MRS 1477
MRS 1477, a dihydropyridine derivative, is a positive allosteric modulator of TRPV1 in the presence of capsaicin. MRS 1477 itself does not induce apoptosis, but the co-existence of MRS 1477 and capsaicin can induce apoptosis.
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- CAS 番号: 212200-21-0
- 分子式: C21H27NO4S
- 分子量:389.51
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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
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| BT-474 | IC50 |
10.6 μM
Compound: 7; MRS1477
|
Antiproliferative activity against human BT-474 cells assessed as inhibition of cell growth by MTT assay
Antiproliferative activity against human BT-474 cells assessed as inhibition of cell growth by MTT assay
|
[PMID: 37000154] |
| MCF7 | IC50 |
3 μM
Compound: 7; MRS1477
|
Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth by MTT assay
Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth by MTT assay
|
[PMID: 37000154] |
| MDA-MB-231 | IC50 |
40.8 μM
Compound: 7; MRS1477
|
Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth by MTT assay
Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth by MTT assay
|
[PMID: 37000154] |
| NIH3T3 | EC50 |
21.3 μM
Compound: 23, MRS-1477
|
Agonist-enhancing activity in epsilon-epitope tagged TRPV1 receptor expressed in mouse NIH3T3 cells assessed as capsaicin-induced 45Ca2+ influx by microplate liquid scintillation counter
Agonist-enhancing activity in epsilon-epitope tagged TRPV1 receptor expressed in mouse NIH3T3 cells assessed as capsaicin-induced 45Ca2+ influx by microplate liquid scintillation counter
|
[PMID: 18809334] |
MRS1477 evokes Ca2+ signals in MCF7 breast cancer cells, but not in primary breast epithelial cells[1].
MRS1477 (2 μM; 72 h) with capsaicine (10 μM) induces apoptosis and increases reactive oxygen species production and caspase activity[1].
MRS1477 (2 μM) increases capsaicin-evoked TRPV1-mediated current density levels[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
化学情報
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CAS 番号 212200-21-0
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分子量 389.51
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分子式 C21H27NO4S
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SMILES
CCOC(C1=C(C2=CC=CC=C2)NC(C)=C(C(SCCOC)=O)C1CC)=O
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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
[1]. Nazıroğlu M, et, al. Targeting breast cancer cells by MRS1477, a positive allosteric modulator of TRPV1 channels. PLoS One. 2017 Jun 22;12(6):e0179950. [Content Brief]
[2]. Kaszas K, et, al. Small molecule positive allosteric modulation of TRPV1 activation by vanilloids and acidic pH. J Pharmacol Exp Ther. 2012 Jan;340(1):152-60. [Content Brief]
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)