PD 128042

Modify Date: 2024-01-03 08:20:14

PD 128042 Structure
PD 128042 structure
Common Name PD 128042
CAS Number 114289-47-3 Molecular Weight 393.56000
Density 1.002g/cm3 Boiling Point 504.7ºC at 760mmHg
Molecular Formula C23H39NO4 Melting Point N/A
MSDS Chinese USA Flash Point 259ºC

 Use of PD 128042


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].

 Names

Name 2,2-dimethyl-N-(2,4,6-trimethoxyphenyl)dodecanamide
Synonym More Synonyms

 PD 128042 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
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

 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%

 Articles25

More 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...

 Synonyms

CI 976
2,2-Dimethyl-N-(2,4,6-trimethoxyphenyl)dodecanamide
C23H39NO4
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