M7065

Sigma-Aldrich

MK-912 hydrochloride hydrate

≥98% (HPLC)

Synonym(s):
L-657,743, (2S-trans)-1,3,4,5′,6,6′,7,12b-Octahydro-1′,3′-dimethyl-spiro[2H-benzofuro[2,3-a]quinolizine-2,4′(1’H)-pyrimidin]-2′(3’H)-one hydrochloride hydrate
Empirical Formula (Hill Notation):
C20H25N3O2 · xHCl · yH2O
Molecular Weight:
339.43 (anhydrous free base basis)
PubChem Substance ID:
NACRES:
NA.77
Pricing and availability is not currently available.

Quality Level

assay

≥98% (HPLC)

form

powder

color

white to beige

solubility

H2O: soluble 16 mg/mL

originator

Merck & Co., Inc., Kenilworth, NJ, U.S.

SMILES string

O.Cl.CN1CCC2(CCN3CCc4c(oc5ccccc45)C3C2)N(C)C1=O

InChI

1S/C20H25N3O2.ClH.H2O/c1-21-11-8-20(22(2)19(21)24)9-12-23-10-7-15-14-5-3-4-6-17(14)25-18(15)16(23)13-20;;/h3-6,16H,7-13H2,1-2H3;1H;1H2

InChI key

WVVGVFGUHPXSJZ-UHFFFAOYSA-N

Gene Information

human ... ADRB2(154)

Packaging

5, 25 mg in glass bottle

Biochem/physiol Actions

Selective α2-adrenoceptor antagonist

Features and Benefits

This compound was developed by Merck & Co., Inc., Kenilworth, NJ, U.S.. To browse the list of other pharma-developed compounds and Approved Drugs/Drug Candidates, click here.
This compound is featured on the α2-Adrenoceptors page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.
This compound is also offered as part of Sigma′s Library of Pharmacologically Active Compounds (LOPAC®1280), a biologically annotated collection of high-quality, ready-to-screen compounds. Click here to learn more.

Other Notes

Material is hygroscopic.

Legal Information

LOPAC is a registered trademark of Sigma-Aldrich Co. LLC

Personal Protective Equipment

dust mask type N95 (US),Eyeshields,Gloves

RIDADR

NONH for all modes of transport

WGK Germany

3

Certificate of Analysis
Certificate of Origin
K Krajnak et al.
Journal of applied physiology (Bethesda, Md. : 1985), 100(4), 1230-1237 (2005-12-13)
The vascular symptoms of hand-arm vibration syndrome, including cold-induced vasospasm, are in part mediated by increased sensitivity of cutaneous arteries to sympathetic stimulation. The goal of the present study was to use a rat tail model to analyze the effects...
alpha 2A-adrenoceptors, not I1-imidazoline receptors, mediate the hypotensive effects of rilmenidine and moxonidine in conscious mice. In vivo and in vitro studies.
Q M Zhu et al.
Annals of the New York Academy of Sciences, 881, 287-289 (1999-07-23)
D D Schwartz et al.
Journal of veterinary pharmacology and therapeutics, 21(2), 107-111 (1998-05-23)
alpha 2-Adrenergic receptor agonists are widely used in veterinary medicine as sedative/hypnotic agents. Four pharmacological subtypes of the alpha 2-adrenergic receptor (A, B, C and D) have been identified based primarily on differences in affinity for several drugs. The purpose...
J R Jasper et al.
Biochemical pharmacology, 55(7), 1035-1043 (1998-05-30)
Alpha-2 adrenergic receptors (alpha2 AR) mediate incorporation of guanosine 5'-O-(gamma-thio)triphosphate ([35S]GTPgammaS) into isolated membranes via receptor-catalyzed exchange of [35S]GTPgammaS for GDP. In the current study, we used [35S]GTPgammaS incorporation to characterize the intrinsic activity and potency of agonists and antagonists...
Kazunori Kawamura et al.
ACS chemical neuroscience, 1(7), 520-528 (2010-07-21)
To evaluate in vivo brain penetration of α(2C)-adrenoceptor (α(2C)-AR) antagonists as a therapeutic agent, we synthesized two new (11)C-labeled selective α(2C)-AR antagonists 4-(6,7-dimethoxy-1,2,3,4-tetrahydroisoquinolin-2-yl)methyl-2-aryl-7-methoxybenzofuran ([(11)C]MBF) and acridin-9-yl-[4-(4-methylpiperazin-1-yl)phenyl]amine ([(11)C]JP-1302) as α(2C)-AR-selective positron emission tomography (PET) probes. The radiochemical yield, specific activity, and...
Articles

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