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Merck
CN
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主要文件

安全信息

SML2152

Sigma-Aldrich

10Panx1 三氟乙酸盐

≥98% (HPLC)

别名:

10Panx trifluoroacetate salt, Trp-Arg-Gln-Ala-Ala-Phe-Val-Asp-Ser-Tyr trifluoroacetate salt, WRQAAFVDSY trifluoroacetate salt

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About This Item

经验公式（希尔记法）:
C58H79N15O16 · xC2HF3O2
CAS号:
955091-53-9
分子量:
1242.34 (free base basis)
UNSPSC代码:
12352200
NACRES:
NA.77

方案

≥98% (HPLC)

表单

film

颜色

white to beige

运输

wet ice

储存温度

−20°C

SMILES字符串

[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

应用

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.

生化/生理作用

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).

储存分类代码

11 - Combustible Solids

WGK

WGK 3

闪点(°F)

Not applicable

闪点(°C)

Not applicable

法规信息

常规特殊物品

历史批次信息供参考:

分析证书(COA)

Lot/Batch Number
0000185350
0000142387
0000185350
0000142387
0000102221

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Stimulation of soluble guanylate cyclase exerts antiinflammatory actions in the liver through a VASP/NF-?B/NLRP3 inflammasome circuit
Roger Flores-Costa, et al.
Proceedings of the National Academy of Sciences of the USA (2020)
Roger J Thompson et al.
Science (New York, N.Y.), 322(5907), 1555-1559 (2008-12-06)
Pannexin-1 (Px1) is expressed at postsynaptic sites in pyramidal neurons, suggesting that these hemichannels contribute to dendritic signals associated with synaptic function. We found that, in pyramidal neurons, N-methyl-d-aspartate receptor (NMDAR) activation induced a secondary prolonged current and dye flux
Nicholas L Weilinger et al.
Nature neuroscience, 19(3), 432-442 (2016-02-09)
Overactivation of neuronal N-methyl-D-aspartate receptors (NMDARs) causes excitotoxicity and is necessary for neuronal death. In the classical view, these ligand-gated Ca(2+)-permeable ionotropic receptors require co-agonists and membrane depolarization for activation. We report that NMDARs signal during ligand binding without activation
C Yi et al.
Cell death and differentiation, 23(10), 1691-1701 (2016-07-09)
In Alzheimer's disease (AD), astrocyte properties are modified but their involvement in this pathology is only beginning to be appreciated. The expression of connexins, proteins forming gap junction channels and hemichannels, is increased in astrocytes contacting amyloid plaques in brains
Stephani Velasquez et al.
Journal of immunology (Baltimore, Md. : 1950), 196(10), 4338-4347 (2016-04-15)
Pannexin1 (Panx1) channels are large high conductance channels found in all vertebrates that can be activated under several physiological and pathological conditions. Our published data indicate that HIV infection results in the extended opening of Panx1 channels (5-60 min), allowing
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