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Art. -Nr.: HY-12819

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MK-1421

MK-1421 is an orally active sstr3 antagonist. MK-1421 inhibits sstr3 with IC₅₀ values of 2.3 nM (human), 1.3 nM (mouse), 0.6 nM (rat), 2.5 nM (dog), and 1.0 nM (rhesus monkey). MK-1421 inhibits hERG (human IC₅₀ 32.2 μM). MK-1421 dose-dependently reduces blood glucose fluctuations and enhances insulin secretion under high glucose conditions but not low glucose conditions, without affecting glucagon or somatostatin release. MK-1421 can be used for research on type 2 diabetes.

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CAS. Nr.: 1235995-16-0
Formel: C₂₇H₂₄FN₉O₂
Molecular Weight:525.54

Speicherung:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (292 KB)

MK-1421 Chemical Structure

CAS. Nr.: 1235995-16-0

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

^[1]

hsst₃

2.3 nM (IC₅₀)

mouse sstr3

1.3 nM (IC₅₀)

rat sstr3

0.6 nM (IC₅₀)

dog sstr3

2.5 nM (IC₅₀)

rhesus sstr3

1.0 nM (IC₅₀)

Alle Somatostatin Receptor Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
CHO	IC₅₀	>100000 nM Compound: 17e , MK-1421	Displacement of [125I]SS-14 from human recombinant SSTR4 expressed in CHO cell membranes incubated for 60 to 90 mins by radioligand binding assay Displacement of [125I]SS-14 from human recombinant SSTR4 expressed in CHO cell membranes incubated for 60 to 90 mins by radioligand binding assay	[PMID: 26005524]
CHO	IC₅₀	1.1 nM Compound: 17e , MK-1421	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	1.3 nM Compound: 17e , MK-1421	Displacement of [125I]SS-14 from mouse recombinant SSTR3 expressed in CHO cell membranes incubated for 60 to 90 mins by radioligand binding assay Displacement of [125I]SS-14 from mouse recombinant SSTR3 expressed in CHO cell membranes incubated for 60 to 90 mins by radioligand binding assay	[PMID: 26005524]
CHO	IC₅₀	2.3 nM Compound: 17e , MK-1421	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	5776 nM Compound: 17e , MK-1421	Displacement of [125I]SS-14 from human recombinant SSTR1 expressed in CHO cell membranes incubated for 60 to 90 mins by radioligand binding assay Displacement of [125I]SS-14 from human recombinant SSTR1 expressed in CHO cell membranes incubated for 60 to 90 mins by radioligand binding assay	[PMID: 26005524]
CHO	IC₅₀	9240 nM Compound: 17e , MK-1421	Displacement of [125I]SS-14 from human recombinant SSTR5 expressed in CHO cell membranes incubated for 60 to 90 mins by radioligand binding assay Displacement of [125I]SS-14 from human recombinant SSTR5 expressed in CHO cell membranes incubated for 60 to 90 mins by radioligand binding assay	[PMID: 26005524]
CHO	IC₅₀	>100000 nM Compound: 17e , MK-1421	Displacement of [125I]SS-14 from human recombinant SSTR2 expressed in CHO cell membranes incubated for 60 to 90 mins by radioligand binding assay Displacement of [125I]SS-14 from human recombinant SSTR2 expressed in CHO cell membranes incubated for 60 to 90 mins by radioligand binding assay	[PMID: 26005524]

In Vitro

MK-1421 (compound 17e) (5 μM; 60 minutes; 2-16 mM glucose) enhances insulin secretion in isolated human pancreatic islets in a glucose-dependent manner^[1].
MK-1421 binds to human sstr3 with an IC₅₀ of 2.3 nM and exhibits functional antagonism with an IC₅₀ of 1.1 nM, and is highly selective for human sstr1, sstr2, sstr4, and sstr5^[1].

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

In Vivo

MK-1421 (compound 17e) (0.03-3 mg/kg; oral; single administration 1 hour before Dextrose (D-Glucose) (HY-B0389) challenge) improves glucose tolerance in lean mice by dose-dependently inhibiting blood glucose excursions during oGTT^[1].

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

Animal Model:

C57BL/6N (lean)^[1]
Dosage:

0.03 mg/kg; 0.1 mg/kg; 0.3 mg/kg; 1 mg/kg; 3 mg/kg
Administration:

p.o.; single dose 1 h prior to dextrose challenge
Result:

Reduced blood glucose excursion in a dose-dependent manner from 0.03 mg/kg to 3 mg/kg.
At 3 mg/kg, inhibition was near 100%.
ED50 for 17e-induced suppression of oGTT glucose levels in mouse was 0.16 mg/kg.
MEDmax (minimal efficacious dose for maximal suppression of blood glucose during oGTT) was 3 mg/kg.

Related Protocols :

Chemical Information

CAS. Nr. 1235995-16-0
Molecular Weight 525.54
Formel C₂₇H₂₄FN₉O₂
SMILES

FC(C=C1)=CN=C1C2=CNC([C@@H]3N[C@@](C4=CN(CC)N=C4)(C5=NN(C)C(O5)=O)C6=C(C(C=CC=C7)=C7N6)C3)=N2
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

Please store the product under the recommended conditions in the Certificate of Analysis.

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (292 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)
Handling Instructions (2659 KB)

Verweise

[1]. Shah SK, et al. Discovery of MK-1421, a Potent, Selective sstr3 Antagonist, as a Development Candidate for Type 2 Diabetes. ACS medicinal chemistry letters. 2015 May 14;6(5):513-7. [Content Brief]

Calculators

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

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.

Bioz

Keywords

MOQ

Minimum order quantity

100 mg

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