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Merck

H127

p-Fluorohexahydro-sila-difenidol hydrochloride

powder, ≥98% (HPLC)

Sinonimo/i:

Cyclohexyl-(4-fluorophenyl)-(3-N-piperidinopropyl)silanol hydrochloride, P-F-HHSiD hydrochloride

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10 MG

CHF 313.00

CHF 313.00


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Informazioni su questo articolo

Formula empirica (notazione di Hill):
C20H32FNOSi · HCl
Numero CAS:
Peso molecolare:
386.02
NACRES:
NA.77
PubChem Substance ID:
UNSPSC Code:
12352200
MDL number:

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Nome del prodotto

p-Fluorohexahydro-sila-difenidol hydrochloride, powder, ≥98% (HPLC)

InChI

1S/C20H32FNOSi.ClH/c21-18-10-12-20(13-11-18)24(23,19-8-3-1-4-9-19)17-7-16-22-14-5-2-6-15-22;/h10-13,19,23H,1-9,14-17H2;1H

SMILES string

Cl[H].O[Si](CCCN1CCCCC1)(C2CCCCC2)c3ccc(F)cc3

InChI key

JMTYYLMGSBSPPK-UHFFFAOYSA-N

assay

≥98% (HPLC)

form

powder

color

white to beige

solubility

H2O: slightly soluble 1.5 mg/mL
45% (w/v) aq 2-hydroxypropyl-β-cyclodextrin: >14 mg/mL
ethanol: soluble

Quality Level

Gene Information

human ... CHRM3(1131)

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SML2324SML0897H1512
Haloperidol powder

Sigma-Aldrich

H1512

Haloperidol

assay

≥98% (HPLC)

assay

≥98% (HPLC)

assay

≥98% (HPLC)

assay

-

form

powder

form

powder

form

powder

form

powder

Quality Level

100

Quality Level

-

Quality Level

100

Quality Level

200

solubility

H2O: slightly soluble 1.5 mg/mL, ethanol: soluble, 45% (w/v) aq 2-hydroxypropyl-β-cyclodextrin: >14 mg/mL

solubility

DMSO: 2 mg/mL, clear

solubility

DMSO: 5 mg/mL, clear (warmed)

solubility

45% (w/v) aq 2-hydroxypropyl-β-cyclodextrin: 0.39 mg/mL, 0.1 M HCl: 3 mg/mL, DMSO: soluble, H2O: insoluble, ethanol: soluble

color

white to beige

color

white to beige

color

white to beige

color

white

Gene Information

human ... CHRM3(1131)

Gene Information

-

Gene Information

-

Gene Information

human ... ABCB1(5243), ADRA1A(148), ADRA2A(150), ADRA2C(152), CHRM1(1128), DRD2(1813), DRD3(1814), DRD4(1815), EBP(10682), HRH1(3269), HTR2A(3356), HTR2C(3358), HTR7(3363), KCNH1(3756), KCNH2(3757), PRNP(5621)
rat ... Adra1a(29412), Adra2a(25083), Chrm1(25229), Chrm2(81645), Drd1a(24316), Drd2(24318), Drd3(29238), Drd4(25432), Hrh1(24448), Htr1a(24473), Htr1b(25075), Htr2a(29595), Htr2c(25187), Oprs1(29336), Slc6a3(24898), Slc6a4(25553)

Application

p-Fluorohexahydro-sila-difenidol hydrochloride (pFHHSid) has been used:
  • as the M3/muscarinic acetylcholine receptor antagonist to study its involvement in carbachol induced Egr-1 biosynthesis using human neuroblastoma cells[1]
  • as M3 receptor antagonist to test its involvement on N,N-diethyl-m-toluamide (DEET)-induced angiogenesis in human umbilical venous endothelial cells (HUVEC)[2]
  • in a study to examine the role of aclidinium on human fibroblast to myofibroblast[3]

Biochem/physiol Actions

High affinity M3 muscarinic acetylcholine receptor antagonist.

Features and Benefits

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

Classe di stoccaggio

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

ppe

Eyeshields, Gloves, type N95 (US)


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S M Jankovic et al.
Methods and findings in experimental and clinical pharmacology, 26(2), 87-91 (2004-04-09)
The Fallopian tubes are sparsely innervated with cholinergic nerve fibers. Acetylcholine is released from these nerves and contracts the smooth muscles of the tubes. The aim of our study was to investigate the effect of acetylcholine on the isthmic segment
Dora E Benavides-Haro et al.
Naunyn-Schmiedeberg's archives of pharmacology, 368(4), 309-315 (2003-09-10)
The effect of the cholinomimetic agent, bethanechol on macroscopic membrane currents was studied in dispersed cat atrial myocytes, using the whole-cell patch-clamp technique. Bethanechol activated an inward rectifying potassium current similar to I(K(ACh)), and a delayed rectifying-like outward current, similar
Kunrong Cheng et al.
American journal of physiology. Gastrointestinal and liver physiology, 295(3), G591-G597 (2008-07-26)
Most colon cancers overexpress M3 muscarinic receptors (M3R), and post-M3R signaling stimulates human colon cancer cell proliferation. Acetylcholine (ACh), a muscarinic receptor ligand traditionally regarded as a neurotransmitter, may be produced by nonneuronal cells. We hypothesized that ACh release by
M T de la Vega et al.
Archives of medical research, 28(4), 493-497 (1997-01-01)
In this study, the authors set out to determine the presence of M3 muscarinic receptors in rat striatum by examining the binding of [3H]N-methylscopolamine ([3H]NMS) to striatal membranes and its displacement by antagonists with different affinity for M1 and M3
Javier Milara et al.
Thorax, 67(3), 229-237 (2011-10-01)
Fibroblast to myofibroblast transition is believed to contribute to airway remodelling in lung diseases such as asthma and chronic obstructive pulmonary disease. This study examines the role of aclidinium, a new long-acting muscarinic antagonist, on human fibroblast to myofibroblast transition.

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