SUVN-911
Based on 1 Customer Validation
SUVN-911 is a potent, selective, brain penetrated and orally bioavailable neuronal nicotinic acetylcholine α4β2 receptor antagonist, with a Ki of 1.5 nM. SUVN-911 has antidepressant activity.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 99.13%
- CAS. Nr.: 2414674-71-6
- Formel: C11H14Cl2N2O
- Molecular Weight:261.15
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Speicherung:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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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
Ki: 1.5 nM (α4β2 receptor)[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
>10 μM
Compound: 9h; SUVN-911
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Inhibition of recombinant human ERG expressed in HEK293 at -80 mV holding potential by whole-cell patch clamp method
Inhibition of recombinant human ERG expressed in HEK293 at -80 mV holding potential by whole-cell patch clamp method
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[PMID: 32026697] |
| HEK293 | IC50 |
7.31 μM
Compound: 9h; SUVN-911
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Antagonist activity at alpha4beta2 nAChR (unknown origin) expressed in HEK293 cells assessed as reduction in acetylcholine-induced currents at -80 mV holding potential by whole-cell patch clamp method
Antagonist activity at alpha4beta2 nAChR (unknown origin) expressed in HEK293 cells assessed as reduction in acetylcholine-induced currents at -80 mV holding potential by whole-cell patch clamp method
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[PMID: 32026697] |
SUVN-911 displays high selectivity for α4β2 over α3β4 nAChR[1].
SUVN-911 shows good selectivity against over 70 receptors which includes GPCRs, ion channels, enzymes, peptides, steroids, second messengers, growth factors and prostaglandins[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
SUVN-911 (1.0-10.0 mg/kg; p.o.; daily; for 3 days) shows significant antidepressant effects[1].
SUVN-911 shows metabolic stability in rats[1].
SUVN-911 (3 mg/kg; p.o.) has shown high oral exposures, longer half-lives and adequate brain penetration in Wistar rats[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male Wistar rats (180-230 g)[1]
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Dosage:1 mg/kg, 3 mg/kg, 10.0 mg/kg
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Administration:Oral administration, daily, for 3 days
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Result:Showed antidepressant like activity with no signs of tachyphylaxis.
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Animal Model:Male Wistar rats (225 ± 25 g)[1]
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Dosage:3 mg/kg (Pharmacokinetic Analysis)
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Administration:Oral administration
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Result:AUC=3507 ng*h/mL, T1/2=3.34 hours.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS. Nr. 2414674-71-6
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Appearance Solid
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Molecular Weight 261.15
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Formel C11H14Cl2N2O
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Color Off-white to light yellow
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SMILES
ClC1=NC=C(OC[C@H]2N[C@@H]3C[C@@H]3C2)C=C1.[H]Cl
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Lösungsmittel & Löslichkeit
DMSO : 125 mg/mL (478.65 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 (sealed storage, away from moisture). 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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Reinheit & Dokumentation
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Data Sheet (272 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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Handling Instructions (2659 KB)
Verweise
[1]. Ramakrishna Nirogi, et al. Discovery and Development of 3-(6-Chloropyridine-3-yloxymethyl)-2-azabicyclo[3.1.0]hexane Hydrochloride (SUVN-911): A Novel, Potent, Selective, and Orally Active Neuronal Nicotinic Acetylcholine α4β2 Receptor Antagonist for the Treatment of Depression. J Med Chem. 2020 Mar 26;63(6):2833-2853. [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 (sealed storage, away from moisture). 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 | 3.8292 mL | 19.1461 mL | 38.2922 mL | 95.7304 mL |
| 5 mM | 0.7658 mL | 3.8292 mL | 7.6584 mL | 19.1461 mL | |
| 10 mM | 0.3829 mL | 1.9146 mL | 3.8292 mL | 9.5730 mL | |
| 15 mM | 0.2553 mL | 1.2764 mL | 2.5528 mL | 6.3820 mL | |
| 20 mM | 0.1915 mL | 0.9573 mL | 1.9146 mL | 4.7865 mL | |
| 25 mM | 0.1532 mL | 0.7658 mL | 1.5317 mL | 3.8292 mL | |
| 30 mM | 0.1276 mL | 0.6382 mL | 1.2764 mL | 3.1910 mL | |
| 40 mM | 0.0957 mL | 0.4787 mL | 0.9573 mL | 2.3933 mL | |
| 50 mM | 0.0766 mL | 0.3829 mL | 0.7658 mL | 1.9146 mL | |
| 60 mM | 0.0638 mL | 0.3191 mL | 0.6382 mL | 1.5955 mL | |
| 80 mM | 0.0479 mL | 0.2393 mL | 0.4787 mL | 1.1966 mL | |
| 100 mM | 0.0383 mL | 0.1915 mL | 0.3829 mL | 0.9573 mL |
SUVN-911 Related Classifications
HY-136146 Related Classifications
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