Granotapide | JTT 130 | CAS#916683-32-4 | hypolipidemic agent

MedKoo Cat#: 596309 | Name: Granotapide

Description:

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

Granotapide, also known as JTT 130, is a hypolipidemic agent that inhibits microsomal triglyceride transfer protein.

Chemical Structure

Granotapide

CAS#916683-32-4

Theoretical Analysis

MedKoo Cat#: 596309

Name: Granotapide

CAS#: 916683-32-4

Chemical Formula: C39H37F3N2O8

Exact Mass: 718.2502

Molecular Weight: 718.72

Elemental Analysis: C, 65.17; H, 5.19; F, 7.93; N, 3.90; O, 17.81

Price and Availability

This product is currently not in stock but may be available through custom synthesis. To ensure cost efficiency, the minimum order quantity is 1 gram. The estimated lead time is 2 to 4 months, with pricing dependent on the complexity of the synthesis (typically high for intricate chemistries). Quotes for quantities below 1 gram will not be provided. To request a quote, please click the button below. Note: If this product becomes available in stock in the future, pricing will be listed accordingly.

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Related CAS #

No Data

Synonym

JTT 130; JTT-130; JTT130; Granotapide;

IUPAC/Chemical Name

diethyl 2-(acetoxy(3-(dimethylcarbamoyl)-4-(4'-(trifluoromethyl)-[1,1'-biphenyl]-2-carboxamido)phenyl)methyl)-2-phenylmalonate

InChi Key

SHEMFPSQQCVFBI-UHFFFAOYSA-N

InChi Code

InChI=1S/C39H37F3N2O8/c1-6-50-36(48)38(37(49)51-7-2,27-13-9-8-10-14-27)33(52-24(3)45)26-19-22-32(31(23-26)35(47)44(4)5)43-34(46)30-16-12-11-15-29(30)25-17-20-28(21-18-25)39(40,41)42/h8-23,33H,6-7H2,1-5H3,(H,43,46)

SMILES Code

O=C(OCC)C(C1=CC=CC=C1)(C(C2=CC=C(NC(C3=CC=CC=C3C4=CC=C(C(F)(F)F)C=C4)=O)C(C(N(C)C)=O)=C2)OC(C)=O)C(OCC)=O

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

>2 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

2934.99.9001

More Info

Instruction

View handling instruction

Preparing Stock Solutions

The following data is based on the product molecular weight 718.72 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

1: Mera Y, Kawai T, Ogawa N, Odani N, Sasase T, Miyajima K, Ohta T, Kakutani M. JTT-130, a novel intestine-specific inhibitor of microsomal triglyceride transfer protein, ameliorates lipid metabolism and attenuates atherosclerosis in hyperlipidemic animal models. J Pharmacol Sci. 2015 Nov;129(3):169-76. doi: 10.1016/j.jphs.2015.10.004. Epub 2015 Oct 20. PubMed PMID: 26598005. 2: Sakata S, Katsumi S, Mera Y, Kuroki Y, Nashida R, Kakutani M, Ohta T. Mechanism of action of hypoglycemic effects of an intestine-specific inhibitor of microsomal triglyceride transfer protein (MTP) in obese rats. J Pharmacol Sci. 2015 Jan;127(1):103-8. doi: 10.1016/j.jphs.2014.11.004. Epub 2014 Nov 22. PubMed PMID: 25704025. 3: Mera Y, Hata T, Ishii Y, Tomimoto D, Kawai T, Ohta T, Kakutani M. JTT-130, a novel intestine-specific inhibitor of microsomal triglyceride transfer protein, reduces food preference for fat. J Diabetes Res. 2014;2014:583752. doi: 10.1155/2014/583752. Epub 2014 May 15. PubMed PMID: 24959597; PubMed Central PMCID: PMC4052484. 4: Sakata S, Ito M, Mera Y, Sasase T, Yamamoto H, Kakutani M, Ohta T. JTT-130, a novel intestine-specific inhibitor of microsomal triglyceride transfer protein, improves hyperglycemia and dyslipidemia independent of suppression of food intake in diabetic rats. J Diabetes Res. 2014;2014:803832. doi: 10.1155/2014/803832. Epub 2014 May 7. PubMed PMID: 24895641; PubMed Central PMCID: PMC4033514. 5: Sakata S, Mera Y, Kuroki Y, Nashida R, Kakutani M, Ohta T. Combination therapy of an intestine-specific inhibitor of microsomal triglyceride transfer protein and peroxisome proliferator-activated receptor γ agonist in diabetic rat. J Diabetes Res. 2014;2014:890639. doi: 10.1155/2014/890639. Epub 2014 Mar 17. PubMed PMID: 24772450; PubMed Central PMCID: PMC3977080. 6: Kostapanos MS, Rizos EC, Papanas N, Maltezos E, Elisaf MS. Mitochondrial triglyceride transfer protein inhibition: new achievements in the treatment of dyslipidemias. Curr Pharm Des. 2013;19(17):3150-60. Review. PubMed PMID: 23317403. 7: Ryder T, Walker GS, Goosen TC, Ruggeri RB, Conn EL, Rocke BN, Lapham K, Steppan CM, Hepworth D, Kalgutkar AS. Insights into the novel hydrolytic mechanism of a diethyl 2-phenyl-2-(2-arylacetoxy)methyl malonate ester-based microsomal triglyceride transfer protein (MTP) inhibitor. Chem Res Toxicol. 2012 Oct 15;25(10):2138-52. doi: 10.1021/tx300243v. Epub 2012 Sep 27. PubMed PMID: 22989032. 8: Hata T, Mera Y, Kawai T, Ishii Y, Kuroki Y, Kakimoto K, Ohta T, Kakutani M. JTT-130, a novel intestine-specific inhibitor of microsomal triglyceride transfer protein, ameliorates impaired glucose and lipid metabolism in Zucker diabetic fatty rats. Diabetes Obes Metab. 2011 Jul;13(7):629-38. doi: 10.1111/j.1463-1326.2011.01387.x. PubMed PMID: 21362121. 9: Hata T, Mera Y, Tadaki H, Kuroki Y, Kawai T, Ohta T, Kakutani M. JTT-130, a novel intestine-specific inhibitor of microsomal triglyceride transfer protein, suppresses high fat diet-induced obesity and glucose intolerance in Sprague-Dawley rats. Diabetes Obes Metab. 2011 May;13(5):446-54. doi: 10.1111/j.1463-1326.2011.01368.x. Epub 2011 Jan 21. PubMed PMID: 21255216. 10: Hata T, Mera Y, Ishii Y, Tadaki H, Tomimoto D, Kuroki Y, Kawai T, Ohta T, Kakutani M. JTT-130, a novel intestine-specific inhibitor of microsomal triglyceride transfer protein, suppresses food intake and gastric emptying with the elevation of plasma peptide YY and glucagon-like peptide-1 in a dietary fat-dependent manner. J Pharmacol Exp Ther. 2011 Mar;336(3):850-6. doi: 10.1124/jpet.110.176560. Epub 2010 Dec 7. Erratum in: J Pharmacol Exp Ther. 2011 Mar;336(3):321-2. PubMed PMID: 21139060. 11: Mera Y, Odani N, Kawai T, Hata T, Suzuki M, Hagiwara A, Katsushima T, Kakutani M. Pharmacological characterization of diethyl-2-({3-dimethylcarbamoyl-4-[(4'-trifluoromethylbiphenyl-2-carbonyl)amino]p henyl}acetyloxymethyl)-2-phenylmalonate (JTT-130), an intestine-specific inhibitor of microsomal triglyceride transfer protein. J Pharmacol Exp Ther. 2011 Feb;336(2):321-7. doi: 10.1124/jpet.110.173807. Epub 2010 Oct 25. PubMed PMID: 20974698. 12: Burnett JR. Drug evaluation: The MTP inhibitor JTT-130 as a potential treatment for hyperlipidemia. IDrugs. 2006 Jul;9(7):495-9. PubMed PMID: 16821163. 13: Aggarwal D, West KL, Zern TL, Shrestha S, Vergara-Jimenez M, Fernandez ML. JTT-130, a microsomal triglyceride transfer protein (MTP) inhibitor lowers plasma triglycerides and LDL cholesterol concentrations without increasing hepatic triglycerides in guinea pigs. BMC Cardiovasc Disord. 2005 Sep 27;5:30. PubMed PMID: 16188040; PubMed Central PMCID: PMC1262701.