1. GPCR/G Protein
    Neuronal Signaling
  2. Somatostatin Receptor
  3. MK-4256

MK-4256 

Cat. No.: HY-13466 Purity: 98.63%
Handling Instructions

MK-4256 is a potent and selective SSTR3 antagonist with IC50s of 0.66 nM and 0.36 nM in human and mouse receptor binding assays, respectively.

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

MK-4256 Chemical Structure

MK-4256 Chemical Structure

CAS No. : 1104599-69-0

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 587 In-stock
Estimated Time of Arrival: December 31
1 mg USD 180 In-stock
Estimated Time of Arrival: December 31
5 mg USD 540 In-stock
Estimated Time of Arrival: December 31
10 mg USD 900 In-stock
Estimated Time of Arrival: December 31
25 mg USD 1800 In-stock
Estimated Time of Arrival: December 31
50 mg USD 2640 In-stock
Estimated Time of Arrival: December 31
100 mg USD 3960 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

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Description

MK-4256 is a potent and selective SSTR3 antagonist with IC50s of 0.66 nM and 0.36 nM in human and mouse receptor binding assays, respectively.

IC50 & Target

IC50: 0.66 nM (human SSTR3), 0.36 nM (mouse SSTR3)[1]

In Vitro

MK-4256 has excellent selectivity against other SSTR subtypes based on in vitro assays. In human receptor binding assays, MK-4256 has IC50s >2 μM for SSTR1 and SSTR2. Although the binding IC50 values on SSTR4 and SSTR5 are below 1 μM, there is still >500-fold selectivity. MK-4256 is tested in functional antagonist assays against SSTR4 and SSTR5. The IC50 values are greater than 5 μM (at least 5000-fold selectivity)[1]. MK-4256 inhibits radiolabeled MK-499 binding of the hERG channel with an IC50=1.74 μM. In a functional patch clamp assay, MK-4256 exhibits 50% blockade of hERG at 3.4 μM concentration[2].

In Vivo

MK-4256 reduces glucose excursion in a dose-dependent fashion with maximal efficacy achieves at doses as low as 0.03 mg/kg po. MK-4256 demonstrates exceptional SSTR3-mediated glucose-lowering efficacy in the mouse oGTT model with minimal hypoglycemia risk. MK-4256 achieves complete ablation of glucose excursion (109%) at 1 mg/kg po. MK-4256 reduces the glucose excursion from 0.003 to 10 mg/kg in a dose-dependent manner. The plasma Cmax of MK-4256 is determined from parallel mouse PK studies. At 0.01, 0.1, and 1 mg/kg oral dose, MK-4256 achieves Cmax of 7, 88, and 493 nM, respectivley[1].

Molecular Weight

494.52

Formula

C₂₇H₂₃FN₈O

CAS No.

1104599-69-0

SMILES

CN1N=CC([[email protected]@]2(C3=NOC(C)=N3)N[[email protected]@H](C4=NC=C(C5=CC=C(F)C=C5)N4)CC6=C2NC7=C6C=CC=C7)=C1

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 : ≥ 100 mg/mL (202.22 mM)

H2O : < 0.1 mg/mL (insoluble)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.0222 mL 10.1108 mL 20.2216 mL
5 mM 0.4044 mL 2.0222 mL 4.0443 mL
10 mM 0.2022 mL 1.0111 mL 2.0222 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 3 mg/mL (6.07 mM); Clear solution

  • 2.

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

    Solubility: ≥ 3 mg/mL (6.07 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
Animal Administration
[1]

Mice[1]
To demonstrate that the observed glucose lowering by MK-4256 is SSTR3-dependent, the effect of a maximally efficacious dosage of MK-4256 on blood glucose excursion during an oGTT was investigated in SSTR3 KO mice. Administration of MK-4256 (1 mg/kg) and compound A (1 mg/kg; des-F-sitagliptin, a DPP-4 inhibitor included as a positive control) to age-matched C57BL/6N male WT mice significantly inhibits blood glucose excursion by 112 and 91%, respectively.

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

References
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Keywords:

MK-4256MK4256MK 4256Somatostatin ReceptorSSTRsSSTRInhibitorinhibitorinhibit

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