MK-1421

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MK-1421 is a potent and selective sstr3 antagonist. MK-1421 regulates insulin secretion by binding to the sstr3. MK-1421 can be used in the research of type 2 diabetes.

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

MK-1421 Chemical Structure

CAS No. : 1235995-16-0

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SSTR1 SSTR2 SSTR3 SSTR5 SSTR4

Biological Activity
Purity & Documentation
References
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Description

MK-1421 is a potent and selective sstr3 antagonist. MK-1421 regulates insulin secretion by binding to the sstr3. MK-1421 can be used in the research of type 2 diabetes^[1].

Cellular Effect

Cell Line	Type	Value	Description	References
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]
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]

Molecular Weight

525.54

Formula

C₂₇H₂₄FN₉O₂

CAS No.

1235995-16-0

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Shah S K, et al. Discovery of MK-1421, a potent, selective sstr3 antagonist, as a development candidate for type 2 diabetes[J]. ACS Medicinal Chemistry Letters, 2015, 6(5): 513-517. [Content Brief]

MK-1421 Related Classifications

Metabolic Disease Endocrinology

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

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The dilution calculator equation

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)	×	Volume _(start)	=	Concentration _(final)	×	Volume _(final)
	×		=		×
C1		V1		C2		V2

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

MK-14211235995-16-0MK1421MK 1421Somatostatin ReceptorSSTRsSSTRSelective antagonistInsulinDiabetes mellitussstr3Inhibitorinhibitorinhibit

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