LGD-6972 sodium

This product is for research use only, not for human use. We do not sell to patients.

For small sizes, please check our retail website as below: www.invivochem.com

Size	Price	Stock
5mg	$345	To Be Confirmed
10mg	$500	To Be Confirmed
25mg	$860	To Be Confirmed
50mg	$1260	To Be Confirmed
100mg	$1800	To Be Confirmed
250mg	$2980	To Be Confirmed

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Cat #: V3774 CAS #: 1207989-22-7 Purity ≥ 98%

Description: LGD-6972 soidum (LGD6972; MB-11262; MB11262) is a novel and orally bioavailable glucagon receptor antagonist with antidiabetic effects. It has linear plasma pharmacokinetics consistent with once daily dosing that is comparable in healthy and T2DM subjects. It also reduces plasma glucose in the postprandial state. Dose-dependent increases in fasting plasma glucagon are observed, but glucagon levels decrease and insulin levels increase after an oral glucose load in T2DM subjects. Inhibition of glucagon action by LGD-6972 was associated with decreases in glucose in both healthy and T2DM subjects, the magnitude of which was sufficient to predict improvement in glycaemic control with longer treatment duration in T2DM patients. The safety and pharmacological profile of LGD-6972 after 14 days of dosing supports continued clinical development.

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Physicochemical and Storage Information
Protocol
Related Biological Data
Stock Solution Preparation
Quality Control Documentation

Molecular Weight (MW)	724.89
Molecular Formula	C43H45N2NaO5S
CAS No.	1207989-22-7
Storage	-20℃ for 3 years in powder form
Storage	-80℃ for 2 years in solvent
Solubility In Vitro	DMSO: ≥ 31 mg/mL
	Water: N/A
	Ethanol: N/A
Synonyms	LGD6972; LGD 6972; LGD-6972 sodium

Protocol	In Vitro	In vitro activity: LGD-6972 is a novel and orally available glucagon receptor antagonist that has linear plasma pharmacokinetics consistent with once daily dosing that is comparable in healthy and T2DM subjects. It also reduces plasma glucose in the postprandial state. Dose-dependent increases in fasting plasma glucagon are observed, but glucagon levels decrease and insulin levels increase after an oral glucose load in T2DM subjects. Inhibition of glucagon action by LGD-6972 was associated with decreases in glucose in both healthy and T2DM subjects, the magnitude of which was sufficient to predict improvement in glycaemic control with longer treatment duration in T2DM patients. The safety and pharmacological profile of LGD-6972 after 14 days of dosing supports continued clinical development.
Protocol	In Vivo	LGD-6972 reduces plasma glucose in the postprandial state. Dose-dependent increases in fasting plasma glucagon are observed, but glucagon levels decrease and insulin levels increase after an oral glucose load in T2DM subjects. LGD-6972 is well tolerated at the doses tested without dose-related or clinically meaningful changes in clinical laboratory parameters. No subject experiences hypoglycaemia.

These protocols are for reference only. InvivoChem does not independently validate these methods.

Related Biological Data

Mean (± SEM) plasma LGD‐6972 concentration versus time profiles by dose for healthy and T2DM subjects in the SAD and the MAD studies.Diabetes Obes Metab. 2017 Jan;19(1):24-32.

Mean (± SEM) change from baseline fasting plasma glucose (FPG) versus time profiles for healthy and T2DM subjects in the SAD and the MAD studies who received PBO or LGD‐6972, Diabetes Obes Metab. 2017 Jan;19(1):24-32.

Effect of LGD‐6972 on mean (± SEM) plasma glucose, glucagon and insulin levels in response to an oral glucose load during an oral glucose tolerance test in the MAD study. Diabetes Obes Metab. 2017 Jan;19(1):24-32.

Preparing Stock Solutions

Solvent volume to be added	Mass (the weight of a compound)
Mother liquor concentration	1mg	5mg	10mg	20mg
1mM	1.3795 mL	6.8976 mL	13.7952 mL	27.5904 mL
5mM	0.2759 mL	1.3795 mL	2.7590 mL	5.5181 mL
10mM	0.1380 mL	0.6898 mL	1.3795 mL	2.7590 mL
20mM	0.0690 mL	0.3449 mL	0.6898 mL	1.3795 mL

Quality Control Documentation	Select Batch Purity ≥ 98% COA MSDS NMR HPLC

The molarity calculator equation

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

Mass

Concentration

Volume

Molecular Weight*

The dilution calculator equation

Concentration_(start) × Volume_(start) = Concentration_(final) × Volume_(final)

This equation is commonly abbreviated as: C₁ V₁ = C₂ V₂

Concentration_(start)

Volume_(start)

Concentration_(final)

Volume_(final)

Step One: Enter information below

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

Step Two: Enter the in vivo formulation

%DMSO + % + %Tween 80 + %ddH₂O

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 add µL PEG300, mix and clarify, next add µL Tween 80,mix and clarify, next add µL ddH₂O,mix and clarify.

Note:

(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.