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Merck
모든 사진(2)

주요 문서

SML3656

Sigma-Aldrich

PAPTP trifluoroacetate

≥98% (HPLC)

동의어(들):

(3-(4-(4-((7-Oxo-7H-furo[3,2-g]benzopyran-4-yl)oxy)butoxy)phenyl)propyl)triphenyl phosphonium trifluoroacetate, (3-(4-(4-(7-Oxo-7H-furo[3,2-g]chromen-4-yloxy)butoxy)phenyl)propyl)triphenylphosphonium trifluoroacetate

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About This Item

실험식(Hill 표기법):
C42H38O5P · xC2HF3O2
Molecular Weight:
653.72 (free base basis)
UNSPSC 코드:
12352200
NACRES:
NA.21

Quality Level

분석

≥98% (HPLC)

양식

powder

저장 조건

desiccated

색상

white to beige

저장 온도

-10 to -25°C

SMILES string

O=C1C=CC2=C(C3=C(C=C2O1)OC=C3)OCCCCOC4=CC=C(C=C4)CCC[P+](C5=CC=CC=C5)(C6=CC=CC=C6)C7=CC=CC=C7

InChI

1S/C42H38O5P/c43-41-25-24-37-40(47-41)31-39-38(26-29-45-39)42(37)46-28-11-10-27-44-33-22-20-32(21-23-33)13-12-30-48(34-14-4-1-5-15-34,35-16-6-2-7-17-35)36-18-8-3-9-19-36/h1-9,14-26,29,31H,10-13,27-28,30H2/q+1

InChI key

MHIFCBNYOHOSHK-UHFFFAOYSA-N

생화학적/생리학적 작용

Kv1.3-selective, mitochondria-targeting Kv1.3 blocker that induces ROS-mediated cancer-selective killing both in vitro and in vivo. More effective than PAP-1.
PAPTP is a PAP-1-derivatized Kv1.3-selective potassium channel blocker with a positively charged lipophilic propyl-triphenylphosphonium (TP) moiety that allows mitochondria-targeted PAPTP delivery. Mitochondria Kv1.3 inhibition induces oxygen species (ROS)-mediated cancer-selective killing both in cultures (by 28%/69%/95% post 24-hr 0/1/10 µM PAPTP treatment of primary B-CLL; 20%/24% normal B-cell death with 0/20 µM PAPTP) and in murine orthotopic models of melanoma and pancreatic ductal adenocarcinoma in vivo (5 µmol/kg q.o.d. via i.p.). PAPTP exhibits higher anti-cancer efficacy than PAP-1 both in vitro and in vivo, and and is less affected by ultidrug resistance (MDR).

주의사항

Hygroscopic

Storage Class Code

11 - Combustible Solids

WGK

WGK 3

Flash Point (°F)

Not applicable

Flash Point (°C)

Not applicable


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시험 성적서(COA)

Lot/Batch Number

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문서 라이브러리 방문

Faye L Styles et al.
Cell death & disease, 12(4), 372-372 (2021-04-09)
Cellular energy metabolism is fundamental for all biological functions. Cellular proliferation requires extensive metabolic reprogramming and has a high energy demand. The Kv1.3 voltage-gated potassium channel drives cellular proliferation. Kv1.3 channels localise to mitochondria. Using high-resolution respirometry, we show Kv1.3

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