PA 1 dihydrochloride

• Supplier: Tocris Bioscience
• Catalog: 4076
• Prices: $199.00, $825.00
• Sizes: 10 mg, 50 mg
• Function Type: Blocker
• Chemical Name: 3,5-Diamino-6-chloro-N-[imino[[4-(2-phenyldiazenyl)phenyl]amino]methyl]-2-pyrazinecarboxamidedihydrochloride
• Formula: C18H16ClN9O.2HCl
• Molecular Weight: 482.75
• Purity: >98 %
• Description: Photoswitchable epithelial sodium channel (ENaC) blocker (IC 50 values are 90 and 390 nM for α β γ and δ β γ ENaCs, respectively, in the trans conformation). Switches conformation from cis to trans at 500 nm and trans to cis at 400 nm. Blocks ENaCs with greater efficacy in the cis conformation, in comparison to the trans conformation, in Xenopus oocytes and HEK293t cells. Partially blocks δ β γ ENaCs in the trans conformation and exhibits near maximal block of δ β γ ENaCs in the cis conformation. Amiloride derivative.

Product References

Novel retinoid X receptor antagonists: specific inhibition of retinoid synergism - Novel retinoid X receptor antagonists: specific inhibition of retinoid synergism

Takahashi B, Ohta K, Kawachi E, Fukasawa H, Hashimoto Y, Kagechika H. J Med Chem. 2002 Aug 1;45(16):3327-30.

Inhibition of mammary carcinoma cell growth by RXR is mediated by the receptor's - Inhibition of mammary carcinoma cell growth by RXR is mediated by the receptor's

Yasmin R, Kannan-Thulasiraman P, Kagechika H, Dawson MI, Noy N. J Mol Biol. 2010 Apr 16;397(5):1121-31.

Discovery of a Potent Retinoid X Receptor Antagonist Structurally Closely Related - Discovery of a Potent Retinoid X Receptor Antagonist Structurally Closely Related

Nakayama M, Yamada S, Ohsawa F, Ohta Y, Kawata K, Makishima M, Kakuta H. ACS Med Chem Lett. 2011 Sep 27;2(12):896-900.