Structure
MK-4256, inhibitor
MK-4256
Purity
98.00%
Synonyms
MK-4256; inhibitor
Purity/Purification
98.00%
Form/Format
Solid. Powder
Solubility
DMSO: 100mg/mL (202.22mM)
(<1mg/ml refers to the product slightly soluble or insoluble)
(<1mg/ml refers to the product slightly soluble or insoluble)
Formula
C27H23FN8O
SMILES
CN1N=CC([C@@]2(C3=NOC(C)=N3)N[C@@H](C4=NC=C(C5=CC=C(F)C=C5)N4)CC6=C2NC7=C6C=CC=C7)=C1
CAS Number
1104599-69-0
Target & IC50
uman SSTR3: ic50 0.66nM
mouse SSTR3: ic50 0.36nM
mouse SSTR3: ic50 0.36nM
In Vitro
MK-4256 decreases the glucose excursion from 0.003 to 10mg/kg in a dose-dependent manner. MK-4256 decreases glucose excursion in a dose-dependent fashion with maximal efficacy achieves at doses of MK-4256 (0.03mg/kg; p.o.) demonstrates exceptional SSTR3-mediated glucose-lowering efficacy in the mouse oGTT model with minimal hypoglycemia risk. MK-4256 (1mg/kg; p.o.) achieves complete ablation of glucose excursion (109%). The plasma Cmax of MK-4256 is determined from parallel mouse PK studies. MK-4256 achieves Cmax of 7, 88, and 493nM, respectively, at 0.01, 0.1, and 1mg/kg oral dose [1].
Preparation and Storage
Store at -20 degree C for 3 years powder
-80 degree C for 2 years in solvent
-80 degree C for 2 years in solvent
Structure
Structure
Related Product Information for MK-4256, inhibitor
MK-4256 is an effective and selective SSTR3 antagonist (IC50s: 0.66nM and 0.36nM in human and mouse receptor binding assays, respectively).
References
He S, et al. The Discovery of MK-4256, a Potent SSTR3 Antagonist as a Potential treatment,of Type 2 Diabetes. ACS Med Chem Lett. 2012 May 7;3(6):484-9.
He S, et al. The Discovery of MK-4256, a Potent SSTR3 Antagonist as a Potential treatment,of Type 2 Diabetes. ACS Med Chem Lett. 2012 May 7;3(6):484-9.
He S, et al. Investigation of Cardiovascular Effects of Tetrahydro-beta-carboline sstr3 antagonists. ACS Med Chem Lett. 2014 Apr 21;5(7):748-53.
He S, et al. Investigation of Cardiovascular Effects of Tetrahydro-beta-carboline sstr3 antagonists. ACS Med Chem Lett. 2014 Apr 21;5(7):748-53.
He S, et al. The Discovery of MK-4256, a Potent SSTR3 Antagonist as a Potential treatment,of Type 2 Diabetes. ACS Med Chem Lett. 2012 May 7;3(6):484-9.
He S, et al. Investigation of Cardiovascular Effects of Tetrahydro-beta-carboline sstr3 antagonists. ACS Med Chem Lett. 2014 Apr 21;5(7):748-53.
He S, et al. Investigation of Cardiovascular Effects of Tetrahydro-beta-carboline sstr3 antagonists. ACS Med Chem Lett. 2014 Apr 21;5(7):748-53.
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Product Notes
The MK-4256 (Catalog #AAA5755199) is an Inhibitor and is intended for research purposes only. The product is available for immediate purchase. It is sometimes possible for the material contained within the vial of "MK-4256, Inhibitor" to become dispersed throughout the inside of the vial, particularly around the seal of said vial, during shipment and storage. We always suggest centrifuging these vials to consolidate all of the liquid away from the lid and to the bottom of the vial prior to opening. Please be advised that certain products may require dry ice for shipping and that, if this is the case, an additional dry ice fee may also be required.Precautions
All products in the AAA Biotech catalog are strictly for research-use only, and are absolutely not suitable for use in any sort of medical, therapeutic, prophylactic, in-vivo, or diagnostic capacity. By purchasing a product from AAA Biotech, you are explicitly certifying that said products will be properly tested and used in line with industry standard. AAA Biotech and its authorized distribution partners reserve the right to refuse to fulfill any order if we have any indication that a purchaser may be intending to use a product outside of our accepted criteria.Disclaimer
Though we do strive to guarantee the information represented in this datasheet, AAA Biotech cannot be held responsible for any oversights or imprecisions. AAA Biotech reserves the right to adjust any aspect of this datasheet at any time and without notice. It is the responsibility of the customer to inform AAA Biotech of any product performance issues observed or experienced within 30 days of receipt of said product. To see additional details on this or any of our other policies, please see our Terms & Conditions page.Item has been added to Shopping Cart
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