Carabersat |
| カタログ番号GC31308 |
Carabersat は強力な抗けいれん薬です。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 184653-84-7
Sample solution is provided at 25 µL, 10mM.
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Carabersat is a potent anticonvulsant agent.
[3H]Carabersat ([3H]SB 204269) binds to rat forebrain membranes with moderate affinity (Kd 40 nM) and pKi values of 7.3[1]. Carabersat is able to bind to mouse forebrain membranes, and the binding is saturable and stereospecific, with a Kd of 53 nM. The labelled [3H]Carabersat produces a Kd of 32 nM[2]. Carabersat (SB-204269, 1-100 μM) has no effect on Na+ current in cultured hippocampal neurones. Carabersat also shows no effect on action potential discharges evoked by elevating external K+[3]. Carabersat (SB-204269) is structurally-related to the benzopyran ATP-sensitive potassium channel (KATP) opener, cromakalim, but has opposite stereochemistry, and the mechanism of action of Carabersat is not thought to involve KATP[4].
Carabersat (5b) significantly elevates anticonvulsant activity in mice[1].
[1]. Wai N. Chan, et al. Synthesis of Novel trans-4-(Substituted-benzamido)-3,4-dihydro-2H-benzo[b]pyran-3-ol Derivatives as Potential Anticonvulsant Agents with a Distinctive Binding Profile. J. Med. Chem., 1996, 39 (23), pp 4537-4539. [2]. Herdon H, et al. The novel anticonvulsant SB 204269 binds to a stereospecific site in the mouse brain. Eur J Pharmacol. 1996 Oct 31;314(3):R7-8. [3]. Caeser M, et al. Lack of effect of the novel anticonvulsant SB-204269 on voltage-dependent currents in neurones cultured from rat hippocampus. Neurosci Lett. 1999 Aug 13;271(1):57-60. [4]. Crespi F, et al. SB-204269 SmithKline Beecham. IDrugs. 1998 Sep;1(5):595-8.
Animal experiment: | Mice[1]In this model, groups of 10-20 naive mice (25-30 g) are assessed for production of a tonic hindlimb extension seizure following a single corneal electroshock using an "up and down" method of shock titration. The effects of drug treatment are expressed as a percentage change from vehicle control values and statistical comparisons between groups are made. Carabersat is administered orally as a fine suspension in 1% methylcellulose one hour before electroshock application[1]. |
References: [1]. Wai N. Chan, et al. Synthesis of Novel trans-4-(Substituted-benzamido)-3,4-dihydro-2H-benzo[b]pyran-3-ol Derivatives as Potential Anticonvulsant Agents with a Distinctive Binding Profile. J. Med. Chem., 1996, 39 (23), pp 4537-4539. | |
| Cas No. | 184653-84-7 | SDF | |
| Canonical SMILES | O=C(N[C@@H]1[C@@H](O)C(C)(C)OC2=CC=C(C(C)=O)C=C12)C3=CC=C(F)C=C3 | ||
| Formula | C20H20FNO4 | M.Wt | 357.38 |
| 溶解度 | 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. |
||
| 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 | 2.7981 mL | 13.9907 mL | 27.9814 mL |
| 5 mM | 559.6 μL | 2.7981 mL | 5.5963 mL |
| 10 mM | 279.8 μL | 1.3991 mL | 2.7981 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
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 5 reference(s) in Google Scholar.)
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