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Telotristat Etiprate (LX 1606 Hippurate) Hydroxylase inhibitor

Name: Telotristat Etiprate (LX 1606 Hippurate)
Brand: Selleck Chemicals
SKU: S2173
Availability: InStock
Rating: 5 (1 reviews)

Cat.No.S2173

Telotristat Etiprate (LX 1606 Hippurate) is an orally bioavailable, tryptophan hydroxylase (TPH) inhibitor with potential antiserotonergic activity, currently in Phase 3.

Chemical Structure

Molecular Weight: 754.15

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: Purity: 99.98%

99.98

Related Targets	P450 (e.g. CYP17) Dehydrogenase PDE phosphatase PPAR HSP (HSP90) Vitamin Transferase Carbohydrate Metabolism Mitochondrial Metabolism Casein Kinase Serine/threonin kinase Lipoxygenase Phospholipase (e.g. PLA) Retinoid Receptor DPP ACE Peroxidases Amino Acids and Derivatives Fatty Acid Synthase FXR HMG-CoA Reductase Carbonic Anhydrase Lipase Decarboxylase DHFR IDO/TDO PCSK9 OXPHOS ROR
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Chemical Information, Storage & Stability

Molecular Weight	754.15	Formula	C₂₇H₂₆ClF₃N₆O₃.C₉H₉NO₃	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	1137608-69-5	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	CCOC(=O)C(CC1=CC=C(C=C1)C2=CC(=NC(=N2)N)OC(C3=C(C=C(C=C3)Cl)N4C=CC(=N4)C)C(F)(F)F)N.C1=CC=C(C=C1)C(=O)NCC(=O)O

Solubility

In vitro
Batch:

DMSO : 100 mg/mL (132.59 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 50 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	5.000mg/ml (6.63mM)	Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	5.000mg/ml (6.63mM)	Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC₅₀/Ki	Tryptophan hydroxylase ^[1]
In vivo	Telotristat Etiprate (LX 1606 Hippurate) (300 mg/kg p.o.) significantly reduces 5-HT in the gut and blood, but not brain 5-HT. At 200 mg/kg p.o., this compound alleviates the severity of trinitrobenzene sulfonic acid (TNBS)-induced colitis with lower expression of some genes encoding inflammation-related cytokines and chemokines in mice. ^[2]
References	[1] http://meeting.ascopubs.org/cgi/content/abstract/27/15S/e14555 [2] https://pubmed.ncbi.nlm.nih.gov/23749550/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT03442725	Completed	Renal Impairment	Ipsen	February 9 2018	Phase 1
NCT03423446	Completed	Hepatic Impairment	Lexicon Pharmaceuticals	November 28 2017	Phase 1
NCT02683577	Completed	Hepatic Impairment	Ipsen	February 2016	Phase 1
NCT02195635	Completed	Drug Interactions	Lexicon Pharmaceuticals	July 2014	Phase 1

Tech Support

Handling Instructions

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