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.
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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: 99.13%
- CAS 番号: 2414674-71-6
- 分子式: C11H14Cl2N2O
- 分子量:261.15
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保管条件:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
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生物活性
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 |
化学情報
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CAS 番号 2414674-71-6
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性状 Solid
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分子量 261.15
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分子式 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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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
溶剤 & 溶解度
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.
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 (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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取扱説明書 (2659 KB)
参考文献
[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 関連分類
HY-136146 関連分類
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