GV-196771A |
| رقم الكتالوجGC31019 |
GV-196771A هو شكل ملح الصوديوم GV196771 ، وهو مضاد لمستقبلات NMDA
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 166974-23-8
Sample solution is provided at 25 µL, 10mM.
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GV-196771A is the sodium salt form of GV196771, is an NMDA receptor antagonist.
GV196771 is a potent antagonist of the modulatory glycine site of the N-methyl-D-aspartate receptor. GV196771 is a potent antagonist of the modulatory glycine site of the NMDA receptor developed for treatment of neuropathic pain. GV196771 is an NMDA receptor antagonist with low oral bioavailability in rats and mice. GV196771 has low oral bioavailability (<10%) and plasma clearance (~2 mL/min/kg) in rats[1].
[1]. Polli JW, et al. The systemic exposure of an N-methyl-D-aspartate receptor antagonist is limited in mice by the P-glycoprotein and breast cancer resistance protein efflux transporters. Drug Metab Dispos. 2004 Jul;32(7):722-6.
Animal experiment: | Mice[1] Male wild-type FVB mdr1a/1b+/+ and Pgp-deficient knockout FVBmdr1a/1b-/- mice (20-30 g) are used. Dose solutions of 0.2 mg/mL for GV196771 and 5.0 mg/mL for GF120918 are prepared fresh using 0.5% hydroxypropylmethylcellulose and 1% Tween 80 as a vehicle. Two hours before the administration of GV196771, the animals are divided into two groups. One group receive a single oral dose (10 mL/kg) of vehicle and the second group receive a single 50 mg/kg oral dose (10 mL/kg) of GF120918. Two hours later, all animals receive a single 2 mg/kg oral dose (10 mL/kg) of GV196771. At scheduled time points, mice are anesthetized with CO2 and blood samples are obtained by cardiac puncture. Blood is centrifuged to yield plasma. The MDR genotype of each animal is confirmed by a polymerase chain reaction assay after study completion. |
References: [1]. Polli JW, et al. The systemic exposure of an N-methyl-D-aspartate receptor antagonist is limited in mice by the P-glycoprotein and breast cancer resistance protein efflux transporters. Drug Metab Dispos. 2004 Jul;32(7):722-6. | |
| Cas No. | 166974-23-8 | SDF | |
| Canonical SMILES | O=C(C(N1)=C(/C=C2C(N(C3=CC=CC=C3)CC/2)=O)C4=C1C=C(Cl)C=C4Cl)[O-].[Na+] | ||
| Formula | C20H13Cl2N2NaO3 | M.Wt | 423.22 |
| الذوبان | Soluble in DMSO | 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 | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.3628 mL | 11.8142 mL | 23.6284 mL |
| 5 mM | 0.4726 mL | 2.3628 mL | 4.7257 mL |
| 10 mM | 0.2363 mL | 1.1814 mL | 2.3628 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 38 reference(s) in Google Scholar.)
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