| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| 25mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| 250mg |
|
||
| 500mg |
|
||
| Other Sizes |
|
Purity: ≥98%
Telotristat (formerly known as LP-778902; LP778902) is the active metabolite of LX1606 (LX-1606; Telotristat etiprate) which is an orally bioavailable and small-molecule inhibitor of tryptophan hydroxylase (TPH, IC50 = 0.028 μM) with potential antiserotonergic activity. Telotristat has activity in controlling diarrhea associated with carcinoid syndrome. Telotristat acts by inhibiting the enzyme tryptophan hydoxylase (TPH) and reduces serotonin production both inside and outside the GI tract without affecting brain serotonin levels. Blocking peripheral serotonin synthesis by telotristat reduces severity of both chemical- and infection-induced intestinal inflammation.
| Targets |
Tryptophan hydroxylase
|
||
|---|---|---|---|
| ln Vitro |
The active component of telotristat etiprate is telotristat. An ethyl ester prodrug called telotristat etiprate is degraded to produce telotristat. An oral serotonin synthesis inhibitor called telotristat etiprate is used to treat carcinoid syndrome[1].
|
||
| ln Vivo |
Following oral administration, very low levels of telotristat etiprate are found. The quick hydrolysis into the active moiety telotristat is the cause of these low levels. The half-life is between four and twelve hours. When multiple doses are administered over the course of two weeks, there is no accumulation of telotristat. Telotristat exposure is roughly dose proportional[1].
|
||
| Animal Protocol |
|
||
| Toxicity/Toxicokinetics |
Hepatotoxicity
In small clinical trials of telotristat in patients with neuroendocrine tumors and symptomatic diarrhea despite stable doses of somatostatin analogues, transient, asymptomatic and mild serum elevations of ALT occurred in 4% to 5% and of GGT in 6% to 9% of treated subjects. Apparent liver injury with jaundice was not observed in the several prelicensure clinical trials and has not been reported in the limited clinical experience with this agent since its approval. Likelihood score: E (unlikely cause of clinically apparent liver injury). |
||
| References | |||
| Additional Infomation |
Telotristat is a phenylalanine derivative.
A tryptophan hydroxylase inhibitor. [Telotristat ethyl] (brand name Xermelo) is a prodrug of telotristat. Telotristat is a Tryptophan Hydroxylase Inhibitor. The mechanism of action of telotristat is as a Tryptophan Hydroxylase Inhibitor. Telotristat is an oral, small molecule inhibitor of tryptophan hydroxylase that is used in the treatment of symptoms of carcinoid syndrome. Telotristat is associated with modest rate of minor serum enzyme elevations during therapy but has not been linked to cases of clinically apparent liver injury. Telotristat is a tryptophan hydroxylase (TPH) inhibitor, with potential anti-serotonergic activity. Upon administration, telotristat binds to and inhibits the activity of TPH. This may result in a reduction in peripheral serotonin (5-HT) production and improvement of serotonin-mediated gastrointestinal effects such as severe diarrhea. TPH, the rate-limiting enzyme in serotonin biosynthesis, is overexpressed in carcinoid tumor cells. See also: Telotristat Ethyl (active moiety of); Telotristat Etiprate (is active moiety of). |
| Molecular Formula |
C25H22CLF3N6O3
|
|
|---|---|---|
| Molecular Weight |
546.93
|
|
| Exact Mass |
546.139
|
|
| Elemental Analysis |
C, 54.90; H, 4.05; Cl, 6.48; F, 10.42; N, 15.37; O, 8.78
|
|
| CAS # |
1033805-28-5
|
|
| Related CAS # |
Telotristat etiprate;1137608-69-5;Telotristat ethyl;1033805-22-9; 1033805-28-5 (acid); 1374745-52-4 (besilate)
|
|
| PubChem CID |
25025298
|
|
| Appearance |
Typically exists as White to light yellow solids at room temperature
|
|
| Density |
1.50±0.1 g/cm3 (20 ºC 760 Torr), 计算值
|
|
| LogP |
5.791
|
|
| Hydrogen Bond Donor Count |
3
|
|
| Hydrogen Bond Acceptor Count |
11
|
|
| Rotatable Bond Count |
8
|
|
| Heavy Atom Count |
38
|
|
| Complexity |
790
|
|
| Defined Atom Stereocenter Count |
2
|
|
| SMILES |
ClC1C([H])=C([H])C(=C(C=1[H])N1C([H])=C([H])C(C([H])([H])[H])=N1)[C@]([H])(C(F)(F)F)OC1C([H])=C(C2C([H])=C([H])C(=C([H])C=2[H])C([H])([H])[C@@]([H])(C(=O)O[H])N([H])[H])N=C(N([H])[H])N=1
|
|
| InChi Key |
NCLGDOBQAWBXRA-PGRDOPGGSA-N
|
|
| InChi Code |
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
|
|
| Chemical 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
|
|
| Synonyms |
|
|
| HS Tariff Code |
2934.99.9001
|
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
|
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
|
|||
|---|---|---|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.57 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (4.57 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (4.57 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
COA