BMS-986121
Based on 1 Customer Validation
BMS-986121 is a positive allosteric modulator (PAM) of the μ opioid receptor extracted from patent WO2014107344. BMS-986121 is built on a chemical scaffold representing a new chemotype for μ receptor PAMs.
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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。
- 純度: 99.96%
- CAS 番号: 313671-26-0
- 分子式: C15H9Cl2N3O2S
- 分子量:366.22
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
Opioid Receptor アイソフォーム固有の製品をすべて表示
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生物活性
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μ Opioid Receptor/MOR |
BMS-986121 (1 μM~1 mM) significantly augments the β-arrestin–recruitment response produced by a low concentration of endomorphin-I (PAM-detection mode). BMS-986121 significantly increases the inhibition of forskolin-stimulated adenylyl cyclase activity produced by a ∼EC10 (30 pM) concentration of endomorphin-I in CHOμ cells. BMS-986121 (100 μM) produces leftward shifts in the potency of endomorphin-I (fourfold) and leu-enkephalin (sixfold), in inhibition of forskolin-stimulated cAMP-accumulation assays in CHO-μ cells[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 313671-26-0
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性状 Solid
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分子量 366.22
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分子式 C15H9Cl2N3O2S
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Color Light yellow to yellow
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SMILES
O=[N+](C1=CC=C(C2=CSC(NC3=C(Cl)C=CC=C3Cl)=N2)C=C1)[O-]
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
溶剤 & 溶解度
DMSO : 100 mg/mL (273.06 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
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データシート (274 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Burford NT, et al. Discovery of positive allosteric modulators and silent allosteric modulators of the μ-opioid receptor. Proc Natl Acad Sci U S A. 2013;110(26):10830-10835. [Content Brief]
[2]. WO2014107344
[3]. Bisignano P, et al. Ligand-Based Discovery of a New Scaffold for Allosteric Modulation of the μ-Opioid Receptor. J Chem Inf Model. 2015;55(9):1836-1843. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.7306 mL | 13.6530 mL | 27.3060 mL | 68.2650 mL |
| 5 mM | 0.5461 mL | 2.7306 mL | 5.4612 mL | 13.6530 mL | |
| 10 mM | 0.2731 mL | 1.3653 mL | 2.7306 mL | 6.8265 mL | |
| 15 mM | 0.1820 mL | 0.9102 mL | 1.8204 mL | 4.5510 mL | |
| 20 mM | 0.1365 mL | 0.6826 mL | 1.3653 mL | 3.4132 mL | |
| 25 mM | 0.1092 mL | 0.5461 mL | 1.0922 mL | 2.7306 mL | |
| 30 mM | 0.0910 mL | 0.4551 mL | 0.9102 mL | 2.2755 mL | |
| 40 mM | 0.0683 mL | 0.3413 mL | 0.6826 mL | 1.7066 mL | |
| 50 mM | 0.0546 mL | 0.2731 mL | 0.5461 mL | 1.3653 mL | |
| 60 mM | 0.0455 mL | 0.2275 mL | 0.4551 mL | 1.1377 mL | |
| 80 mM | 0.0341 mL | 0.1707 mL | 0.3413 mL | 0.8533 mL | |
| 100 mM | 0.0273 mL | 0.1365 mL | 0.2731 mL | 0.6826 mL |