NTE-122 | CAS#166967-84-6 | ACAT inhibitor

MedKoo Cat#: 563381 | Name: NTE-122

Description:

WARNING: This product is for research use only, not for human or veterinary use.

NTE-122 is a potent, selective and competitive inhibitor of Acyl-CoA:cholesterol acyltransferase (ACAT).

Chemical Structure

NTE-122

CAS#166967-84-6

Theoretical Analysis

MedKoo Cat#: 563381

Name: NTE-122

CAS#: 166967-84-6

Chemical Formula: C38H58N6O2

Exact Mass: 630.4621

Molecular Weight: 630.92

Elemental Analysis: C, 72.34; H, 9.27; N, 13.32; O, 5.07

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Synonym

NTE-122; NTE 122; NTE122;

IUPAC/Chemical Name

trans-1,4-Bis[[1-cyclohexyl-3-(4-dimethylamino phenyl)ureido]methyl]cyclohexane

InChi Key

SIHFCVXQGXGQQO-WXUXXXNLSA-N

InChi Code

InChI=1S/C38H58N6O2/c1-41(2)33-23-19-31(20-24-33)39-37(45)43(35-11-7-5-8-12-35)27-29-15-17-30(18-16-29)28-44(36-13-9-6-10-14-36)38(46)40-32-21-25-34(26-22-32)42(3)4/h19-26,29-30,35-36H,5-18,27-28H2,1-4H3,(H,39,45)(H,40,46)/t29-,30-

SMILES Code

O=C(NC1=CC=C(N(C)C)C=C1)N(C[C@H]2CC[C@H](CN(C3CCCCC3)C(NC4=CC=C(N(C)C)C=C4)=O)CC2)C5CCCCC5

Appearance

Solid powder

Purity

>98% (or refer to the Certificate of Analysis)

Shipping Condition

Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition

Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility

Soluble in DMSO

Shelf Life

>3 years if stored properly

Drug Formulation

This drug may be formulated in DMSO

Stock Solution Storage

0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code

2934.99.03.00

More Info

Product Data

Product Data

Instruction

View handling instruction

Biological target:

NTE-122 is a potent, selective and competitive inhibitor of Acyl-CoA:cholesterol acyltransferase (ACAT).

In vitro activity:

NTE-122 markably inhibited [3H]oleate incorporation into cholesteryl esters in HepG2 cells incubated with 5 microg/ml 25-hydroxycholesterol as a stimulus for ACAT (IC50=6.0 nM). NTE-122 pronouncedly inhibited the secretion of radiolabeled cholesteryl esters in proportion to the inhibition of cellular cholesterol esterification, and it significantly reduced the secretion of radiolabeled triglycerides and apoB mass in HepG2 cells incubated with 25-hydroxycholesterol. Reference: Jpn J Pharmacol. 1999 Feb;79(2):159-67. https://pubmed.ncbi.nlm.nih.gov/10202850/

In vivo activity:

NTE-122 (1, 3 and 10 mg/kg per day) lowered the total cholesterol levels in both plasma and liver dose-dependently (by 99% and 94% at 10 mg/kg per day, respectively). In the aortic wall of the rabbits given NTE-122, the atherosclerotic lesion area in both aortic arch and thoracic aorta were dose-dependently reduced (by 100% at 10 mg/kg per day), and the total cholesterol content in aortic arch was also lowered significantly at more than 3 mg/kg per day. These results suggest that NTE-122 is capable of exhibiting anti-atherosclerotic effects. Reference: Jpn J Pharmacol. 2001 May;86(1):120-3. https://pubmed.ncbi.nlm.nih.gov/11430463/

Preparing Stock Solutions

The following data is based on the product molecular weight 630.92 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

Formulation protocol:

1, Azuma Y, Kawasaki T, Ikemoto K, Ohno K, Yamada T, Yamasaki M, Nobuhara Y. Effects of NTE-122, a novel acyl-CoA:cholesterol acyltransferase inhibitor, on cholesterol esterification and high-density lipoprotein-induced cholesterol efflux in macrophages. Jpn J Pharmacol. 1999 Feb;79(2):159-67. doi: 10.1254/jjp.79.159. PMID: 10202851. 2, Azuma Y, Kawasaki T, Ohno K, Seto J, Yamada T, Yamasaki M, Nobuhara Y. Effects of NTE-122, a novel acyl-CoA:cholesterol acyltransferase inhibitor, on cholesterol esterification and secretions of apolipoprotein B-containing lipoprotein and bile acids in HepG2. Jpn J Pharmacol. 1999 Feb;79(2):151-8. doi: 10.1254/jjp.79.151. PMID: 10202850. 3. Azuma Y, Date K, Ohno K, Matsushiro S, Nobuhara Y, Yamada T. NTE-122, an acyl-coa:cholesterol acyltransferase inhibitor, prevents the progression of atherogenesis in cholesterol-fed rabbits. Jpn J Pharmacol. 2001 May;86(1):120-3. doi: 10.1254/jjp.86.120. PMID: 11430463. 4. Azuma Y, Seto J, Ohno K, Mikami H, Yamada T, Yamasaki M, Chiba M, Nobuhara Y. Effects of NTE-122, an acyl-CoA:cholesterol acyltransferase inhibitor, on cholesterol esterification and lipid secretion from CaCo-2 cells, and cholesterol absorption in rats. Jpn J Pharmacol. 1999 May;80(1):81-4. doi: 10.1254/jjp.80.81. PMID: 10446760.

In vitro protocol:

In vivo protocol:

1. Azuma Y, Date K, Ohno K, Matsushiro S, Nobuhara Y, Yamada T. NTE-122, an acyl-coa:cholesterol acyltransferase inhibitor, prevents the progression of atherogenesis in cholesterol-fed rabbits. Jpn J Pharmacol. 2001 May;86(1):120-3. doi: 10.1254/jjp.86.120. PMID: 11430463. 2. Azuma Y, Seto J, Ohno K, Mikami H, Yamada T, Yamasaki M, Chiba M, Nobuhara Y. Effects of NTE-122, an acyl-CoA:cholesterol acyltransferase inhibitor, on cholesterol esterification and lipid secretion from CaCo-2 cells, and cholesterol absorption in rats. Jpn J Pharmacol. 1999 May;80(1):81-4. doi: 10.1254/jjp.80.81. PMID: 10446760.

1: Azuma Y, Date K, Ohno K, Matsushiro S, Nobuhara Y, Yamada T. NTE-122, an acyl-coa:cholesterol acyltransferase inhibitor, prevents the progression of atherogenesis in cholesterol-fed rabbits. Jpn J Pharmacol. 2001 May;86(1):120-3. PubMed PMID: 11430463. 2: Ohgami N, Kuniyasu A, Furukawa K, Miyazaki A, Hakamata H, Horiuchi S, Nakayama H. Glibenclamide acts as an inhibitor of acyl-CoA:cholesterol acyltransferase enzyme. Biochem Biophys Res Commun. 2000 Oct 22;277(2):417-22. PubMed PMID: 11032738. 3: Nakayama H, Ohgami N, Kuniyasu A, Miyazaki A, Hakamata H, Horiuchi S. [Glibenclamide inhibits cholesterol metabolism in macrophage]. Nihon Yakurigaku Zasshi. 1999 Oct;114 Suppl 1:150P-153P. Japanese. PubMed PMID: 10629872. 4: Azuma Y, Seto J, Ohno K, Mikami H, Yamada T, Yamasaki M, Chiba M, Nobuhara Y. Effects of NTE-122, an acyl-CoA:cholesterol acyltransferase inhibitor, on cholesterol esterification and lipid secretion from CaCo-2 cells, and cholesterol absorption in rats. Jpn J Pharmacol. 1999 May;80(1):81-4. PubMed PMID: 10446760. 5: Azuma Y, Kawasaki T, Ikemoto K, Ohno K, Yamada T, Yamasaki M, Nobuhara Y. Effects of NTE-122, a novel acyl-CoA:cholesterol acyltransferase inhibitor, on cholesterol esterification and high-density lipoprotein-induced cholesterol efflux in macrophages. Jpn J Pharmacol. 1999 Feb;79(2):159-67. PubMed PMID: 10202851. 6: Azuma Y, Kawasaki T, Ohno K, Seto J, Yamada T, Yamasaki M, Nobuhara Y. Effects of NTE-122, a novel acyl-CoA:cholesterol acyltransferase inhibitor, on cholesterol esterification and secretions of apolipoprotein B-containing lipoprotein and bile acids in HepG2. Jpn J Pharmacol. 1999 Feb;79(2):151-8. PubMed PMID: 10202850. 7: Azuma Y, Kawasaki T, Ikemoto K, Obata K, Ohno K, Sajiki N, Yamada T, Yamasaki M, Nobuhara Y. Cholesterol-lowering effects of NTE-122, a novel acyl-CoA:cholesterol acyltransferase (ACAT) inhibitor, on cholesterol diet-fed rats and rabbits. Jpn J Pharmacol. 1998 Nov;78(3):355-64. PubMed PMID: 9869270. 8: Kawasaki T, Miyazaki A, Hakamata H, Matsuda H, Horiuchi S. Biochemical evidence for oligomerization of rat adrenal acyl-coenzyme A:cholesterol acyltransferase. Biochem Biophys Res Commun. 1998 Mar 17;244(2):347-52. PubMed PMID: 9514926.