CAS 114289-47-3|PD 128042
| 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 | / |
| MSDS | ChineseUSA | Flash Point | 259ºC |
Names
| Name | 2,2-dimethyl-N-(2,4,6-trimethoxyphenyl)dodecanamide |
|---|---|
| Synonym | More Synonyms |
PD 128042 BiologicalActivity
| 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 |
| InChIKey | WAFNZAURAWBNDZ-UHFFFAOYSA-N |
| SMILES | CCCCCCCCCCC(C)(C)C(=O)Nc1c(OC)cc(OC)cc1OC |
Toxicological Information
CHEMICAL IDENTIFICATION |
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 |
