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Merck

SML0539

T863

≥98% (HPLC), DGAT1 inhibitor, powder

Sinónimos:

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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Acerca de este artículo

Fórmula empírica (notación de Hill):
C22H26N4O3
Número CAS:
Peso molecular:
394.47
UNSPSC Code:
51111800
PubChem Substance ID:
NACRES:
NA.77
MDL number:
Assay:
≥98% (HPLC)
Form:
powder
Quality level:
Servicio técnico
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Nombre del producto

T863, ≥98% (HPLC)

Quality Level

assay

≥98% (HPLC)

form

powder

color

white to beige

solubility

DMSO: 15 mg/mL (clear solution)

storage temp.

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-

InChI key

FUIYMYNYUHVDPT-HDJSIYSDSA-N

Application

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 Actions

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.
T863 is an orally active, selective and potent DGAT1 inhibitor.


Clase de almacenamiento

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable



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Exogenous monounsaturated fatty acids promote a ferroptosis-resistant cell state
Magtanong L, et al.
Cell Chemical Biology, 26(3), 420-432 (2019)
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
DGAT1-dependent lipid droplet biogenesis protects mitochondrial function during starvation-induced autophagy
Nguyen TB, et al.
Developmental Cell, 42(1), 9-21 (2017)