Ugrás a tartalomra
Merck

SML2304

Sigma-Aldrich

Clozapine N-oxide hydrochloride

≥98% (HPLC), powder, muscarinic DREADD activator

Szinonimák:

Clozapine N-oxide hydrochloride, 8-Chloro-11-(4-methyl-1-piperazinyl)-5H-dibenzo[b,e](1,4)diazepine N-oxide, hydrochloride salt

Bejelentkezésa Szervezeti és Szerződéses árazás megtekintéséhez


About This Item

Tapasztalati képlet (Hill-képlet):
C18H19ClN4O · xHCl
CAS-szám:
Molekulatömeg:
342.82 (free base basis)
UNSPSC kód:
12352119
NACRES:
NA.77

product name

Clozapine N-oxide hydrochloride, ≥98% (HPLC), Water soluble Clozapine N-oxide

biológiai forrás

synthetic

Teszt

≥98% (HPLC)

form

powder

tárolási körülmény

desiccated

oldhatóság

DMSO: 40 mg/mL
water: 40 mg/mL

kiszállítva

ambient

tárolási hőmérséklet

2-8°C

SMILES string

ClC1=CC2=C(NC(C=CC=C3)=C3C(N4CC[N+]([O-])(C)CC4)=N2)C=C1.[xHCl]

InChI

1S/C18H19ClN4O/c1-23(24)10-8-22(9-11-23)18-14-4-2-3-5-15(14)20-16-7-6-13(19)12-17(16)21-18/h2-7,12,20H,8-11H2,1H3

Nemzetközi kémiai azonosító kulcs

OGUCZBIQSYYWEF-UHFFFAOYSA-N

Általános leírás

Clozapine N-oxide hydrochloride is a water soluble form of Clozapine N-oxide (CNO) (Sigma cat# C0832). CNO is a pharmacologically inert metabolite of the atypical anti-psychotic drug clozapine. CNO is a ligand for the engineered Gq protein coupled receptors (GPCRs) in the chemogenetic Designer Receptors Exclusively Activated by Designer Drug (DREADD). The typical use of DREADD is testing, enhancing neuronal firing and activating Gq signaling in neuronal and non-neuronal cells.

The selective targeting of DREADD systems to cell population can be achieved by using a cell type-specific promoter to drive DREADD expression, and the expression of this promoter can be further controlled using a recombinase-based system. DREADDs possess a low affinity for endogenous ligands and little constitutive activity, but may be activated by synthetic compounds such as CNO.

DREADD systems are activated by low nM concentrations of CNO and mobilize intracellular calcium. CNO appears to be pharmacologically and behaviorally inert in mice and rats when administered at the recommended doses (generally 0.1–3 mg/kg). CNO is commonly administrated via injection but also can be mixed into food chow or drinking water.

Egyéb megjegyzések

This is not a pharmaceutical grade product.

Piktogramok

Skull and crossbones

Figyelmeztetés

Danger

Figyelmeztető mondatok

Veszélyességi osztályok

Acute Tox. 3 Oral - STOT SE 3

Célzott szervek

Central nervous system

Tárolási osztály kódja

6.1C - Combustible acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects

WGK

WGK 3

Lobbanási pont (F)

Not applicable

Lobbanási pont (C)

Not applicable


Analitikai tanúsítványok (COA)

Analitikai tanúsítványok (COA) keresése a termék sarzs-/tételszámának megadásával. A sarzs- és tételszámok a termék címkéjén találhatók, a „Lot” vagy „Batch” szavak után.

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Georgia M Alexander et al.
Neuron, 63(1), 27-39 (2009-07-18)
Examining the behavioral consequences of selective CNS neuronal activation is a powerful tool for elucidating mammalian brain function in health and disease. Newly developed genetic, pharmacological, and optical tools allow activation of neurons with exquisite spatiotemporal resolution; however, the inaccessibility
Jean-Marc Guettier et al.
Proceedings of the National Academy of Sciences of the United States of America, 106(45), 19197-19202 (2009-10-28)
Impaired functioning of pancreatic beta cells is a key hallmark of type 2 diabetes. beta cell function is modulated by the actions of different classes of heterotrimeric G proteins. The functional consequences of activating specific beta cell G protein signaling
Michael J Krashes et al.
The Journal of clinical investigation, 121(4), 1424-1428 (2011-03-03)
Several different neuronal populations are involved in regulating energy homeostasis. Among these, agouti-related protein (AgRP) neurons are thought to promote feeding and weight gain; however, the evidence supporting this view is incomplete. Using designer receptors exclusively activated by designer drugs
Blaine N Armbruster et al.
Proceedings of the National Academy of Sciences of the United States of America, 104(12), 5163-5168 (2007-03-16)
We evolved muscarinic receptors in yeast to generate a family of G protein-coupled receptors (GPCRs) that are activated solely by a pharmacologically inert drug-like and bioavailable compound (clozapine-N-oxide). Subsequent screening in human cell lines facilitated the creation of a family
Daniel J Urban et al.
Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology, 41(5), 1404-1415 (2015-09-19)
Elucidating how the brain's serotonergic network mediates diverse behavioral actions over both relatively short (minutes-hours) and long period of time (days-weeks) remains a major challenge for neuroscience. Our relative ignorance is largely due to the lack of technologies with robustness

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