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G3416

Sigma-Aldrich

5′-Guanidinonaltrindole di(trifluoroacetate) salt hydrate

solid, ≥98% (HPLC)

동의어(들):

GNTI

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About This Item

실험식(Hill 표기법):
C27H29N5O3 · 2C2HF3O2 · xH2O
CAS Number:
219655-57-9
Molecular Weight:
699.60 (anhydrous basis)
MDL number:
MFCD29923417
UNSPSC 코드:
12352202
PubChem Substance ID:
24278454
NACRES:
NA.77
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Quality Level

100

분석

≥98% (HPLC)

양식

solid

solubility

H2O: 30 mg/mL

저장 온도

2-8°C

유전자 정보

human ... OPRK1(4986)

애플리케이션

5′-Guanidinonaltrindole di(trifluoroacetate) salt hydrate (GNTI) has been used as a selective κ opioid receptor antagonist:
  • to study the influence of opioid receptor types on the anti-hyperalgesic effect of dipeptidyl peptidase 4 (DPP4) inhibitors in inflammation[1]
  • to study the role of κ opioid receptor in the forebrain-dependent associative task, Whisker-Trace Eyeblink conditioning (WTEB)[2]
  • to validate its inhibitory actions on Akt kinase activities[3]

생화학적/생리학적 작용

5′-Guanidinonaltrindole di(trifluoroacetate) (GNTI) is a 5‘-guanidine derivative[4] and a selective κ opiate receptor antagonist.[1][5] It is five-fold more potent and 500-fold more selective than norbinaltorphimine (nor-BNI) for the κ opioid receptor in smooth muscle preparations.[5]

특징 및 장점

This compound is featured on the Opioid Receptors page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.

법적 정보

Sold under US Patent No. 6,500,824.

Storage Class Code

11 - Combustible Solids

WGK

WGK 3

Flash Point (°F)

Not applicable

Flash Point (°C)

Not applicable

개인 보호 장비

Eyeshields, Gloves, type N95 (US)

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시험 성적서(COA)

Lot/Batch Number
065K4610
096K4605
103K4605
060K4610

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문서 라이브러리 방문

Pathology and glia type specific changes of the DPP4 activity in the spinal cord contributes to the development and maintenance of hyperalgesia and shapes opioid signalling in chronic pain states
KiralyK, et al.
Scientific reports (2017)
Ryan Loh et al.
Behavioural brain research, 323, 1-10 (2017-01-26)
Previous work from our laboratory has shown that nonspecific kappa opioid receptor (KOR) antagonism in primary somatosensory cortex (S1) can inhibit acquisition for the forebrain-dependent associative task, Whisker-Trace Eyeblink conditioning (WTEB). Although studies have demonstrated that KOR activation can alter
Pathology and glia type specific changes of the DPP4 activity in the spinal cord contributes to the development and maintenance of hyperalgesia and shapes opioid signalling in chronic pain states
KiralyK, et al.
Scientific Reports (2017)
R M Jones et al.
European journal of pharmacology, 396(1), 49-52 (2000-05-24)
5'-Guanidinonaltrindole (GNTI) possesses 5-fold greater opioid antagonist potency (K(e)=0.04 nM) and an order of magnitude greater selectivity (selectivity ratios >500) than the prototypical kappa-opioid receptor antagonist, norbinaltorphimine, in smooth muscle preparations. Binding and functional studies conducted on cloned human opioid
C T Chan et al.
Molecular imaging and biology, 11(3), 144-158 (2008-12-03)
Protein phosphorylation mediated by protein kinases controls numerous cellular processes. A genetically encoded, generalizable split firefly luciferase (FL)-assisted complementation system was developed for noninvasive monitoring phosphorylation events and efficacies of kinase inhibitors in cell culture and in small living subjects
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