LY 344864 (Synonyms: LY344864;LY-344864) |
| Catalog No.GC17039 |
A 5-HT1F receptor antagonist
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 186544-26-3
Sample solution is provided at 25 µL, 10mM.
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IC50 Value: 6 nM（Ki） LY344864 is a selective receptor agonist with an affinity of 6 nM (Ki) at the recently cloned 5-HT1F receptor. It possesses little affinity for the 56 other serotonergic and non-serotonergic neuronal binding sites examined [1]. in vitro: he 5-HT1A, 5-HT1B and 5-HT1D receptor agonists 8-OH-DPAT (3 microM), CP93129 (3 microM) and L694247 (3 microM), but not the 5-HT1F receptor agonist LY344864 (1 - 3 microM) inhibited evoked IPSCs [2]. in vivo: After an intravenous dose of 1 mg/kg, rat plasma LY344864 levels declined with time whereas brain cortex levels remained relatively constant for the first 6 hours after injection. Oral and intravenous LY344864 administration potently inhibited dural protein extravasation caused by electrical stimulation of the trigeminal ganglion in rats [1]. Sumatriptan, zolmitriptan, rizatriptan, and naratriptan all contracted the rabbit saphenous vein from baseline tone, whereas LY344864 in concentrations up to 10(-4) M did not contract the rabbit saphenous vein. Furthermore, vascular contractions to sumatriptan were markedly augmented in the presence of prostaglandin F(2alpha) (PGF(2alpha)). However, even in the presence of PGF(2alpha) (3 x 10(-7) M), LY344864 did not contract the rabbit saphenous vein in concentrations well in excess of its 5-HT(1F) receptor affinity (pK(i) = 8.2) [3]. Clinical trial: N/A
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Animal experiment: |
Rats[2]Male albino Wistar rats are divided into different groups. Rats in the experimental LY344864 and sham groups receive LY 344864 (1 or 2 μg/5 μL; intracerebroventricular [i.c.v.]), vehicle (5 μl/rat i.c.v.), or saline (5 μl/rat i.c.v.) during the acquisition phase[2] |
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References: [1]. Phebus LA, et al. Characterization of LY344864 as a pharmacological tool to study 5-HT1F receptors: binding affinities, brain penetration and activity in the neurogenic dural inflammation model of migraine. Life Sci. 1997;61(21):2117-26. |
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| Cas No. | 186544-26-3 | SDF | |
| Synonyms | LY344864;LY-344864 | ||
| Chemical Name | (R)-N-(3-(dimethylamino)-2,3,4,9-tetrahydro-1H-carbazol-6-yl)-4-fluorobenzamide | ||
| Canonical SMILES | CN([C@]1([H])CCC2=C(C3=C(N2)C=CC(NC(C4=CC=C(F)C=C4)=O)=C3)C1)C | ||
| Formula | C21H22FN3O | M.Wt | 351.42 |
| Solubility | DMSO : ≥ 350 mg/mL (995.96 mM) | 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 | 2.8456 mL | 14.228 mL | 28.456 mL |
| 5 mM | 0.5691 mL | 2.8456 mL | 5.6912 mL |
| 10 mM | 0.2846 mL | 1.4228 mL | 2.8456 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: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)
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