UPF-523
Based on 1 Customer Validation
UPF-523 (AIDA), a rigid (carboxyphenyl) glycine derivative, is a relatively potent and selective antagonist of group I metabotropic glutamate receptors (mGlu1a) with an IC50 of 214 μM. But UPF-523 has no effect on group II (mGlu2), group III (mGlu4) receptors or ionotropic glutamate receptors. UPF-523 has the potential for the research of the acute arthritis.
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: 99.89%
- CAS 番号: 168560-79-0
- 分子式: C11H11NO4
- 分子量:221.21
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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
生物活性
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mGluR1a 214 μM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Huh-7 | CC50 |
>10 μM
Compound: GNF-Pf-1401
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NOVARTIS: Cytotoxicity against human hepatocellular carcinoma cell line (Huh7)
NOVARTIS: Cytotoxicity against human hepatocellular carcinoma cell line (Huh7)
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[PMID: 18579783] |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Naive male hooded Lister rats (320–350 g)[1]
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Dosage:0.18 mg/kg
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Administration:I.p.; 0.5 ml per 100 g
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Result:Showed no gross motor abnormalities and normal righting reflexes.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 168560-79-0
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性状 Solid
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分子量 221.21
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分子式 C11H11NO4
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Color White to off-white
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SMILES
O=C(C1(N)CCC2=C1C=CC(C(O)=O)=C2)O
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別名
AIDA
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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
H2O : 16.67 mg/mL (75.36 mM; ultrasonic and adjust pH to 10 with NaOH)
DMSO : 9.52 mg/mL (43.04 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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 (274 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]. Nielsen KS, et al. Class I mGlu receptor antagonist 1-aminoindan-1,5-dicarboxylic acid blocks contextual but not cue conditioning in rats. Eur J Pharmacol. 1997;326(2-3):105-108. [Content Brief]
[2]. Zhang LP, et al. The Role of Type 1 Metabotropic Glutamate Receptors in the Generation of Dorsal Root Reflexes Induced by Acute Arthritis or the Spinal Infusion of 4-Aminopyridine in the Anesthetized Rat. J Pain. 2000;1(2):151-161. [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 / H2O | 1 mM | 4.5206 mL | 22.6030 mL | 45.2059 mL | 113.0148 mL |
| 5 mM | 0.9041 mL | 4.5206 mL | 9.0412 mL | 22.6030 mL | |
| 10 mM | 0.4521 mL | 2.2603 mL | 4.5206 mL | 11.3015 mL | |
| 15 mM | 0.3014 mL | 1.5069 mL | 3.0137 mL | 7.5343 mL | |
| 20 mM | 0.2260 mL | 1.1301 mL | 2.2603 mL | 5.6507 mL | |
| 25 mM | 0.1808 mL | 0.9041 mL | 1.8082 mL | 4.5206 mL | |
| 30 mM | 0.1507 mL | 0.7534 mL | 1.5069 mL | 3.7672 mL | |
| 40 mM | 0.1130 mL | 0.5651 mL | 1.1301 mL | 2.8254 mL | |
| H2O | 50 mM | 0.0904 mL | 0.4521 mL | 0.9041 mL | 2.2603 mL |
| 60 mM | 0.0753 mL | 0.3767 mL | 0.7534 mL | 1.8836 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.