Ifenprodil Tartrate

製品コードS4091 バッチS409104

印刷

化学情報

Synonyms

N/A

Storage
(From the date of receipt)

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

化学式

2(C₂₁H₂₇NO₂).C₄H₆O₆

分子量

800.98

CAS No.

23210-58-4

Solubility (25°C)*

体外

DMSO

100 mg/mL (124.84 mM)

Ethanol

100 mg/mL (124.84 mM)

Water

5 mg/mL (6.24 mM)

体内（毎回新しく調製した物を用意してください）

Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	5.000mg/ml (6.24mM)	Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	1.250mg/ml (1.56mM)	Taking the 1 mL working solution as an example, add 50 μL of 25 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. 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	Ifenprodil is an atypical noncompetitive antagonist at the NMDA receptor, it interacts with high affinity at a homogeneous population of NMDA receptors in neonatal rat forebrain with IC50 of 0.3 μM.
in vitro	Ifenprodil inhibits NMDA-induced currents at NR1A/NR2B and NR1A/NR2A receptors with IC50 of 0.34 μM and 146 μM in oocytes voltage-clamped at -70 mV. Ifenprodil may act as a weak open-channel blocker of NR1A/NR2A receptors, the degree of inhibition seen with 100 μM Ifenprodil at NR1A/NR2A receptors is not altered by changes in the concentration of extracellular glycine. The inhibitory effect of 1 mM Ifenprodil at NR1A/NR2B receptors is reduced by increasing the concentration of glycine. ^[1] Ifenprodil (10 μM) inhibits virtually all of the NMDA receptor-evoked current in very young rat cortical neurons that contain a single population of receptors exhibiting a high affinity for glycine. Ifenprodil (10 μM) inhibits both the high-affinity population and a significant proportion of the low-affinity component in older rat cortical neurons, thus revealing three pharmacologically distinct populations of NMDA receptors in single neurons. ^[2] Ifenprodil antagonizes NMDA receptors in an activity-dependent manner, whilst also increasing the receptor affinity for glutamate recognition-site agonists. Ifenprodil inhibition curves against 10 μM and 100 μM NMDA-evoked currents yielded IC50 values of 0.88 μM and 0.17 μM, respectively. Ifenprodil (3 μM) potentiates to approximately 200% of control levels in rat cultured cortical neurones. Ifenprodil exhibits a 39- and 50-fold higher affinity for the agonist-bound activated and desensitized states of the NMDA receptor, respectively, relative to the resting, agonist-unbound state. Ifenprodil binding to the NMDA receptor results in a 6-fold higher affinity for glutamate site agonists. ^[3]

製品説明

Ifenprodil is an atypical noncompetitive antagonist at the NMDA receptor, it interacts with high affinity at a homogeneous population of NMDA receptors in neonatal rat forebrain with IC50 of 0.3 μM.

in vitro

Ifenprodil inhibits NMDA-induced currents at NR1A/NR2B and NR1A/NR2A receptors with IC50 of 0.34 μM and 146 μM in oocytes voltage-clamped at -70 mV. Ifenprodil may act as a weak open-channel blocker of NR1A/NR2A receptors, the degree of inhibition seen with 100 μM Ifenprodil at NR1A/NR2A receptors is not altered by changes in the concentration of extracellular glycine. The inhibitory effect of 1 mM Ifenprodil at NR1A/NR2B receptors is reduced by increasing the concentration of glycine. ^[1] Ifenprodil (10 μM) inhibits virtually all of the NMDA receptor-evoked current in very young rat cortical neurons that contain a single population of receptors exhibiting a high affinity for glycine. Ifenprodil (10 μM) inhibits both the high-affinity population and a significant proportion of the low-affinity component in older rat cortical neurons, thus revealing three pharmacologically distinct populations of NMDA receptors in single neurons. ^[2] Ifenprodil antagonizes NMDA receptors in an activity-dependent manner, whilst also increasing the receptor affinity for glutamate recognition-site agonists. Ifenprodil inhibition curves against 10 μM and 100 μM NMDA-evoked currents yielded IC50 values of 0.88 μM and 0.17 μM, respectively. Ifenprodil (3 μM) potentiates to approximately 200% of control levels in rat cultured cortical neurones. Ifenprodil exhibits a 39- and 50-fold higher affinity for the agonist-bound activated and desensitized states of the NMDA receptor, respectively, relative to the resting, agonist-unbound state. Ifenprodil binding to the NMDA receptor results in a 6-fold higher affinity for glutamate site agonists. ^[3]

プロトコル(参考用のみ)

参考

https://pubmed.ncbi.nlm.nih.gov/7901753/
https://pubmed.ncbi.nlm.nih.gov/9482779/
https://pubmed.ncbi.nlm.nih.gov/9003561/

カスタマーフィードバック

: Data from [Data independently produced by , , Brain Res Bull, 2016, 127:56-65]

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：

Propafenone facilitates mitochondrial-associated ferroptosis and synergizes with immunotherapy in melanoma [ J Immunother Cancer, 2024, 12(11)e009805]	PubMed: 39581704
Therapeutic advantage of targeting lysosomal membrane integrity supported by lysophagy in malignant glioma [ Cancer Sci, 2022, 113(8):2716-2726]	PubMed: 35657693
A combinatorial CRISPR-Cas9 screen identifies ifenprodil as an adjunct to sorafenib for liver cancer treatment [ Cancer Res, 2021, canres.1017.2021]	PubMed: 34666996
Bivalves are NO different: nitric oxide as negative regulator of metamorphosis in the Pacific oyster, Crassostrea gigas [ BMC Dev Biol, 2020, 20(1):23]	PubMed: 33228520
Brain-derived neurotrophic factor (BDNF) in the rostral anterior cingulate cortex (rACC) contributes to neuropathic spontaneous pain-related aversion via NR2B receptors. [ Brain Res Bull, 2016, 127:56-65]	PubMed: 27575004

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。

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