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[CAS NO. 1033805-28-5] Telotristat
| Ships within | Stock | Price | Qty | Total |
Please click "REQUEST A QUOTE" button if there is no stock, or you need other sizes or custom synthesis.
| Catalog: | HY-13055B |
| Brand: | MCE |
| CAS: | 1033805-28-5 |
Overview
| MDL | MFCD20528907 |
|---|---|
| Molecular Weight | 546.93 |
| Molecular Formula | C25H22ClF3N6O3 |
| SMILES | N[C@@H](CC1=CC=C(C2=NC(N)=NC(O[C@H](C3=CC=C(Cl)C=C3N4N=C(C)C=C4)C(F)(F)F)=C2)C=C1)C(O)=O |
Summary
Telotristat (LP-778902) is a potent tryptophan hydroxylase inhibitor with an in vivo IC 50 of 0.028 μM.
IC50 & Target
IC50: 0.028 μM (tryptophan hydroxylase) [1]
In Vitro
Telotristat is the active moiety of telotristat etiprate. Telotristat etiprate is an ethyl ester prodrug which is hydrolyzed to telotristat. Telotristat etiprate is orally available serotonin synthesis inhibitor for the treatment of carcinoid syndrome [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Telotristat etiprate is present in very low levels after oral administration. These low levels are due to rapid hydrolysis into the active moiety telotristat. The half-life ranges from approximately 4-12 h. There is no accumulation of telotristat with multiple dose administration over 2 weeks. Exposure to telotristat is approximately dose proportional [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date | Phase |
|---|---|---|---|---|
| NCT03453489 | Barbara Ann Karmanos Cancer Institute|National Cancer Institute (NCI) |
Carcinoid Syndrome|Metastatic Nonfunctional Well Differentiated Neuroendocrine Neoplasm
|
June 20, 2018 | Phase 2 |
| NCT02147808 | Lexicon Pharmaceuticals |
Drug Interactions
|
May 2014 | Phase 1 |
| NCT01104415 | Lexicon Pharmaceuticals |
Carcinoid Syndrome
|
June 15, 2010 | Phase 2 |
| NCT02155205 | Lexicon Pharmaceuticals |
QT Interval
|
May 2014 | Phase 1 |
| NCT02063659 | Lexicon Pharmaceuticals |
Carcinoid Syndrome
|
March 11, 2014 | Phase 3 |
| NCT04776876 | M.D. Anderson Cancer Center |
Advanced Neuroendocrine Neoplasm|Carcinoid Syndrome
|
March 1, 2021 | Phase 2 |
| NCT04034745 | Andrew Hendifar, MD|Lexicon Pharmaceuticals|Cedars-Sinai Medical Center |
Pancreatic Cancer|Neuroendocrine Tumors|Cachexia; Cancer
|
October 2020 | |
| NCT03302845 | Lexicon Pharmaceuticals |
Drug-drug Interaction
|
September 21, 2017 | Phase 1 |
| NCT04065165 | European Organisation for Research and Treatment of Cancer - EORTC|Ipsen |
Small Intestinal NET|Carcinoid Heart Disease
|
April 2020 | Phase 3 |
| NCT02157584 | Lexicon Pharmaceuticals |
Healthy
|
June 2014 | Phase 1 |
| NCT02683577 | Ipsen |
Hepatic Impairment
|
February 2016 | Phase 1 |
| NCT04672876 | University of Chicago |
Neuroendocrine Tumors
|
January 2022 | Phase 2 |
| NCT04810091 | M.D. Anderson Cancer Center|TerSera Therapeutics LLC |
Locally Advanced Neuroendocrine Neoplasm|Metastatic Neuroendocrine Neoplasm
|
May 18, 2021 | Phase 3 |
| NCT03910387 | Emory University|TerSera Therapeutics LLC |
Locally Advanced Unresectable Pancreatic Adenocarcinoma|Metastatic Pancreatic Adenocarcinoma|Recurrent Pancreatic Adenocarcinoma|Stage III Pancreatic Cancer AJCC v8|Stage IV Pancreatic Cancer AJCC v8
|
April 17, 2019 | Phase 2 |
| NCT02195635 | Lexicon Pharmaceuticals |
Drug Interactions
|
July 2014 | Phase 1 |
| NCT03442725 | Ipsen |
Renal Impairment
|
February 9, 2018 | Phase 1 |
| NCT02026063 | Lexicon Pharmaceuticals |
Carcinoid Syndrome
|
January 14, 2014 | Phase 3 |
| NCT03423446 | Lexicon Pharmaceuticals |
Hepatic Impairment
|
November 28, 2017 | Phase 1 |
| NCT02157558 | Lexicon Pharmaceuticals |
Drug Interactions
|
July 2014 | Phase 1 |
| NCT04713202 | Chandrikha Chandrasekhara|TerSera Therapeutics LLC|Big Ten Cancer Research Consortium |
Neuroendocrine Tumors|Carcinoid Syndrome|Diarrhea
|
March 3, 2021 | Phase 2 |
| NCT03790111 | TerSera Therapeutics LLC |
Biliary Tract Cancer
|
March 13, 2019 | Phase 2 |
| NCT04543955 | Aman Chauhan|TerSera Therapeutics LLC|University of Kentucky |
Neuroendocrine Tumors
|
July 19, 2021 | Phase 2 |
| NCT01677910 | Lexicon Pharmaceuticals |
Carcinoid Syndrome
|
January 8, 2013 | Phase 3 |
| NCT01456052 | Lexicon Pharmaceuticals |
Ulcerative Colitis
|
January 30, 2012 | Phase 2 |
| NCT00853047 | Lexicon Pharmaceuticals |
Carcinoid Syndrome
|
March 2009 | Phase 2 |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 33.33 mg/mL ( 60.94 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 1.8284 mL | 9.1419 mL | 18.2839 mL |
| 5 mM | 0.3657 mL | 1.8284 mL | 3.6568 mL |
| 10 mM | 0.1828 mL | 0.9142 mL | 1.8284 mL |
References
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