You are here:Home-Chemical Inhibitors & Agonists-GPCR-Somatostatin Receptor-MK-4256
MK-4256

Chemical Structure : MK-4256

CAS No.: 1104599-69-0

MK-4256 (MK 4256;MK4256)

Catalog No.: PC-61088Not For Human Use, Lab Use Only.

A potent, selective, orally active somatostatin receptor SSTR3 antagonist with binding Ki of 0.66 nM, >500-fold selectivity over SSTR1/2/4/5.

Packing Price Stock Quantity
100 mg Get quote
250 mg Get quote
500 mg Get quote
1 g Get quote

Bulk size, bulk discount!

E-mail: sales@probechem.com

Tech Support: tech@probechem.com

Purity & Documentation Purity: >98% (HPLC)

Biological Activity

A potent, selective, orally active somatostatin receptor SSTR3 antagonist with binding Ki of 0.66 nM, >500-fold selectivity over SSTR1/2/4/5; reduces glucose excursion in a dose-dependent fashion with maximal efficacy achieved at doses as low as 0.03 mg/kg po, with minimal hypoglycemia risk; preclinical tirals are discontinued due to dose-dependent QTc in conscious cardiovascular (CV) dog model.

Physicochemical Properties

M.Wt 494.534
Formula C27H23FN8O
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

3-((1R,3R)-3-(5-(4-fluorophenyl)-1H-imidazol-2-yl)-1-(1-methyl-1H-pyrazol-4-yl)-2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indol-1-yl)-5-methyl-1,2,4-oxadiazole

References

1. He S, et al. ACS Med Chem Lett. 2012 May 7;3(6):484-9.

2. He S, et al. ACS Med Chem Lett. 2014 Apr 21;5(7):748-53.

3. He S, et al. Bioorg Med Chem Lett. 2016 Mar 15;26(6):1529-1535.

Copyright © 2022 probechem.com. All Rights Reserved. probechem Copyright

Contact Us sales@probechem.com

Bulk Inquiry

* Indicates a Required FieldYour information is safe with us.

  • *Product name:
  • *Applicant name:
  • *Email address:
  • *Organization name:
  • *Requested quantity:
  • *Country:
  • *Additional Information:

Get Quote

* Indicates a Required FieldYour information is safe with us.

  • *Product name:
  • *Applicant name:
  • *Email address:
  • *Organization name:
  • *Requested quantity:
  • *Country:
  • Additional Information: