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Merck

SML0539

Sigma-Aldrich

T863

≥98% (HPLC)

Synonym(e):

2-((1,4-trans)-4-(4-(4-Amino-7,7-dimethyl-7H-pyrimido[4,5-b][1,4]oxazin-6-yl)- phenyl)cyclohexyl)acetic acid, T-863, trans-4-[4-(4-Amino-7,7-dimethyl-7H-pyrimido[4,5-b][1,4]oxazin-6-yl)phenyl]-cyclohexaneacetic acid

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About This Item

Empirische Formel (Hill-System):
C22H26N4O3
CAS-Nummer:
Molekulargewicht:
394.47
MDL-Nummer:
UNSPSC-Code:
51111800
PubChem Substanz-ID:
NACRES:
NA.77

Qualitätsniveau

Assay

≥98% (HPLC)

Form

powder

Farbe

white to beige

Löslichkeit

DMSO: 15 mg/mL (clear solution)

Lagertemp.

2-8°C

SMILES String

CC1(C)Oc2ncnc(N)c2N=C1c3ccc(cc3)[C@@H]4CC[C@H](CC4)CC(O)=O

InChI

1S/C22H26N4O3/c1-22(2)19(26-18-20(23)24-12-25-21(18)29-22)16-9-7-15(8-10-16)14-5-3-13(4-6-14)11-17(27)28/h7-10,12-14H,3-6,11H2,1-2H3,(H,27,28)(H2,23,24,25)/t13-,14-

InChIKey

FUIYMYNYUHVDPT-HDJSIYSDSA-N

Anwendung

T863 has been used as a diglyceride acyltransferase (DGAT1) inhibitor:
  • to provide the opportunity to precisely control the DGAT inhibition
  • to treat mouse embryonic fibroblasts (MEFs) to analyse lipid droplet biogenesis
  • to specifically block neutral lipid synthesis and lipid droplet formation in HT-1080 cells
  • to block lipid droplet (LD) formation

Biochem./physiol. Wirkung

T863 is an orally active, selective and potent DGAT1 (Acyl-CoA:diacylglycerol acyltransferase 1) inhibitor that interacts with the acyl-CoA binding site of DGAT1, and inhibits triacylglycerol synthesis in cells. T863 causes weight loss, reduction in serum and liver triglycerides, and improved insulin sensitivity in obese mice.

Lagerklassenschlüssel

11 - Combustible Solids

WGK

WGK 3

Flammpunkt (°F)

Not applicable

Flammpunkt (°C)

Not applicable


Analysenzertifikate (COA)

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In der Dokumentenbibliothek finden Sie die Dokumentation zu den Produkten, die Sie kürzlich erworben haben.

Die Dokumentenbibliothek aufrufen

Angela Castoldi et al.
Nature communications, 11(1), 4107-4107 (2020-08-17)
Foamy macrophages, which have prominent lipid droplets (LDs), are found in a variety of disease states. Toll-like receptor agonists drive triacylglycerol (TG)-rich LD development in macrophages. Here we explore the basis and significance of this process. Our findings indicate that
Exogenous monounsaturated fatty acids promote a ferroptosis-resistant cell state
Magtanong L, et al.
Cell Chemical Biology, 26(3), 420-432 (2019)
Jesus A Silvas et al.
bioRxiv : the preprint server for biology (2020-08-04)
Therapeutics targeting replication of SARS coronavirus 2 (SARS-CoV-2) are urgently needed. Coronaviruses rely on host membranes for entry, establishment of replication centers and egress. Compounds targeting cellular membrane biology and lipid biosynthetic pathways have previously shown promise as antivirals and
DGAT1-dependent lipid droplet biogenesis protects mitochondrial function during starvation-induced autophagy
Nguyen TB, et al.
Developmental Cell, 42(1), 9-21 (2017)
Lipid droplet formation in Mycobacterium tuberculosis infected macrophages requires IFN gamma/HIF-1alpha signaling and supports host defense
Knight M, et al.
PLoS Pathogens, 14(1), e1006874-e1006874 (2018)

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