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Droxidopa (L-DOPS; SM5688) is a potent, orally active norepinephrine precursor. Droxidopa increases standing blood pressure, ameliorates symptoms of orthostatic hypotension and improves standing ability. Droxidopa has the potential for the research of neurogenic orthostatic hypotension (nOH) and alternative ADHD (attention deficit hyperactivity disorder).
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: 99.72%
- CAS 番号: 23651-95-8
- 分子式: C9H11NO5
- 分子量:213.19
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
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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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HepG2 | EC50 |
0.004 μM
Compound: Droxidopa
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Activation of human PXR expressed in human HepG2 (DPX-2) cells assessed as induction of CYP3A4 after 24 hrs by luminescent analysis
Activation of human PXR expressed in human HepG2 (DPX-2) cells assessed as induction of CYP3A4 after 24 hrs by luminescent analysis
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[PMID: 20966043] |
| HepG2 | EC50 |
63.1 μM
Compound: Droxidopa
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Activation of rat PXR expressed in human HepG2 cells after 24 hrs by luciferase reporter gene based luminescent analysis
Activation of rat PXR expressed in human HepG2 cells after 24 hrs by luciferase reporter gene based luminescent analysis
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[PMID: 20966043] |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:250-380g male Sprague-Dawley rats[2]
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Dosage:200 mg/kg (10 mg/kg, i.p. benserazide was given to the animals at 20 or 30 min prior to L-DOPS injection)
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Administration:I.p.
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Result:Significantly decreased hyperactivity of BZ-pretreated SHR/NCrl at 30 (P < 0.01) and 40 min (P < 0.05) post-injection, improved inattention-like behavior of SHR/NCrl, and ameliorated impulsive-like behavior of SHR/NCrl and Wistar rats.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 23651-95-8
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性状 Solid
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分子量 213.19
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分子式 C9H11NO5
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Color White to off-white
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SMILES
OC1=C(O)C=CC([C@@H](O)[C@@H](C(O)=O)N)=C1
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別名
Droxidopa; L-DOPS; DOPS; SM5688
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
溶剤 & 溶解度
DMSO : 21.74 mg/mL (101.97 mM; ultrasonic and warming and adjust pH to 3 with 1 M HCl and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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 (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Horacio Kaufmann, et al. Droxidopa for neurogenic orthostatic hypotension. Neurology, 2014; 83(4).
[2]. Dela Peña I, et al. Droxidopa alters dopamine neuron and prefrontal cortex activity and improves attention-deficit/hyperactivity disorder-like behaviors in rats. Eur J Pharmacol. 2021 Feb 5;892:173826. [Content Brief]
[3]. Cao LF, et al. Restoring Spinal Noradrenergic Inhibitory Tone Attenuates Pain Hypersensitivity in a Rat Model of Parkinson's Disease. Neural Plast. 2016;2016:6383240. [Content Brief]
[4]. Kaufmann H. L-dihydroxyphenylserine (Droxidopa): a new therapy for neurogenic orthostatic hypotension: the US experience. Clin Auton Res. 2008 Mar;18 Suppl 1:19-24. [Content Brief]
Complete Stock Solution Preparation Table
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 4.6907 mL | 23.4533 mL | 46.9065 mL | 117.2663 mL |
| 5 mM | 0.9381 mL | 4.6907 mL | 9.3813 mL | 23.4533 mL | |
| 10 mM | 0.4691 mL | 2.3453 mL | 4.6907 mL | 11.7266 mL | |
| 15 mM | 0.3127 mL | 1.5636 mL | 3.1271 mL | 7.8178 mL | |
| 20 mM | 0.2345 mL | 1.1727 mL | 2.3453 mL | 5.8633 mL | |
| 25 mM | 0.1876 mL | 0.9381 mL | 1.8763 mL | 4.6907 mL | |
| 30 mM | 0.1564 mL | 0.7818 mL | 1.5636 mL | 3.9089 mL | |
| 40 mM | 0.1173 mL | 0.5863 mL | 1.1727 mL | 2.9317 mL | |
| 50 mM | 0.0938 mL | 0.4691 mL | 0.9381 mL | 2.3453 mL | |
| 60 mM | 0.0782 mL | 0.3909 mL | 0.7818 mL | 1.9544 mL | |
| 80 mM | 0.0586 mL | 0.2932 mL | 0.5863 mL | 1.4658 mL | |
| 100 mM | 0.0469 mL | 0.2345 mL | 0.4691 mL | 1.1727 mL |
Droxidopa 関連分類
HY-13458 関連分類
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