AF-353 is a P2X3 receptor antagonist. Antagonism of the P2X3 receptor is one of the potential therapeutic strategies for the management of neuropathic pain because P2X3 receptors are predominantly localized on small to medium diameter C- and Aδ-fiber primary afferent neurons, which are related to the pain-sensing system.
CAS Number: 865305-30-2
Molecular Weight: 400.21
Chemical Name: 5-(5-iodo-4-methoxy-2-propan-2-ylphenoxy)pyrimidine-2,4-diamine
Appearance: Solid Power.
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: Soluble in DMSO
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined.
HS Tariff Code: 382200
How to use
AF-353 (Ro-4) is a highly potent inhibitor of α, β-meATP-evoked intracellular calcium flux in cell lines expressing recombinant rat and human P2X3 and human P2X2/3 channels. AF-353 (Ro-4) also blocks human P2X2/3 channel function with marginally reduced potency with a p50 of 7.3.
AF-353 (Ro-4) does not compromise oxygen levels or cardiac function. AF-353 (Ro-4) (10 mg/kg, 20 mg/kg; i.v.; for 4-6 hours) inhibits the purinergic response in both normal and spinal cord-injured (SCI) rats. AF-353 (Ro-4) (10 mg/kg, 20 mg/kg; i.v.; for 4-6 hours) also reduces the inter-contractile interval in normal but not in SCI rats; however, the frequency of non-voiding (NVC) in SCI rats is significantly reduced.
- Jung YH, Kim YO, Lin H, Cho JH, Park JH, Lee SD, Bae J, Kang KM, Kim YG, PaeAN, Ko H, Park CS, Yoon MH, Kim YC. Discovery of Potent Antiallodynic Agents for Neuropathic Pain Targeting P2X3 Receptors. ACS Chem Neurosci. 2017 Apr 6. doi:10.1021/acschemneuro.6b00401. [Epub ahead of print] PubMed PMID: 28323403.
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