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Technical Data
| Formula | 2(C21H27NO2).C4H6O6 |
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| Molecular Weight | 800.98 | CAS No. | 23210-58-4 | |
| Solubility (25°C)* | In vitro | DMSO | 100 mg/mL (124.84 mM) | |
| Ethanol | 100 mg/mL (124.84 mM) | |||
| Water | 5 mg/mL (6.24 mM) | |||
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* <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. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.) |
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Preparing Stock Solutions
Biological Activity
| Description | 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. | ||
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| 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] |
Protocol (from reference)
References
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Customer Product Validation
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Data from [Data independently produced by , , Brain Res Bull, 2016, 127:56-65]
Selleck's Ifenprodil Tartrate has been cited by 4 publications
| 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 |
RETURN POLICY
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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.
NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.