Cat. No.: HY-13466

MK-4256

5 Cited Publications

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Based on 5 publication(s) in Google Scholar

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.

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Pureté: 99.07%
CAS No.: 1104599-69-0
Formule: C₂₇H₂₃FN₈O
Masse moléculaire:494.52

Stockage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

MK-4256 Chemical Structure

CAS No.: 1104599-69-0

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Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (5)
Solvant et solubilité
- In Vitro
- In Vivo
Protocole
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

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]

Voir tous les produits spécifiques à Isoform Somatostatin Receptor :

Cellular Effect

Cell Line	Type	Value	Description	References
CHO	IC₅₀	0.36 nM Compound: 8, MK-4256	Displacement of [125I]SS-28 from mouse SSTR3 transfected in CHO cells after 60 to 90 mins Displacement of [125I]SS-28 from mouse SSTR3 transfected in CHO cells after 60 to 90 mins	[PMID: 24900499]
CHO	IC₅₀	0.46 nM Compound: 8, MK-4256	Inhibition of mouse SSTR3 transfected in CHO cells assessed as inhibition of SRIF-induced reduction of cAMP accumulation after 45 mins Inhibition of mouse SSTR3 transfected in CHO cells assessed as inhibition of SRIF-induced reduction of cAMP accumulation after 45 mins	[PMID: 24900499]
CHO	IC₅₀	0.66 nM Compound: 8, MK-4256	Displacement of [125I]SS-28 from human SSTR3 transfected in CHO cells after 60 to 90 mins Displacement of [125I]SS-28 from human SSTR3 transfected in CHO cells after 60 to 90 mins	[PMID: 24900499]
CHO	IC₅₀	0.7 nM Compound: 1, MK-4256	Displacement of [125I]SS-14 from human recombinant SSTR3 expressed in CHO cell membranes incubated for 60 to 90 mins by radioligand binding assay Displacement of [125I]SS-14 from human recombinant SSTR3 expressed in CHO cell membranes incubated for 60 to 90 mins by radioligand binding assay	[PMID: 26005524]
CHO	IC₅₀	0.9 nM Compound: 1, MK-4256	Antagonist activity against human recombinant SSTR3 expressed in CHO cells assessed as reduction in forskolin-induced cAMP accumulation in presence of SS-14 by time-resolved fluorescence assay Antagonist activity against human recombinant SSTR3 expressed in CHO cells assessed as reduction in forskolin-induced cAMP accumulation in presence of SS-14 by time-resolved fluorescence assay	[PMID: 26005524]
CHO	IC₅₀	0.95 nM Compound: 8, MK-4256	Inhibition of human SSTR3 transfected in CHO cells assessed as inhibition of SRIF-induced reduction of cAMP accumulation after 45 mins Inhibition of human SSTR3 transfected in CHO cells assessed as inhibition of SRIF-induced reduction of cAMP accumulation after 45 mins	[PMID: 24900499]
CHO	IC₅₀	2362 nM Compound: 8, MK-4256	Displacement of [125I]SS-28 from human SSTR-1 transfected in CHO cells after 60 to 90 mins Displacement of [125I]SS-28 from human SSTR-1 transfected in CHO cells after 60 to 90 mins	[PMID: 24900499]
CHO	IC₅₀	384 nM Compound: 8, MK-4256	Displacement of [125I]SS-28 from human SSTR-4 transfected in CHO cells after 60 to 90 mins Displacement of [125I]SS-28 from human SSTR-4 transfected in CHO cells after 60 to 90 mins	[PMID: 24900499]
CHO	IC₅₀	4025 nM Compound: 8, MK-4256	Displacement of [125I]SS-14 from human SSTR-2 transfected in CHO cells after 60 to 90 mins Displacement of [125I]SS-14 from human SSTR-2 transfected in CHO cells after 60 to 90 mins	[PMID: 24900499]
CHO	IC₅₀	533 nM Compound: 8, MK-4256	Displacement of [125I]SS-28 from human SSTR-5 transfected in CHO cells after 90 to 120 mins Displacement of [125I]SS-28 from human SSTR-5 transfected in CHO cells after 90 to 120 mins	[PMID: 24900499]
CHO-K1	IC₅₀	0.46 nM Compound: MK-4256	Antagonist activity at mouse SST3 expressed in CHO-K1 cells assessed as inhibition of SRIF-14-induced foreskin-stimulated cAMP accumulation after 45 mins by TR-FRET assay Antagonist activity at mouse SST3 expressed in CHO-K1 cells assessed as inhibition of SRIF-14-induced foreskin-stimulated cAMP accumulation after 45 mins by TR-FRET assay	[PMID: 24944745]
CHO-K1	IC₅₀	0.95 nM Compound: MK-4256	Antagonist activity at human SST3 expressed in CHO-K1 cells assessed as inhibition of SRIF-14-induced foreskin-stimulated cAMP accumulation after 45 mins by TR-FRET assay Antagonist activity at human SST3 expressed in CHO-K1 cells assessed as inhibition of SRIF-14-induced foreskin-stimulated cAMP accumulation after 45 mins by TR-FRET assay	[PMID: 24944745]

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].

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

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 C_max of MK-4256 is determined from parallel mouse PK studies. At 0.01, 0.1, and 1 mg/kg oral dose, MK-4256 achieves C_max of 7, 88, and 493 nM, respectivley^[1].

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

Chemical Information

CAS No. 1104599-69-0
Appearance Solid
Masse moléculaire 494.52
Formule C₂₇H₂₃FN₈O
Color Light yellow to yellow
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
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (5)

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Journal Impact Factor

Cell Syst

Pancreatic islet oscillation rhythmicity arises from δ and α cell interactions. [Abstract]

2026 Jun 17;17(6):101587. PMID: 41997145
Acta Physiol

In the rat pancreas, somatostatin tonically inhibits glucagon secretion and is required for glucose-induced inhibition of glucagon secretion. [Abstract]

2020 Jul;229(3):e13464. PMID: 32145704
Am J Physiol Endocrinol Metab

A role for vagal activity in preventing the suppression of glucagon secretion by GLP-1 during hypoglycemia. [Abstract]

2026 May 1;330(5):E737-E746. PMID: 41973537
Islets

Beta cell primary cilia mediate somatostatin responsiveness via SSTR3. [Abstract]

2023 Dec 31;15(1):2252855. PMID: 37660302
bioRxiv

Pancreatic α-cells are functionally heterogeneous and sex-dependently regulated by neighboring endocrine cells. [Abstract]

2025 Aug 28:2025.08.23.671946. PMID: 40909609

Solvant et solubilité

In Vitro:

DMSO : ≥ 100 mg/mL (202.22 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

* "≥" means soluble, but saturation unknown.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Calculateur de molarité

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 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

This protocol yields a clear solution of ≥ 3 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (30.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil

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

This protocol yields a clear solution of ≥ 3 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (30.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Protocole

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.

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

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (281 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[1]. 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. [Content Brief]

[2]. He S, et al. Investigation of Cardiovascular Effects of Tetrahydro-β-carboline sstr3 antagonists. ACS Med Chem Lett. 2014 Apr 21;5(7):748-53. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.0222 mL	10.1108 mL	20.2216 mL	50.5541 mL
	5 mM	0.4044 mL	2.0222 mL	4.0443 mL	10.1108 mL
	10 mM	0.2022 mL	1.0111 mL	2.0222 mL	5.0554 mL
	15 mM	0.1348 mL	0.6741 mL	1.3481 mL	3.3703 mL
	20 mM	0.1011 mL	0.5055 mL	1.0111 mL	2.5277 mL
	25 mM	0.0809 mL	0.4044 mL	0.8089 mL	2.0222 mL
	30 mM	0.0674 mL	0.3370 mL	0.6741 mL	1.6851 mL
	40 mM	0.0506 mL	0.2528 mL	0.5055 mL	1.2639 mL
	50 mM	0.0404 mL	0.2022 mL	0.4044 mL	1.0111 mL
	60 mM	0.0337 mL	0.1685 mL	0.3370 mL	0.8426 mL
	80 mM	0.0253 mL	0.1264 mL	0.2528 mL	0.6319 mL
	100 mM	0.0202 mL	0.1011 mL	0.2022 mL	0.5055 mL

Keywords

MK-4256

5 Cited Publications

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MK-4256

MCE Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) MK-4256

Voir tous les produits spécifiques à Isoform Somatostatin Receptor

Activité biologique

Chemical Information

Publications (5)

Solvant et solubilité

Protocole

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

MK-4256

MCE Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) MK-4256

Voir tous les produits spécifiques à Isoform Somatostatin Receptor

Activité biologique

Chemical Information

Publications (5)

Solvant et solubilité

Protocole

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

MK-4256 Related Classifications

HY-13466 Related Classifications