[CAS NO. 1423018-12-5] LY2922470

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PRODUCTS SPECIFICATIONS [1423018-12-5]

Catalog

HY-19835

Brand

MCE

CAS

1423018-12-5

DESCRIPTION [1423018-12-5]

Overview

MDL	-
Molecular Weight	475.60
Molecular Formula	C28H29NO4S
SMILES	COC1=C(N(CC2=CC=C(COC3=CC=C([C@@H](C#CC)CC(O)=O)C=C3)S2)CCC4)C4=CC=C1

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

Summary

LY2922470 is a potent, selective and orally available agonist of the G protein-coupled receptor 40 (GPR40) , with EC ₅₀ s of 7 nM, 1 nM and 3 nM for human GPR40, mouse GPR40 and rat GPR40, respectively. LY2922470 reduces glucose levels along with significant increases in insulin and GLP-1 , is potential for the treatment of type 2 diabetes mellitus (T2DM) ^[1] .

IC50 & Target

EC50：7 nM (human GPR40), 1 nM (mouse GPR40), 3 nM (rat GPR40) ^[1]

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase
NCT01867216	Eli Lilly and Company	Diabetes Mellitus, Type 2	June 2013	Phase 1
NCT01746017	Eli Lilly and Company	Diabetes Mellitus, Type 2	December 2012	Phase 1

Appearance

Solid

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, protect from light

* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility

In Vitro:

DMSO : ≥ 125 mg/mL ( 262.83 mM )

* "≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.1026 mL	10.5130 mL	21.0261 mL
5 mM	0.4205 mL	2.1026 mL	4.2052 mL
10 mM	0.2103 mL	1.0513 mL	2.1026 mL

* Please refer to the solubility information to select the appropriate solvent.

In Vivo:

1.

Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

Solubility: ≥ 2.08 mg/mL (4.37 mM); Clear solution
2.

Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)

Solubility: ≥ 2.08 mg/mL (4.37 mM); Clear solution
3.

Add each solvent one by one: 10% DMSO >> 90% corn oil

Solubility: ≥ 2.08 mg/mL (4.37 mM); Clear solution

* All of the co-solvents are available by MCE.

References

[1] Hamdouchi C, et al. The Discovery, Preclinical, and Early Clinical Development of Potent and Selective GPR40 Agonists for the Treatment of Type 2 Diabetes Mellitus (LY2881835, LY2922083, and LY2922470). J Med Chem. 2016 Dec 22;59(24):10891-10916.

Synonyms

Benzenepropanoic acid, 4-[[5-[(3,4-dihydro-8-methoxy-1(2H)-quinolinyl)methyl]-2-thienyl]methoxy]-β-1-propyn-1-yl-, (βS)-

(βS)-4-[[5-[(3,4-Dihydro-8-methoxy-1(2H)-quinolinyl)methyl]-2-thienyl]methoxy]-β-1-propyn-1-ylbenzenepropanoic acid

LY 2922470

(S)-3-(4-((5-((8-Methoxy-3,4-dihydroquinolin-1(2H)-yl)methyl)thiophen-2-yl)methoxy)phenyl)hex-4-ynoic acid