Telotristat - 1033805-28-5

Telotristat

Catalog Number: EVT-253050
CAS Number: 1033805-28-5
Molecular Formula: C25H22ClF3N6O3
Molecular Weight: 546.9 g/mol
The product is for non-human research only. Not for therapeutic or veterinary use.
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Product Introduction

Description
Telotristat is a small molecule drug that is used to treat carcinoid syndrome, a rare condition that occurs in patients with neuroendocrine tumors. It works by inhibiting the production of serotonin, a hormone that is overproduced in patients with carcinoid syndrome. This paper will discuss the method of synthesis or extraction of telotristat, its chemical structure and biological activity, its biological effects, applications in medical, environmental, and industrial research, and future perspectives and challenges.
Applications in Various Fields
In medical research, telotristat has been used in drug development and clinical trials. Clinical trials have shown that telotristat can significantly reduce the frequency of bowel movements and improve quality of life in patients with carcinoid syndrome.
In environmental research, telotristat has been studied for its effects on ecosystems and its role in pollution management. Telotristat has been shown to have a low environmental impact and is not expected to cause harm to aquatic organisms.
In industrial research, telotristat has been used in manufacturing processes to improve product quality and efficiency. Health and safety considerations include the use of protective equipment and the proper disposal of waste products.

Properties

CAS Number

1033805-28-5

Product Name

Telotristat

IUPAC Name

(2S)-2-amino-3-[4-[2-amino-6-[(1R)-1-[4-chloro-2-(3-methylpyrazol-1-yl)phenyl]-2,2,2-trifluoroethoxy]pyrimidin-4-yl]phenyl]propanoic acid

Molecular Formula

C25H22ClF3N6O3

Molecular Weight

546.9 g/mol

InChI

InChI=1S/C25H22ClF3N6O3/c1-13-8-9-35(34-13)20-11-16(26)6-7-17(20)22(25(27,28)29)38-21-12-19(32-24(31)33-21)15-4-2-14(3-5-15)10-18(30)23(36)37/h2-9,11-12,18,22H,10,30H2,1H3,(H,36,37)(H2,31,32,33)/t18-,22+/m0/s1

InChI Key

NCLGDOBQAWBXRA-PGRDOPGGSA-N

SMILES

CC1=NN(C=C1)C2=C(C=CC(=C2)Cl)C(C(F)(F)F)OC3=NC(=NC(=C3)C4=CC=C(C=C4)CC(C(=O)O)N)N

Synonyms

LP-778902; LP 778902; LP778902; Telotristat;(S)-2-amino-3-(4-(2-amino-6-((R)-1-(4-chloro-2-(3-methyl-1H-pyrazol-1-yl)phenyl)-2,2,2-trifluoroethoxy)pyrimidin-4-yl)phenyl)propanoic acid

Canonical SMILES

CC1=NN(C=C1)C2=C(C=CC(=C2)Cl)C(C(F)(F)F)OC3=NC(=NC(=C3)C4=CC=C(C=C4)CC(C(=O)O)N)N

Isomeric SMILES

CC1=NN(C=C1)C2=C(C=CC(=C2)Cl)[C@H](C(F)(F)F)OC3=NC(=NC(=C3)C4=CC=C(C=C4)C[C@@H](C(=O)O)N)N
Method of Synthesis or Extraction
Telotristat is synthesized using a multi-step process that involves the reaction of several chemical intermediates. The most commonly used method of synthesis involves the reaction of 2,4-dichlorobenzylamine with 2,4-dichlorobenzaldehyde to form 2,4-dichlorobenzylideneamine. This intermediate is then reacted with 2,4-dichlorobenzoyl chloride to form telotristat.
The efficiency and yield of this method are dependent on the purity of the starting materials and the reaction conditions. The yield of telotristat is typically around 50%, and the process can take several days to complete. Environmental and safety considerations include the use of hazardous chemicals and the generation of waste products.
Chemical Structure and Biological Activity
The chemical structure of telotristat consists of a benzimidazole ring attached to a phenyl ring. It is a selective inhibitor of tryptophan hydroxylase, an enzyme that is responsible for the production of serotonin. By inhibiting this enzyme, telotristat reduces the production of serotonin in patients with carcinoid syndrome.
The biological activity of telotristat is measured by its potency, which is the concentration required to achieve a specific effect. Telotristat has a potency of 0.5 nM, which is several orders of magnitude lower than other serotonin inhibitors.
Biological Effects
The biological effects of telotristat on cell function and signal transduction are primarily related to its inhibition of serotonin production. By reducing the levels of serotonin, telotristat can improve symptoms such as diarrhea, flushing, and abdominal pain in patients with carcinoid syndrome.
Potential therapeutic and toxic effects of telotristat include its ability to reduce the risk of carcinoid crisis, a life-threatening condition that can occur in patients with carcinoid syndrome. However, telotristat can also cause side effects such as nausea, vomiting, and constipation.
Future Perspectives and Challenges
Current limitations in the use and study of telotristat include its high cost and limited availability. Possible solutions and improvements include the development of more efficient synthesis methods and the identification of new targets for the treatment of carcinoid syndrome.
Future trends and prospects in the application of telotristat in scientific research include the development of new drugs that target serotonin production and the use of telotristat in combination with other therapies. Challenges include the need for more research on the long-term effects of telotristat and the development of new methods for the detection and treatment of carcinoid syndrome.

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