BMS-986187
Based on 1 Customer Validation
BMS-986187 is an δ-opioid receptor-selective positive allosteric modulator (PAM) with an EC50 of 0.03 μM and a pKB of 6.02 (～1 μM). BMS-986187 has no observable PAM activity at the μ-receptor (EC50=3 μM).
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- Pureté: 99.66%
- CAS No.: 684238-37-7
- Formule: C31H34O4
- Masse moléculaire:470.60
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Stockage:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
Voir tous les produits spécifiques à Isoform Opioid Receptor
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Activité biologique
Description
IC50 & Target
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δ Opioid Receptor/DOR |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO | EC50 |
0.03 μM
Compound: 2, BMS-986187
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Positive allosteric modulation of human delta opioid receptor-1 expressed in CHO cells assessed as potentiation of leu-enkephalin-induced response after 90 mins by beta-arrestin recruitment assay
Positive allosteric modulation of human delta opioid receptor-1 expressed in CHO cells assessed as potentiation of leu-enkephalin-induced response after 90 mins by beta-arrestin recruitment assay
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[PMID: 25901762] |
| CHO | EC50 |
2.6 μM
Compound: 2, BMS-986187
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Positive allosteric modulation of human mu opioid receptor-1 expressed in CHO cells assessed as potentiation of endomorphin 1-induced response after 90 mins by beta-arrestin recruitment assay
Positive allosteric modulation of human mu opioid receptor-1 expressed in CHO cells assessed as potentiation of endomorphin 1-induced response after 90 mins by beta-arrestin recruitment assay
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[PMID: 25901762] |
In Vitro
BMS-986187 (1 nM-100 uM) produces little or no activity in agonist mode, but in PAM mode (in the presence of an EC20 of leu-enkephalin (in CHO-OPRD1 cells) or endomorphin 1 (in CHO-OPRM1 cells)) produces a response with an EC50 of 48 nM in CHO-OPRD1 cells and 2 μM in CHO-OPRM1 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 684238-37-7
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Appearance Solid
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Masse moléculaire 470.60
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Formule C31H34O4
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Color White to off-white
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SMILES
CC1=C(C=CC=C1)COC2=CC=C(C=C2)C3C4=C(OC(CC(C)(C5)C)=C3C5=O)CC(C)(C)CC4=O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Solvant et solubilité
In Vitro:
DMSO : 5 mg/mL (10.62 mM; ultrasonic and warming and heat to 60°C; 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 (protect from light). 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 (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Pureté et documentation
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Fiche technique (273 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instruction de manipulation (2659 KB)
Références
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 (protect from light). 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 | 2.1249 mL | 10.6247 mL | 21.2495 mL | 53.1237 mL |
| 5 mM | 0.4250 mL | 2.1249 mL | 4.2499 mL | 10.6247 mL | |
| 10 mM | 0.2125 mL | 1.0625 mL | 2.1249 mL | 5.3124 mL |
BMS-986187 Related Classifications
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