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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

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
Juan Mauricio Garré et al.
The Journal of neuroscience : the official journal of the Society for Neuroscience, 36(17), 4785-4801 (2016-04-29)
We show here that the growth factor FGF-1 is proinflammatory in the spinal cord and explore the inflammatory mechanisms. FGF-1 applied to rat spinal astrocytes in culture initiates calcium signaling and induces secretion of ATP that within minutes increases membrane
Philipp Prager et al.
PloS one, 11(10), e0165653-e0165653 (2016-10-28)
Systemic hypertension is a risk factor of age-related macular degeneration (AMD), a chronic inflammatory disease. Acute hypertension is caused by increased extracellular osmolarity after intake of dietary salt (NaCl). We determined in cultured human retinal pigment epithelial (RPE) cells whether
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
Pablo Pelegrin et al.
The EMBO journal, 25(21), 5071-5082 (2006-10-13)
P2X(7) receptors are ATP-gated cation channels; their activation in macrophage also leads to rapid opening of a membrane pore permeable to dyes such as ethidium, and to release of the pro-inflammatory cytokine, interleukin-1beta (IL-1beta). It has not been known what
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