VU0409106
Based on 1 Customer Validation
VU0409106 is a potent and selective mGlu5 negative allosteric modulator (NAM) with an IC50 of 24 nM. VU0409106 shows anxiolytic effects in rat models in a concentration-dependent manner. VU0409106 also penetrates the blood-brain barrier (BBB).
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
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: 99.76%
- CAS 番号: 1276617-62-9
- 分子式: C15H11FN4O2S
- 分子量:330.34
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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
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
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mGlu5 24 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
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| HEK293 | IC50 |
49 nM
Compound: 24, VU0409106
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Allosteric modulation of human mGlu5 receptor expressed in HEK cells assessed as effect on glutamate-induced calcium mobilization
Allosteric modulation of human mGlu5 receptor expressed in HEK cells assessed as effect on glutamate-induced calcium mobilization
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[PMID: 24074843] |
| HEK293-A | IC50 |
24 nM
Compound: 24, VU0409106
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Negative allosteric modulation of rat mGlu5 receptor expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilization preincubated for 140 seconds prior to glutamate-stimulation measured after 60 seconds
Negative allosteric modulation of rat mGlu5 receptor expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilization preincubated for 140 seconds prior to glutamate-stimulation measured after 60 seconds
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[PMID: 24074843] |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:CD-1 mice[1]
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Dosage:10 mg/kg (10% Tween 80 formulation)
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Administration:Intraperitoneal injection.
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Result:
1.19 Pharmacokinetic Parameters of VU0409106 in CD-1 mice[1].
IP (10 mg/kg) Plasma Tmax (h) 0.25 Plasma Cmax (ng/mL) 1450 Brain Tmax (h) 0.25 Brain Cmax (ng/mL) 1350 AUCplasma (ng/mL•h) 702 AUCbrain (ng/mL•h) 696 B/P ratio 0.99
化学情報
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CAS 番号 1276617-62-9
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性状 Solid
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分子量 330.34
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分子式 C15H11FN4O2S
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Color White to off-white
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SMILES
CC1=CSC(NC(C2=CC(F)=CC(OC3=CN=CN=C3)=C2)=O)=N1
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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 : 2 mg/mL (6.05 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. 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 (272 KB)
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SDS (251 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Felts AS, et al. Discovery of VU0409106: A negative allosteric modulator of mGlu5 with activity in a mouse model of anxiety. Bioorg Med Chem Lett. 2013 Nov 1;23(21):5779-85. [Content Brief]
[2]. Morrison RD, et al. The role of aldehyde oxidase and xanthine oxidase in the biotransformation of a novel negative allosteric modulator of metabotropic glutamate receptor subtype 5. Drug Metab Dispos. 2012 Sep;40(9):1834-45. [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 | 3.0272 mL | 15.1359 mL | 30.2718 mL | 75.6796 mL |
| 5 mM | 0.6054 mL | 3.0272 mL | 6.0544 mL | 15.1359 mL |
VU0409106 関連分類
HY-110180 関連分類
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