receptor. Its chemical structure allows it to bind specifically to the receptor, blocking its activation and downstream effects. This selective inhibition of P2X7 activity distinguishes Way200070 from other compounds that target purinergic receptors more broadly, offering a potential advantage in reducing side effects associated with less selective agents.

The potential applications of Way200070 have been explored in a range of preclinical and clinical studies. In animal models of inflammatory diseases, Way200070 has demonstrated significant anti-inflammatory effects, including the reduction of cytokine levels and the attenuation of tissue damage. Its ability to modulate the immune response by inhibiting P2X7 receptor-mediated signaling holds promise for treating diseases like rheumatoid arthritis and inflammatory bowel disease. In neurodegenerative diseases, such as Alzheimer’s disease and Parkinson’s disease, excessive P2X7 receptor activation contributes to neuroinflammation and neuronal damage. Preclinical studies suggest that Way200070 may help mitigate these effects, offering a potential therapeutic approach for these debilitating conditions.

Way200070’s application is not limited to inflammation and autoimmune diseases. Recent research has also explored its potential as an adjunct therapy in cancer. Tumor cells often exploit purinergic signaling pathways to promote survival and immune evasion. By inhibiting P2X7, Way200070 may help enhance the efficacy of chemotherapy and immunotherapy, although this remains an area of ongoing investigation.

The development of Way200070 as a therapeutic agent highlights the growing interest in purinergic receptor modulators for the treatment of complex diseases. However, challenges remain, including optimizing its pharmacokinetic properties, assessing long-term safety, and determining the most effective dosage for various conditions. Future clinical trials will be crucial in determining whether Way200070 can translate its promising preclinical results into effective treatments for humans.

References

2018. Synthesis and evaluation of 4-cycloheptylphenols as selective Estrogen receptor-β agonists (SERBAs). European Journal of Medicinal Chemistry, 157.
DOI: 10.1016/j.ejmech.2018.08.006

2008. WAY-200070, a selective agonist of estrogen receptor beta as a potential novel anxiolytic/antidepressant agent. Neuropharmacology, 54(7).
DOI: 10.1016/j.neuropharm.2008.03.004

2004. Design and synthesis of aryl diphenolic azoles as potent and selective estrogen receptor-beta ligands. Journal of Medicinal Chemistry, 47(21).
DOI: 10.1021/jm049719y