Telotristat (Synonyms: LP-778902)

Name: Telotristat
Brand: MedChemExpress
SKU: HY-13055B
Rating: 4.5 (1 reviews)

Cat. No.: HY-13055B Purity: 99.76%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

Telotristat (LP-778902) is a potent tryptophan hydroxylase inhibitor with an in vivo IC₅₀ of 0.028 μM.

For research use only. We do not sell to patients.

Telotristat Chemical Structure

CAS No. : 1033805-28-5

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10 mM * 1 mL in DMSO ready for reconstitution	USD 102	In-stock	Estimated Time of Arrival: December 31
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10 mM * 1 mL in DMSO	USD 102	In-stock	Estimated Time of Arrival: December 31
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5 mg	USD 85	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 125	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 260	In-stock	Estimated Time of Arrival: December 31
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100 mg	USD 680	In-stock	Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

Other Forms of Telotristat:

Telotristat etiprate In-stock
Telotristat ethyl In-stock

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Description

Telotristat (LP-778902) is a potent tryptophan hydroxylase inhibitor with an in vivo IC₅₀ 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].

MedChemExpress (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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

Molecular Weight

546.93

Formula

C₂₅H₂₂ClF₃N₆O₃

CAS No.

1033805-28-5

Appearance

Solid

Color

White to light yellow

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvent & Solubility

In Vitro:

DMSO : 33.33 mg/mL (60.94 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
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

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (4.57 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (4.57 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (4.57 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.76%

Select Batch:

Data Sheet (273 KB) SDS (0 KB)

COA (248 KB) HNMR (302 KB) LCMS (266 KB)

Handling Instructions (2659 KB)

References

[1]. Lapuerta P, et al. Telotristat etiprate, a novel inhibitor of serotonin synthesis for the treatment of carcinoid syndrome. Clin. Invest. (Lond.) (2015) 5(5), 447–456

[2]. US20080153852

Cell Assay ^[2]	BON CBA cells are grown in equal volume of DMEM and F12K with 5% bovine serum for 3-4 hours (20 K cell/well) and telotristat is added at a concentration range of 0.07 to 50 μM. The cells are incubated at 37°C overnight. 50 μM of the culture supernatant is then taken for 5HTP measurement. The supernatant is mixed with equal volume of 1M TCA, then filtered through glass fiber. The filtrate is loaded on reverse phase HPLC for 5HTP concentration measurement. The cell viability is measured by treating the remaining cells with Celltiter-Glo Luminescent Cell Viability Assay^[2]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[2]	Rats: 14-week-old male C57 albino mice are dosed once daily by oral gavage at 5-10 mL/kg for four consecutive days. Five hours after the last dose, the animals are quickly sacrificed. 5-HT is extracted from the blood or tissues and measured by HPLC. Blood samples are taken for exposure analysis^[2]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References	[1]. Lapuerta P, et al. Telotristat etiprate, a novel inhibitor of serotonin synthesis for the treatment of carcinoid syndrome. Clin. Invest. (Lond.) (2015) 5(5), 447–456 [2]. US20080153852

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	1.8284 mL	9.1419 mL	18.2839 mL	45.7097 mL
	5 mM	0.3657 mL	1.8284 mL	3.6568 mL	9.1419 mL
	10 mM	0.1828 mL	0.9142 mL	1.8284 mL	4.5710 mL
	15 mM	0.1219 mL	0.6095 mL	1.2189 mL	3.0473 mL
	20 mM	0.0914 mL	0.4571 mL	0.9142 mL	2.2855 mL
	25 mM	0.0731 mL	0.3657 mL	0.7314 mL	1.8284 mL
	30 mM	0.0609 mL	0.3047 mL	0.6095 mL	1.5237 mL
	40 mM	0.0457 mL	0.2285 mL	0.4571 mL	1.1427 mL
	50 mM	0.0366 mL	0.1828 mL	0.3657 mL	0.9142 mL
	60 mM	0.0305 mL	0.1524 mL	0.3047 mL	0.7618 mL

Telotristat Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Telotristat1033805-28-5LP-778902LP778902LP 778902Tryptophan HydroxylaseInhibitorinhibitorinhibit

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Telotristat (Synonyms: LP-778902)

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Other Forms of Telotristat:

Telotristat Related Antibodies

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Biological Activity

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Telotristat Related Antibodies

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Complete Stock Solution Preparation Table

Telotristat Related Classifications

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