Dipraglurant
Based on 1 Customer Validation
Dipraglurant (ADX48621) is a potent, selective, orally active and brain penetrant mGluR5 negative allosteric modulator (NAM), with an IC50 of 21 nM. Dipraglurant can reduce Levodopa-induced dyskinesia (LID) in vivo. Dipraglurant is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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: 99.97%
- CAS 番号: 872363-17-2
- 分子式: C16H12FN3
- 分子量:265.29
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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
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Help & FAQs
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生物活性
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mGluR5 21 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
20 nM
Compound: Dipraglurant, ADX48621 series
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Negative allosteric modulation of human mGluR5 expressed in HEK293 cells assessed as calcium mobilization by FLIPR assay
Negative allosteric modulation of human mGluR5 expressed in HEK293 cells assessed as calcium mobilization by FLIPR assay
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[PMID: 23434029] |
Dipraglurant (1-10 μM; 15 min) counteracts the abnormal membrane responses and calcium rise induced either by the D2R agonist quinpirole or by caged dopamine (NPEC-Dopamine)[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Dipraglurant exhibits Cmax (1.040, 1.380, 5.310 ng/mL) Tmax (1.0, 0.5, 1.0 h) and AUCinf (2.230, 2.860, 15.700) following p.o. administration (3, 10, 30 mg/kg) in macaque[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 872363-17-2
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性状 Solid
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分子量 265.29
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分子式 C16H12FN3
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Color White to off-white
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SMILES
FC1=CN2C(C=C1)=NC(CCC#CC3=NC=CC=C3)=C2
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別名
ADX48621
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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 2 years -20°C 1 year
溶剤 & 溶解度
DMSO : ≥ 40 mg/mL (150.78 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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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取扱説明書 (2659 KB)
参考文献
[2]. Bezard E, et, al. The mGluR5 negative allosteric modulator dipraglurant reduces dyskinesia in the MPTP macaque model. Mov Disord. 2014 Jul;29(8):1074-9. [Content Brief]
[3]. Sciamanna G, et, al. Negative allosteric modulation of mGlu5 receptor rescues striatal D2 dopamine receptor dysfunction in rodent models of DYT1 dystonia. Neuropharmacology. 2014 Oct;85:440-50. [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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.7695 mL | 18.8473 mL | 37.6946 mL | 94.2365 mL |
| 5 mM | 0.7539 mL | 3.7695 mL | 7.5389 mL | 18.8473 mL | |
| 10 mM | 0.3769 mL | 1.8847 mL | 3.7695 mL | 9.4236 mL | |
| 15 mM | 0.2513 mL | 1.2565 mL | 2.5130 mL | 6.2824 mL | |
| 20 mM | 0.1885 mL | 0.9424 mL | 1.8847 mL | 4.7118 mL | |
| 25 mM | 0.1508 mL | 0.7539 mL | 1.5078 mL | 3.7695 mL | |
| 30 mM | 0.1256 mL | 0.6282 mL | 1.2565 mL | 3.1412 mL | |
| 40 mM | 0.0942 mL | 0.4712 mL | 0.9424 mL | 2.3559 mL | |
| 50 mM | 0.0754 mL | 0.3769 mL | 0.7539 mL | 1.8847 mL | |
| 60 mM | 0.0628 mL | 0.3141 mL | 0.6282 mL | 1.5706 mL | |
| 80 mM | 0.0471 mL | 0.2356 mL | 0.4712 mL | 1.1780 mL | |
| 100 mM | 0.0377 mL | 0.1885 mL | 0.3769 mL | 0.9424 mL |
Dipraglurant 関連分類
HY-14859 関連分類
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