Istradefylline

製品コードS2790 バッチS279001

印刷

化学情報

Synonyms

KW-6002

Storage
(From the date of receipt)

3 years -20°C powder
1 years -80°C in solvent

化学式

C₂₀H₂₄N₄O₄

分子量

384.43

CAS No.

155270-99-8

Solubility (25°C)*

体外

DMSO

6 mg/mL (15.6 mM)

Water

Insoluble

Ethanol

Insoluble

体内（毎回新しく調製した物を用意してください）

	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O	0.3mg/ml
Suspension	30%propylene glycol 1 5%Tween80 2 65%D5W	30.0mg/ml	Taking the 1 mL working solution as an example, add 300 μL of 100 mg/ml clarified propylene glycol stock solution to 50 μL of Tween 80, mix evenly to clarify it; then continue to add 650 μL of D5W to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	Istradefylline (KW-6002) is a selective adenosine A2A receptor (A2AR) antagonist with K_i of 2.2 nM. Phase 3.
in vitro	The affinity of Istradefylline for the A2AR is 70-fold greater than that for the A1 receptor with K_i of 2.2 nM versus 150 nM. ^[1] Exposure of primary rat striatal astrocytes to Istradefylline results in concentration-dependent abolition of bFGF induction of astrogliosis in vitro. ^[5] Binding affinities (K_i) of Istradefylline for A1 receptor, A2A receptor, and A3 receptor in human are >287 nM, 9.12 nM, and >681 nM, respectively, for A1 receptor and A2A receptor in rat 50.9 nM and 1.57 nM, respectively, and for A1 receptor and A2A receptor in mouse 105.02 nM and 1.87 nM, respectively. ^[6]
in vivo	Istradefylline reverses CGS21680-induced and reserpine-induced catalepsy with ED50 of 0.05 mg/kg and 0.26 mg/kg, respectively. Istradefylline is over 10 times as potent in these models compared to other adenosine antagonists and dopamine agonist drugs. Administration of Istradefylline in combination with LevoDOPA (50 mg/kg) exerts prominent effects on haloperidol-induced and reserpine-induced catalepsy. ^[2] Oral administration of Istradefylline at 10 mg/kg to MPTP-treated common marmosets produces an increase in locomotor activity to approximately twice that of control and improves motor disability. Administration of Istradefylline (10 mg/kg, po, 90 minutes before SKF80723/quinpirole/LevoDOPA) in combination with SKF80723 (1 mg/kg, ip), quinpirole (0.06 mg/kg ip), or LevoDOPA (2.5 mg/kg po) produces a significant additive effect on locomotor activity and improvement of motor disability but not dyskinesia. ^[3] In the MPTP mice model, Istradefylline significantly attenuates striatal dopamine depletion under various conditions. Pretreatment with Istradefylline (3.3 mg/kg, i.p.) before a single dose of MPTP attenuates the partial dopamine and DOPAC depletions measured in striata 1 week later. ^[1] Oral administration of Istradefylline protects against the loss of nigral dopaminergic neuronal cells induced by 6-hydroxydopamine in rats, and prevents the functional loss of dopaminergic nerve terminals in the striatum and the ensuing gliosis caused by MPTP in mice. ^[4] Chronic Istradefylline treatment does not improve the reversal deficits in dopamine-depleted rats. ^[7] The tremulous jaw movements induced by pimozide are significantly reduced by co-administration of either Istradefylline or tropicamide. Pimozide-induced increases in ventrolateral striatal c-Fos expression are reduced by a behaviorally effective dose of Istradefylline, in contrast to tropicamide by which c-Fos expression in pimozide-treated rats is actually increased. ^[8]

プロトコル(参考用のみ)

動物実験	動物モデル	Common marmosets (Callithrix jacchus) with MPTP treatment
	投薬量	10 mg/kg
	投与方法	Oral gavage

参考

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カスタマーフィードバック

: , , Neurotox Res, 2015, 27(3):229-45.

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Transcriptional control of pancreatic cancer immunosuppression by metabolic enzyme CD73 in a tumor-autonomous and -autocrine manner [ Nat Commun, 2023, 14(1):3364]	PubMed: 37291128
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A2A Receptor Activation Attenuates Hypertensive Cardiac Remodeling via Promoting Brown Adipose Tissue-Derived FGF21. [ Cell Metab, 2018, 28(3):476-489]	PubMed: 30017353
The Role of Adenosine A1 and A2A Receptors in the Caffeine Effect on MDMA-Induced DA and 5-HT Release in the Mouse Striatum. [Gorska AM, et al. Neurotox Res, 2015, 27(3):229-45]

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。