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Key Documents

SML2152

Sigma-Aldrich

10Panx1 trifluoroacetate salt

≥98% (HPLC)

Synonyme(s) :

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

Formule empirique (notation de Hill):
C58H79N15O16 · xC2HF3O2
Numéro CAS:
955091-53-9
Poids moléculaire :
1242.34 (free base basis)
Code UNSPSC :
12352200
Nomenclature NACRES :
NA.77

Pureté

≥98% (HPLC)

Forme

film

Couleur

white to beige

Conditions d'expédition

wet ice

Température de stockage

−20°C

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

Clé InChI

JCJASTVQGSKHKZ-QZHJRRRASA-N

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.

Actions biochimiques/physiologiques

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).

Code de la classe de stockage

11 - Combustible Solids

Classe de danger pour l'eau (WGK)

WGK 3

Point d'éclair (°F)

Not applicable

Point d'éclair (°C)

Not applicable

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Consulter la Bibliothèque de documents

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)
Soshi Seike et al.
Biochimica et biophysica acta, 1858(12), 3150-3156 (2016-11-05)
Beta-toxin produced by Clostridium perfringens is a key virulence factor of fatal hemorrhagic enterocolitis and enterotoxemia. This toxin belongs to a family of β-pore-forming toxins (PFTs). We reported recently that the ATP-gated P2X We examined the effect of Panx1 in
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
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
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
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