ZK 200775 (Synonyms: ZK200775; MPQX) |
| رقم الكتالوجGC16300 |
ZK 200775 (ZK200775) هو مضاد AMPA / kainate انتقائي للغاية مع نشاط ضئيل ضد NMDA ؛ لها قيم Ki 3.2 نانومتر و 100 نانومتر و 8.5 μ ؛ M مقابل quisqualate و kainate و NMDA ، على التوالي.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 161605-73-8
Sample solution is provided at 25 µL, 10mM.
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Fanapanel (ZK200775) is a highly selective AMPA/kainate antagonist with little activity against NMDA; have Ki values of 3.2 nM, 100 nM, and 8.5 μM against quisqualate, kainate, and NMDA, respectively.
In the cortical slice preparation assay, ZK200775 gave Ki values of 3.2 nM, 100 nM, and 8.5 μM against quisqualate, kainate, and NMDA, respectively. In the spreading depression assay, it gave IC50 values of 200 nM, 76 nM, 13 μM, and 18 μM against quisqualate, kainate, NMDA, and glycine [1].
ZK200775 elevated the threshold for AMPA- and kainate-induced clonic seizures in mice with a THRD50 (threshold dose) of 2.9 (1.7–4.6) and 1.6 (1.3–2.0) mg/kg i.v., whereas the threshold for NMDA-induced seizures was elevated only in doses, THRD50 of 24.1 (21.9–26.5) mg/kg i.v., which affected motor coordination in the rotating rod, ED50 14.6 (12.1–17.6) mg/kg. ZK200775 in doses of 10 and 30 mg/kg i.v. reduced muscle tone in genetically spastic rats [1]. ZK200775 (3.0 but not 1.5 or 6.0 mg/kg) significantly decreased the nicotine-induced (0.6 mg/kg) DA release in the NAcc and nicotine-stimulated LMA. ZK200775 (1.5, 3.0, 6.0 mg/kg) alone influenced neither DA release nor LMA. ZK200775 showed 34-fold selectivity for AMPA receptors compared to NMDA receptors and no affinity to nicotine receptors
References:
[1]. Turski L, et al. ZK200775: a phosphonate quinoxalinedione AMPA antagonist for neuroprotection in stroke and trauma. Proc Natl Acad Sci U S A. 1998 Sep 1;95(18):10960-5.
[2]. Kosowski AR, et al. Nicotine-induced dopamine release in the nucleus accumbens is inhibited by the novel AMPA antagonist ZK200775 and the NMDA antagonist CGP39551. Psychopharmacology (Berl). 2004 Aug;175(1):114-23.
| Cas No. | 161605-73-8 | SDF | |
| المرادفات | ZK200775; MPQX | ||
| Chemical Name | ((7-morpholino-2,3-dioxo-6-(trifluoromethyl)-3,4-dihydroquinoxalin-1(2H)-yl)methyl)phosphonic acid | ||
| Canonical SMILES | FC(F)(C(C(N1CCOCC1)=C2)=CC(NC3=O)=C2N(C3=O)CP(O)(O)=O)F | ||
| Formula | C14H15N3O6F3P | M.Wt | 409.25 |
| الذوبان | DMSO : 1.25 mg/mL (3.05 mM; Need ultrasonic) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.4435 mL | 12.2175 mL | 24.4349 mL |
| 5 mM | 0.4887 mL | 2.4435 mL | 4.887 mL |
| 10 mM | 0.2443 mL | 1.2217 mL | 2.4435 mL |
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Quality Control & SDS
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- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
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Average Rating: 5 (Based on Reviews and 9 reference(s) in Google Scholar.)
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