Lasmiditan (Synonyms: COL-144, LY573144) |
| Catalog No.GC15121 |
5-HT1F receptor agonist
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 439239-90-4
Sample solution is provided at 25 µL, 10mM.
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Lasmiditan is a selective agonist of 5-HT1F receptor with Ki value of 2.21nM [1].
Lasmiditan shows great selectivity against 5-HT1F over other human recombinant 5-HT receptor subtypes as well as other members of 5-HT1 family. The Ki values for 5-HT2A-2C, 5-HT6 and 5-HT7 are all above 2μM. In the in vitro functional assay, lasmiditan shows high functional selectivity for 5-HT1F with EC50 value of 43.1nM. Moreover, oral administration of lasmiditan potently decreases the dural plasma protein extravasation with ID50 value of 2×104μg/kg in the migraine models. It also inhibits trigeminal stimulation-induced c-fos expression in the nucleus caudalis. Furthermore, lasmiditan is proved to be an effective treatment in acute migraine after the phase II trials. And the oral administration is found to be better than the intravenous administration [1, 2]
References:
[1] Nelson D L, Phebus L A, Johnson K W, et al. Preclinical pharmacological profile of the selective 5-HT1F receptor agonist lasmiditan. Cephalalgia, 2010, 30(10): 1159-1169.
[2] Tfelt-Hansen P C, Olesen J. The 5-HT1F receptor agonist lasmiditan as a potential treatment of migraine attacks: a review of two placebo-controlled phase II trials. The journal of headache and pain, 2012, 13(4): 271-275.
| Cas No. | 439239-90-4 | SDF | |
| Synonymes | COL-144, LY573144 | ||
| Chemical Name | 2,4,6-trifluoro-N-[6-(1-methylpiperidine-4-carbonyl)pyridin-2-yl]benzamide | ||
| Canonical SMILES | CN1CCC(CC1)C(=O)C2=NC(=CC=C2)NC(=O)C3=C(C=C(C=C3F)F)F | ||
| Formula | C19H18F3N3O2 | M.Wt | 377.36 |
| Solubility | DMF: 25 mg/ml,DMSO: 25 mg/ml,Ethanol: 30 mg/ml,Ethanol:PBS (pH 7.2) (1:20): 0.04 mg/ml | 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 | 2.65 mL | 13.2499 mL | 26.4999 mL |
| 5 mM | 0.53 mL | 2.65 mL | 5.3 mL |
| 10 mM | 0.265 mL | 1.325 mL | 2.65 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
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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 19 reference(s) in Google Scholar.)
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