P2X6 Activators
P2X6 Activators are a collection of compounds that target the ion channel function of P2X6, a member of the P2X receptor family, known to be activated by adenosine triphosphate (ATP). Direct activators such as ATP itself, 2-Methylthio ATP, and P2X6 Activators are a collection of compounds that target the ion channel function of P2X6, a member of the P2X receptor family, known to be activated by adenosine triphosphate (ATP). Direct activators such as ATP itself, 2-Methylthio ATP, and BzATP enhance the receptor's activity by binding to its extracellular domain, thus inducing ion channel opening and cation influx. This influx results in cellular depolarization and the initiation of downstream signaling events. The synthetic analogs 2-Methylthio ATP and BzATP offer higher affinity binding and potency compared to ATP, leading to more robust P2X6 activation. Furthermore, the presence of metal ions such as Zinc and Magnesium can allosterically potentiate the receptor's sensitivity to ATP, suggesting a fine-tuning mechanism for P2X6 activation in the presence of these ions.
Indirect activators also play a significant role in P2X6 regulation; NF546, by stimulating P2Y receptors, promotes the release of ATP, thus creating an autocrine loop that can lead to the activation of P2X6. Probenecid functions by inhibiting pannexin-1 channels, which control ATP release, thereby increasing the availability of ATP for P2X6 activation. The selective inhibition of P2Y6 by MRS2578 can enhance P2X6 activity by preventing receptor desensitization. Additionally, compounds like PPADS and Suramin, although generally antagonistic towards P2 receptors, can have a paradoxical enhancing effect on P2X6 by preferentially inhibiting other P2X subtypes, reducing competitive binding, and thereby facilitating P2X6 receptor activation. TNP-ATP, despite being an antagonist, can act as a partial agonist on P2X6, providing subtle yet significant receptor stimulation. Lastly, Clopidogrel contributes to P2X6 activation indirectly by increasing extracellular ATP levels through the inhibition of ATP breakdown, thereby maintaining a high concentration gradient for P2X6 activation.
| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
ADP | 58-64-0 | sc-507362 | 5 g | $54.00 | ||
ATP directly activates P2X6 by binding to its extracellular domain, causing the receptor to open its ion channel and allow cation influx, leading to depolarization of the cell membrane and consequent cellular responses. | ||||||
2-Methylthioadenosine Triphosphate Sodium Salt | 100020-57-3 | sc-202910 | 10 mg | $620.00 | ||
2-Methylthioadenosine Triphosphate Sodium Salt (2-Methylthio ATP) is a potent P2X receptor agonist that binds to P2X6 with higher affinity than ATP, leading to enhanced channel opening and prolonged depolarization compared to ATP. | ||||||
NF 546 | 1006028-37-0 | sc-361275 sc-361275A | 10 mg 50 mg | $550.00 $2000.00 | ||
NF 546 is a P2Y receptor agonist that indirectly enhances P2X6 activity by increasing the release of endogenous ATP from cells, which in turn can activate P2X6 receptors in an autocrine or paracrine manner. | ||||||
Probenecid | 57-66-9 | sc-202773 sc-202773A sc-202773B sc-202773C | 1 g 5 g 25 g 100 g | $28.00 $39.00 $100.00 $277.00 | 28 | |
Probenecid is an inhibitor of pannexin-1 channels, which are often co-expressed with P2X receptors and regulate ATP release. Inhibition of pannexin-1 by Probenecid can increase extracellular ATP levels, indirectly enhancing P2X6 activity. | ||||||
Zinc | 7440-66-6 | sc-213177 | 100 g | $48.00 | ||
Zinc can act as a modulatory agent on P2X receptors. At certain concentrations, zinc has been shown to potentiate the activity of P2X6 by stabilizing the open state of the ion channel. | ||||||