GI 181771
GI 181771 is a cholecystokinin 1 receptor agonist investigated for the treatment of obesity.
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: 305366-98-7
- 分子式: C34H31N5O6
- 分子量:605.64
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
生物活性
Target: Cholecystokinin 1 receptor[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO | EC50 |
0.8 nM
Compound: A, G1181771X
|
Activity at CCK1R (unknown origin) expressed in CHO cells assessed as stimulation of intracellular calcium responses
Activity at CCK1R (unknown origin) expressed in CHO cells assessed as stimulation of intracellular calcium responses
|
[PMID: 25862198] |
| CHO | EC50 |
10 pM
Compound: A, G1181771X
|
Activity at CCK1R (unknown origin) expressed in CHO cells assessed as CCK EC50 measured as intracellular calcium responses at 0.1 nM (Rvb = 7 to 14 pM)
Activity at CCK1R (unknown origin) expressed in CHO cells assessed as CCK EC50 measured as intracellular calcium responses at 0.1 nM (Rvb = 7 to 14 pM)
|
[PMID: 25862198] |
| CHO | EC50 |
13 pM
Compound: A, G1181771X
|
Activity at CCK1R (unknown origin) expressed in CHO cells assessed as CCK EC50 measured as intracellular calcium responses at 0.01 nM (Rvb = 7 to 14 pM)
Activity at CCK1R (unknown origin) expressed in CHO cells assessed as CCK EC50 measured as intracellular calcium responses at 0.01 nM (Rvb = 7 to 14 pM)
|
[PMID: 25862198] |
| CHO | EC50 |
190 pM
Compound: A, G1181771X
|
Activity at CCK1R (unknown origin) expressed in CHO cells assessed as CCK EC50 measured as intracellular calcium responses at 1 nM (Rvb = 7 to 14 pM)
Activity at CCK1R (unknown origin) expressed in CHO cells assessed as CCK EC50 measured as intracellular calcium responses at 1 nM (Rvb = 7 to 14 pM)
|
[PMID: 25862198] |
| CHO | EC50 |
2.4 pM
Compound: A, G1181771X
|
Activity at CCK1R (unknown origin) expressed in CHO cells assessed as CCK EC50 measured as intracellular calcium responses at 0.316 nM (Rvb = 7 to 14 pM)
Activity at CCK1R (unknown origin) expressed in CHO cells assessed as CCK EC50 measured as intracellular calcium responses at 0.316 nM (Rvb = 7 to 14 pM)
|
[PMID: 25862198] |
| CHO | EC50 |
283 nM
Compound: 1, GI181771X
|
Agonist activity at human CCK1 receptor expressed in CHO cells assessed as induction of calcium release by FLIPR assay
Agonist activity at human CCK1 receptor expressed in CHO cells assessed as induction of calcium release by FLIPR assay
|
[PMID: 20851601] |
| CHO | EC50 |
63.8 nM
Compound: 1, GI181771X
|
Agonist activity at rat CCK1 receptor expressed in CHO cells assessed as induction of calcium release by FLIPR assay
Agonist activity at rat CCK1 receptor expressed in CHO cells assessed as induction of calcium release by FLIPR assay
|
[PMID: 20851601] |
| CHO | IC50 |
105 nM
Compound: A, G1181771X
|
Displacement of [125I]CCK from CCK1R (unknown origin) expressed in CHO cells
Displacement of [125I]CCK from CCK1R (unknown origin) expressed in CHO cells
|
[PMID: 25862198] |
| CHO | IC50 |
128 nM
Compound: A, G1181771X
|
Displacement of [125I]BDZ1 from CCK1R (unknown origin) expressed in CHO cells
Displacement of [125I]BDZ1 from CCK1R (unknown origin) expressed in CHO cells
|
[PMID: 25862198] |
| CHO | IC50 |
131 nM
Compound: 1, GI181771X
|
Displacement of [125I]CCK8 from human CCK1 receptor expressed in CHO cells
Displacement of [125I]CCK8 from human CCK1 receptor expressed in CHO cells
|
[PMID: 20851601] |
| CHO | IC50 |
2.7 nM
Compound: A, G1181771X
|
Displacement of [125I]BDZ2 from CCK2R (unknown origin) expressed in CHO cells
Displacement of [125I]BDZ2 from CCK2R (unknown origin) expressed in CHO cells
|
[PMID: 25862198] |
| CHO | IC50 |
5.6 nM
Compound: A, G1181771X
|
Displacement of [125I]CCK from CCK2R (unknown origin) expressed in CHO cells
Displacement of [125I]CCK from CCK2R (unknown origin) expressed in CHO cells
|
[PMID: 25862198] |
| CHO | IC50 |
52.6 nM
Compound: 1, GI181771X
|
Displacement of [125I]CCK8 from rat CCK1 receptor expressed in CHO cells
Displacement of [125I]CCK8 from rat CCK1 receptor expressed in CHO cells
|
[PMID: 20851601] |
化学情報
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CAS 番号 305366-98-7
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分子量 605.64
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分子式 C34H31N5O6
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SMILES
O=C(O)C1=CC=CC(NC(N[C@H]2C(N(CC(N(C(C)C)C3=CC=CC=C3)=O)C4=CC=CC=C4N(C5=CC=CC=C5)C2=O)=O)=O)=C1
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輸送条件
Room temperature in continental US; may vary elsewhere.
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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
[1]. Myer JR, et al. Species- and dose-specific pancreatic responses and progression in single- and repeat-dose studies with GI181771X: a novel cholecystokinin 1 receptor agonist in mice, rats, and monkeys. Toxicol Pathol. 2014 Jan;42(1):260-74. [Content Brief]
[2]. Roses AD, et al. Stimulation of cholecystokinin-A receptors with Gl181771X: a failed clinical trial that did not test the pharmacogenetic hypothesis for reduction of food intake. Clin Pharmacol Ther. 2009 Apr;85(4):362-5. [Content Brief]
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)