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[CAS NO. 1037792-44-1] MBX-2982
| Ships within | Stock | Price | Qty | Total |
Please click "REQUEST A QUOTE" button if there is no stock, or you need other sizes or custom synthesis.
| Catalog: | HY-15291 |
| Brand: | MCE |
| CAS: | 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 |
8 Publications Citing Use of MCE
- [1]Nat Commun. 2022 Nov 17;13(1):7033.
- [2]J Exp Clin Cancer Res. 2018 Nov 29;37(1):295.
- [3]FASEB J. 2016 Jan;30(1):324-35.
- [4]Cell Commun Signal. 2019 May 23;17(1):49
- [5]Invest Ophthalmol Vis Sci. 2017 Jun 1;58(7):2930-2938.
- [6]Patent. US9895370B2.
- [7]Patent. US20170143714A1.
- [8]College of Pharmacy. Seoul National University. 2015 Aug.
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
DMSO : 50 mg/mL ( 111.47 mM ; Need ultrasonic)
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 |
-
1.
Add each solvent one by one: 10% DMSO >> 90% corn oil
Solubility: ≥ 2.75 mg/mL (6.13 mM); Clear solution
References
- [1] Hothersall JD, et al. Sustained wash-resistant receptor activation responses of GPR119 agonists. Eur J Pharmacol. 2015 Sep 5;762:430-42.
- [2] Lan H, et al. Agonists at GPR119 mediate secretion of GLP-1 from mouse enteroendocrine cells through glucose-independent pathways. Br J Pharmacol. 2012 Apr;165(8):2799-807.
- [3] Yang JW, et al. GPR119: a promising target for nonalcoholic fatty liver disease. FASEB J. 2016 Jan;30(1):324-35.
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