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PD 128042

Names

[ CAS No. ]:
114289-47-3

[ Name ]:
PD 128042

[Synonym ]:
CI 976
2,2-Dimethyl-N-(2,4,6-trimethoxyphenyl)dodecanamide
C23H39NO4

Biological Activity

[Description]:

PD 128042 (CI 976) is a potent, orally active, and selective inhibitor of ACAT (acyl coenzyme A:cholesterol acyltransferase) with an IC50s of 73 nM. PD 128042 is also a potent LPAT (lysophospholipid acyltransferase) inhibitor. PD 128042 inhibits Golgi-associated LPAT activity (IC50=15 μM). PD 128042 inhibits multiple membrane trafficking steps, including ones found in the endocytic and secretory pathway[1][2][3].

[Related Catalog]:

Research Areas >> Metabolic Disease

[In Vivo]

PD 128042 (CI 976) (10-30 mg/kg; gavage, in the chronic cholesterol-fed rat model) decreases non-high density lipoprotein (HDL)-cholesterol and increases HDL-cholesterol in rats with pre-established dyslipidemia[4].

[References]

[1]. Chambers K, et al. A unique lysophospholipid acyltransferase (LPAT) antagonist, CI-976, affects secretory and endocytic membrane trafficking pathways. J Cell Sci. 2005;118(Pt 14):3061-3071.

[2]. O'Brien PM, et al. Inhibitors of acyl-CoA:cholesterol O-acyl transferase (ACAT) as hypocholesterolemic agents. 8. Incorporation of amide or amine functionalities into a series of disubstituted ureas and carbamates. Effects on ACAT inhibition in vitro and efficacy in vivo. J Med Chem. 1994;37(12):1810-1822.

[3]. Drecktrah D, et al. Inhibition of a Golgi complex lysophospholipid acyltransferase induces membrane tubule formation and retrograde trafficking. Mol Biol Cell. 2003;14(8):3459-3469.

[4]. Krause BR, et al. In vivo evidence that the lipid-regulating activity of the ACAT inhibitor CI-976 in rats is due to inhibition of both intestinal and liver ACAT. J Lipid Res. 1993;34(2):279-294.

Chemical & Physical Properties

[ Density]:
1.002g/cm3

[ Boiling Point ]:
504.7ºC at 760mmHg

[ Molecular Formula ]:
C23H39NO4

[ Molecular Weight ]:
393.56000

[ Flash Point ]:
259ºC

[ Exact Mass ]:
393.28800

[ PSA ]:
56.79000

[ LogP ]:
6.28090

[ Vapour Pressure ]:
2.59E-10mmHg at 25°C

[ Index of Refraction ]:
1.503

MSDS

Click to get detail MSDS

Toxicological Information

CHEMICAL IDENTIFICATION

RTECS NUMBER :
JR2052000
CHEMICAL NAME :
Dodecanamide, 2,2-dimethyl-N-(2,4,6-trimethoxyphenyl)-
CAS REGISTRY NUMBER :
114289-47-3
LAST UPDATED :
199612
DATA ITEMS CITED :
1
MOLECULAR FORMULA :
C23-H39-N-O4

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
157 gm/kg/56W-C
TOXIC EFFECTS :
Nutritional and Gross Metabolic - weight loss or decreased weight gain
REFERENCE :
TOXID9 Toxicologist. (Soc. of Toxicology, Inc., 475 Wolf Ledge Parkway, Akron, OH 44311) V.1- 1981- Volume(issue)/page/year: 13,317,1993

Safety Information

[ Hazard Statements ]:
H413

[ Personal Protective Equipment ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

[ Hazard Codes ]:
Xi

[ RIDADR ]:
NONH for all modes of transport

[ HS Code ]:
2924299090

Customs

[ HS Code ]: 2924299090

[ Summary ]:
2924299090. other cyclic amides (including cyclic carbamates) and their derivatives; salts thereof. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:30.0%

Articles

cPLA2α and EHD1 interact and regulate the vesiculation of cholesterol-rich, GPI-anchored, protein-containing endosomes.

Mol. Biol. Cell 23(10) , 1874-88, (2012)

The lipid modifier phospholipase A2 catalyzes the hydrolysis of phospholipids to inverted-cone-shaped lysophospholipids that contribute to membrane curvature and/or tubulation. Conflicting findings ex...

Use of acyltransferase inhibitors to block vesicular traffic between the ER and Golgi complex.

Meth. Enzymol. 404 , 115-25, (2005)

This article describes the use of acyltransferase inhibitors as probes for studying the potential role of lysophospholipid acyltransferases (LPAT) in intracellular membrane trafficking in the secretor...

A unique lysophospholipid acyltransferase (LPAT) antagonist, CI-976, affects secretory and endocytic membrane trafficking pathways.

J. Cell Sci. 118(Pt 14) , 3061-71, (2005)

Previous studies have shown that inhibition of a Golgi-complex-associated lysophospholipid acyltransferase (LPAT) activity by the drug CI-976 stimulates Golgi tubule formation and subsequent redistrib...


More Articles

Related Compounds