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Cat. No.: HY-12819

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MK-1421

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.

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CAS No.: 1235995-16-0
Formule: C₂₇H₂₄FN₉O₂
Masse moléculaire:525.54

Stockage:

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

Data Sheet (272 KB)

MK-1421 Chemical Structure

CAS No.: 1235995-16-0

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

Activité biologique
- Description
- Cellular Effect
Chemical Information
Pureté et documentation
Références
Calculators
Help & FAQs
Classifications
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Activité biologique

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].

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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]

Chemical Information

CAS No. 1235995-16-0
Masse moléculaire 525.54
Formule 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
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage

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

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (272 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]. 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]

Calculators

Calculateur de molarité

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

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Concentration _(final) Concentration _(final)

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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.

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100 mg

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Activité biologique
- Description
Chemical Information
Pureté et documentation
Références

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MK-1421

Voir tous les produits spécifiques à Isoform Somatostatin Receptor

Activité biologique

Chemical Information

Pureté et documentation

Références

Calculators

Help & FAQs

MK-1421 Related Classifications

HY-12819 Related Classifications