Application
10Panx1 trifluoroacetate salt has been used as the selective pannexin-1 mimetic inhibitory peptide to study the involvement of pannexin-1 in praliciguat (PRL) inhibition of the NACHT, LRR, and PYD domain-containing protein 3 (NLRP3) inflammasome.
Biochem/physiol Actions
Reversible pannexin-1 (panx1) channel blocker that inhibits P2X7R substrate uptake and protects neurons against NMDAR overactivation.
The pannexin-1 (panx1) extracellular sequence-derived 10panx1 functions as a reversible panx1 channel blocker (IC50 = 52 μM; human panx1-overexpressing HEK cells) that effectively inhibits ATP-induced dye-uptake in panx1 HEK cells co-expressing rat or human P2X7R (IC50 = 93 μM), as well as in murine J774 and human alveolar macrophages (Effective conc. 100-200 μM). 10panx1 (100 μM) is shown to protect rat hippocampal neurons against death induction upon NMDAR overactivation by excitotoxic concentrations of NMDA (100 μM) in cultures and ameliorate withdrawal symptoms among morphine-treated rats in vivo (10 μg/rat via intrathecal injection).
| assay | ≥98% (HPLC) |
| form | film |
| color | white to beige |
| shipped in | wet ice |
| storage temp. | −20°C |
| SMILES string | [nH]1c2c(c(c1)C[C@H](N)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(=O)N)C(=O)N[C@@H](C)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc4ccccc4)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc3ccc(cc3)O)C(=O)O)cccc2 |
| InChI | 1S/C58H79N15O16/c1-29(2)47(56(87)70-42(26-46(77)78)53(84)72-44(28-74)55(86)71-43(57(88)89)24-33-16-18-35(75)19-17-33)73-54(85)41(23-32-11-6-5-7-12-32)69-49(80)31(4)65-48(79)30(3)66-51(82)40(20-21-45(60)76)68-52(83)39(15-10-22-63-58(61)62)67-50(81)37(59)25-34-27-64-38-14-9-8-13-36(34)38/h5-9,11-14,16-19,27,29-31,37,39-44,47,64,74-75H,10,15,20-26,28,59H2,1-4H3,(H2,60,76)(H,65,79)(H,66,82)(H,67,81)(H,68,83)(H,69,80)(H,70,87)(H,71,86)(H,72,84)(H,73,85)(H,77,78)(H,88,89)(H4,61,62,63)/t30-,31-,37-,39-,40-,41-,42-,43-,44-,47-/m0/s1 |
| InChI key | JCJASTVQGSKHKZ-QZHJRRRASA-N |
