[CAS NO. 1037792-44-1] MBX-2982

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PRODUCTS SPECIFICATIONS [1037792-44-1]

Catalog

HY-15291

Brand

MCE

CAS

1037792-44-1

DESCRIPTION [1037792-44-1]

Overview

MDL	MFCD22628771
Molecular Weight	448.54
Molecular Formula	C22H24N8OS
SMILES	CCC1=CN=C(N2CCC(C3=NC(COC4=CC=C(N5N=NN=C5)C=C4)=CS3)CC2)N=C1

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

8 Publications Citing Use of MCE

Summary

MBX-2982 is a selective, orally-available G protein-coupled receptor 119 ( GPR119 ) agonist.

IC50 & Target

GPR119 ^[1]

In Vitro

In cells pre-treated with MBX-2982 (1 µM) in “chronic incubation/washout” experiments, cAMP accumulation captured by IBMX inclusion is significantly increased compared to control cells (P<0.01; ANOVA; n=3-6) despite extensive washing to remove excess agonist. AR-231,453 produces sustained responses in a similar concentration range to those observed with acute stimulation (a small 1.82 fold shift), with pEC ₅₀ s of 8.67±0.11 and 8.93±0.17, respectively. Likewise, a large but less severe shift in concentration responses (57.54 fold) is observed for MBX-2982 with respective sustained and acute pEC ₅₀ s of 7.03±0.13 and 8.79±0.12 ^[1] .

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

In Vivo

To examine whether the observations in GLUTag and the primary intestinal cells has physiological relevance, C57BL/6 mice are treated with the GPR119 agonist MBX-2982 at a dose of 10 mg/kg. Note that in order to examine a direct GPR119 effect, no DPP-IV inhibitor is co-administered in this experiment, but a DPP-IV inhibitor is used to preserve active GLP-1 in the blood samples. The plasma GLP-1 levels from the mice dosed with MBX-2982 are increased without a glucose load, indicating that GPR119-mediated GLP-1 secretion is not dependent on glucose ^[2] .

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

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase
NCT04432090	AdventHealth Translational Research Institute	Diabetes Mellitus, Type 1	April 21, 2021	Phase 2
NCT01035879	CymaBay Therapeutics, Inc.	Diabetes	December 2009	Phase 2

Appearance

Solid

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : 50 mg/mL ( 111.47 mM ; Need ultrasonic)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.2295 mL	11.1473 mL	22.2946 mL
5 mM	0.4459 mL	2.2295 mL	4.4589 mL
10 mM	0.2229 mL	1.1147 mL	2.2295 mL

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

In Vivo:

1.

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

Solubility: ≥ 2.75 mg/mL (6.13 mM); Clear solution

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