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.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 1235995-16-0
- 分子式: C27H24FN9O2
- 分子量:525.54
-
保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
生物活性
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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] |
化学情報
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CAS 番号 1235995-16-0
-
分子量 525.54
-
分子式 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
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輸送条件
Room temperature in continental US; may vary elsewhere.
-
保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)