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Merck

SML1340

Sigma-Aldrich

ML193 trifluoroacetate

≥98% (HPLC)

Synonim(y):

AC1LOE9L, CID-1261822, CID1261822, N-{4-[(3,4-Dimethyl-1,2-oxazol-5-yl)sulfamoyl]phenyl}-6,8-dimethyl-2-(pyridin-2-yl)quinoline-4-carboxamide trifluoroacetate

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About This Item

Wzór empiryczny (zapis Hilla):
C28H25N5O4S · C2HF3O2
Numer CAS:
Masa cząsteczkowa:
641.62
Kod UNSPSC:
12352200
Identyfikator substancji w PubChem:
NACRES:
NA.77

Poziom jakości

Próba

≥98% (HPLC)

Postać

powder

kolor

white to beige

rozpuszczalność

DMSO: 25 mg/mL, clear

temp. przechowywania

2-8°C

ciąg SMILES

FC(F)(C(O)=O)F.CC1=C(ON=C1C)NS(C2=CC=C(NC(C3=CC(C4=CC=CC=N4)=NC5=C3C=C(C)C=C5C)=O)C=C2)(=O)=O

Działania biochem./fizjol.

ML193 is a potent and selective piperadinyloxadiazolone antagonist for G protein-coupled receptor (GPCR) GPR55, a receptor for L-α-lysophosphatidylinositol (LPI) which also binds synthetic cannabinoids, and signals through several endogenous pathways. GPR55 is highly abundant in the CNS as well as in intestine, bone marrow, spleen, platelets, immune and endothelial cells. Its role is not completely understood, but has been implicated in inflammatory pain, neuropathic pain, metabolic disorder, bone development, and cancer. Selective antagonists are needed to further elucidate the role of GPR55 in physiology and pathobiology. ML193 (CID1261822) has 221 nM potency for GPR55 and >145-fold, >27-fold and >145-fold antagonist selectivity against GPR35, cannabinoid receptors CB1 and CB2, respectively and >145-fold agonist selectivity against GPR35, CB1 and CB2. ML193 is inhibits the downstream responses of ERK phosphorylation with an IC50 of 65 nM and PKC βII translocation with an IC50 of 10 μM.
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Kod klasy składowania

11 - Combustible Solids

Klasa zagrożenia wodnego (WGK)

WGK 3

Temperatura zapłonu (°F)

Not applicable

Temperatura zapłonu (°C)

Not applicable


Certyfikaty analizy (CoA)

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Dokumenty związane z niedawno zakupionymi produktami zostały zamieszczone w Bibliotece dokumentów.

Odwiedź Bibliotekę dokumentów

Justine Yu et al.
The Journal of biological chemistry, 288(31), 22481-22492 (2013-07-03)
The L-α-lysophosphatidylinositol (LPI)-sensitive receptor GPR55 is coupled to Ca(2+) signaling. Low levels of GPR55 expression in the heart have been reported. Similar to other G protein-coupled receptors involved in cardiac function, GPR55 may be expressed both at the sarcolemma and
Evangelia Kotsikorou et al.
Biochemistry, 52(52), 9456-9469 (2013-11-28)
GPR55 is a class A G protein-coupled receptor (GPCR) that has been implicated in inflammatory pain, neuropathic pain, metabolic disorder, bone development, and cancer. Initially deorphanized as a cannabinoid receptor, GPR55 has been shown to be activated by non-cannabinoid ligands
Sandra Cecconi et al.
International journal of molecular sciences, 20(12) (2019-06-20)
Endocannabinoids are key-players of female fertility and potential biomarkers of reproductive dysfunctions. Here, we investigated localization and expression of cannabinoid receptor type-1 and -2 (CB1R and CB2R), G-protein coupled receptor 55 (GPR55), and transient receptor potential vanilloid type 1 channel

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