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.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit : 99.96%
- CAS. Nr.: 313671-26-0
- Formel: C15H9Cl2N3O2S
- Molecular Weight:366.22
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
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Biologische Aktivität
Beschreibung
IC50 & Target
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μ Opioid Receptor/MOR |
In Vitro
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.
Chemical Information
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CAS. Nr. 313671-26-0
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Appearance Solid
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Molecular Weight 366.22
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Formel 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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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Lösungsmittel & Löslichkeit
In Vitro:
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)
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Reinheit & Dokumentation
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Data Sheet (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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Handling Instructions (2659 KB)
Verweise
[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
| 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 |
BMS-986121 Related Classifications
HY-141515 Related Classifications
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