| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
CP-465022 (0.0001 μM-10 μM) suppresses kainic acid-induced reactions somewhat slowly and in a concentration-dependent manner; the compound's estimated IC50 is 25 nM, and at 3.2 μM, it almost completely blocks the response [1]. CP-465022 While 1 µM for 10 minutes lowered the current measured after 8 seconds of NMDA application by 26%, it had little influence on NMDA-induced peak currents. In primary cultures of cortical and cerebellar granule neurons, CP-465,022 at 10 µM reduces NMDA-induced peak currents in cortical neurons by 36%, as evaluated at 8 seconds times 70% d [1]. In cultured rat cerebellar granule neurons, CP-465022 1 µM suppressed peak NMDA currents for 10 minutes at an average inhibition rate of 19%. At 8 seconds, the NMDA current inhibition rate was measured and found to be 45%, in agreement with cortical neurons. A comparable circumstance was noted [1]. (100 nM -10 µM) CP-465022 inhibits whole-cell currents produced by kainate in the voltage-clamped rat hippocampal, at 100 nM Kainate currents produced in 200 seconds, 500 nM, and 1 µM are inhibited by CP465,022. This time span was nearly entirely inhibited (99.3%) by CP-465,022[1].
|
|---|---|
| References |
| Molecular Formula |
C30H28CLFN4O5
|
|---|---|
| Molecular Weight |
579.018529891968
|
| Exact Mass |
578.173
|
| CAS # |
199656-46-7
|
| Related CAS # |
CP-465022;199655-36-2;CP-465022 hydrochloride;1785666-59-2
|
| PubChem CID |
70340453
|
| Appearance |
Typically exists as solid at room temperature
|
| Hydrogen Bond Donor Count |
2
|
| Hydrogen Bond Acceptor Count |
9
|
| Rotatable Bond Count |
9
|
| Heavy Atom Count |
41
|
| Complexity |
846
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
C(/C(=O)O)=C/C(=O)O.C(C1=NC2=CC=C(F)C=C2C(=O)N1C1C=CC=CC=1Cl)=CC1=CC=CC(CN(CC)CC)=N1
|
| InChi Key |
WLLUWLRVXIHECY-KSUUAYPFSA-N
|
| InChi Code |
InChI=1S/C26H24ClFN4O.C4H4O4/c1-3-31(4-2)17-20-9-7-8-19(29-20)13-15-25-30-23-14-12-18(28)16-21(23)26(33)32(25)24-11-6-5-10-22(24)27;5-3(6)1-2-4(7)8/h5-16H,3-4,17H2,1-2H3;1-2H,(H,5,6)(H,7,8)/b15-13+;2-1-
|
| Chemical Name |
(Z)-but-2-enedioic acid;3-(2-chlorophenyl)-2-[(E)-2-[6-(diethylaminomethyl)pyridin-2-yl]ethenyl]-6-fluoroquinazolin-4-one
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
|
|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.7271 mL | 8.6353 mL | 17.2706 mL | |
| 5 mM | 0.3454 mL | 1.7271 mL | 3.4541 mL | |
| 10 mM | 0.1727 mL | 0.8635 mL | 1.7271 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
