NTE-122
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MedKoo CAT#: 563381

CAS#: 166967-84-6

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

Chemical Structure

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NTE-122
CAS# 166967-84-6
Product data Instruction

Theoretical Analysis

MedKoo Cat#: 563381
Name: NTE-122
CAS#: 166967-84-6
Chemical Formula: C38H58N6O2
Exact Mass: 630.46
Molecular Weight: 630.922
Elemental Analysis: C, 72.34; H, 9.27; N, 13.32; O, 5.07

Price and Availability

Size Price Availability Quantity
5mg USD 340 2 Weeks
10mg USD 560 2 Weeks
25mg USD 1015 2 Weeks
50mg USD 1665 2 Weeks
100mg USD 2665 2 Weeks
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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.

Recalculate based on batch purity %
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: 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.
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.

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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.