LY2365109 hydrochloride

Name: LY2365109 hydrochloride
Brand: MedChemExpress
SKU: HY-100416A
Rating: 4.5 (1 reviews)

Cat. No.: HY-100416A Purity: 98.69%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

LY2365109 hydrochloride is a potent and selective GlyT1 inhibitor, with an IC₅₀ of 15.8 nM for glycine uptake in cells over-expressing hGlyT1a.

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

LY2365109 hydrochloride Chemical Structure

CAS No. : 1779796-27-8

Size	Price	Stock	Quantity

Free Sample (0.1 - 0.5 mg)		Apply Now
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 110	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 110	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 100	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 160	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 300	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 450	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 650	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of LY2365109 hydrochloride:

LY2365109 Get quote

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GlyT1 GlyT2

Biological Activity
Purity & Documentation
References
Customer Review

Description

LY2365109 hydrochloride is a potent and selective GlyT1 inhibitor, with an IC₅₀ of 15.8 nM for glycine uptake in cells over-expressing hGlyT1a^[1]^[2].

IC₅₀ & Target

hGlyT1

15.8 nM nM (IC₅₀)

In Vivo

LY2365109 hydrochloride (0.3-30 mg/kg; p.o.) produces dose-dependent elevations in CSF levels of glycine^[1].
LY2365109 hydrochloride increases seizure thresholds in mice^[2].

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

Animal Model:	Male Sprague-Dawley rats (250-300 g)^[1]
Dosage:	0.3 mg/kg, 1 mg/kg, 5 mg/kg, 10 mg/kg, 30 mg/kg
Administration:	Oral administration
Result:	Produced dose-dependent elevations in CSF levels of glycine measured 1 h after dosing.

Molecular Weight

421.91

Formula

C₂₂H₂₈ClNO₅

CAS No.

1779796-27-8

Appearance

Solid

Color

White to off-white

SMILES

O=C(O)CN(CCOC1=CC=C(C2=CC=C(OCO3)C3=C2)C=C1C(C)(C)C)C.Cl[H]

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility

In Vitro:

DMSO : ≥ 31 mg/mL (73.48 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : 1 mg/mL (2.37 mM; ultrasonic and warming and heat to 80°C)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.3702 mL	11.8509 mL	23.7017 mL
5 mM	0.4740 mL	2.3702 mL	4.7403 mL
10 mM	0.2370 mL	1.1851 mL	2.3702 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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

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 (5.93 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 (5.93 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 (5.93 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).

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

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: 98.69%

Select Batch:

Data Sheet (272 KB) SDS (393 KB)

COA (246 KB) LCMS (267 KB)

Handling Instructions (2659 KB)

References

[1]. Perry KW et al. Neurochemical and behavioral profiling of the selective GlyT1 inhibitors ALX5407 and LY2365109 indicate a preferential action in caudal vs. cortical brain areas. Neuropharmacology. 2008 Oct;55(5):743-54. [Content Brief]

[2]. Shen HY et al. Glycine transporter 1 is a target for the treatment of epilepsy. Neuropharmacology. 2015 Dec;99:554-65. [Content Brief]

Complete Stock Solution Preparation Table

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

H₂O / DMSO	1 mM	2.3702 mL	11.8509 mL	23.7017 mL	59.2543 mL
DMSO	5 mM	0.4740 mL	2.3702 mL	4.7403 mL	11.8509 mL
	10 mM	0.2370 mL	1.1851 mL	2.3702 mL	5.9254 mL
	15 mM	0.1580 mL	0.7901 mL	1.5801 mL	3.9503 mL
	20 mM	0.1185 mL	0.5925 mL	1.1851 mL	2.9627 mL
	25 mM	0.0948 mL	0.4740 mL	0.9481 mL	2.3702 mL
	30 mM	0.0790 mL	0.3950 mL	0.7901 mL	1.9751 mL
	40 mM	0.0593 mL	0.2963 mL	0.5925 mL	1.4814 mL
	50 mM	0.0474 mL	0.2370 mL	0.4740 mL	1.1851 mL
	60 mM	0.0395 mL	0.1975 mL	0.3950 mL	0.9876 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.