| Size | Price | Stock | Qty |
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| 25mg |
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| 50mg |
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| 100mg |
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LY-344864 (LY344864) is a novel, potent and selective receptor agonist of 5-HT1F with Ki of 6 nM. Compared to the 56 other serotonergic and non-serotonergic neuronal binding sites that were studied, it exhibits negligible affinity. It has been demonstrated that LY344864 is a full agonist, having an impact comparable to that of serotonin.
| Targets |
human 5-HT1F Receptor ( IC50 = 0.006 μM ); human 5-HT1A Receptor ( IC50 = 0.530 μM ); human 5-HT1B Receptor ( IC50 = 0.549 μM );
human 5-HT1D Receptor ( IC50 = 0.575 μM ); human 5-HT1E Receptor ( IC50 = 1.415 μM ); human 5-HT2B Receptor ( IC50 = 1.695 μM ); Human 5-HT2A Receptor ( IC50 = 3.499 μM ); Human 5-HT3A Receptor ( IC50 = 3.935 mM ); Human 5-HT7 Receptor ( IC50 = 4.851 μM ); rat α2-adrenergic receptor ( IC50 = 3.69 μM ); rat α1-adrenergic receptor ( IC50 = 5.06 μM ) |
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| ln Vitro |
LY 344864 binds to human 5-HT1F, 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT3A, 5-HT2B, 5-HT2C, and 5-HT7, as well as rat α1-adrenergic and rat α2-adrenergic receptors with Kis of 0.006, 0.530, 0.549, 0.575, 1.415, 3.935, 1.695, 3.499, 4.851, 5.06 and 3.69 μM, respectively[1]. LY 344864 is a inducer of mitochondrial biogenesis[2].
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| ln Vivo |
LY 344864 (0-10 ng/kg; oral or intravenous; once) inhibits neurogenic dural inflammation in a rat migraine model [1]. LY 344864 (1 mg/kg; intravenous injection; once) can cross the blood-brain barrier to a certain extent in rats [1]. LY 344864 (2 mg/kg; i.p.; daily for 14 days) attenuates dopaminergic neuron loss and improves behavioral endpoints in a mouse model of Parkinson's disease [2]. Animal model: Male Wistar rat, migraine model [1] Dosage: 1-10 ng/kg (oral), 0.3-2 ng/kg (intravenous injection) Administration method: oral, 75 minutes before trigeminal nerve stimulation or intravenously Injection, stimulation results 10 minutes before trigeminal nerve stimulation: When injected intravenously 10 minutes before stimulation, it can inhibit inflammation, with an ID50 (median infectious dose) of 0.6 ng/kg. When administered orally 75 minutes before trigeminal nerve stimulation, an ID50 of 1.2 ng/kg was obtained. Animal model: Male C57BL/6 mice, Parkinson's disease model [2] Dose: 2 mg/kg Administration: intraperitoneal injection, starting 7 days after injury, daily for 14 days Results: Compared with vehicle, Attenuated TH-ir loss in the striatum and substantia nigra-treated lesioned animals also increased locomotor activity in 6-hydroxydopamine-lesioned mice, whereas vehicle treatment had no effect.
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| Animal Protocol |
Male Wistar rats, migraine pain model
1-10 ng/kg (oral), 0.3-2 ng/kg (intravenous) Oral, 75 minutes before trigeminal stimulation or intravenous, 10 minutes before trigeminal stimulation |
| References |
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| Molecular Formula |
C21H22FN3O
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|---|---|
| Molecular Weight |
351.43
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| Exact Mass |
351.17
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| Elemental Analysis |
C, 71.77; H, 6.31; F, 5.41; N, 11.96; O, 4.55
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| CAS # |
186544-26-3
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| Related CAS # |
LY 344864 S-enantiomer; 186544-27-4; LY 344864 racemate; 186543-64-6; LY 344864 hydrochloride; 1217756-94-9
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| Appearance |
Solid powder
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| SMILES |
CN(C)[C@@H]1CCC2=C(C1)C3=C(N2)C=CC(=C3)NC(=O)C4=CC=C(C=C4)F.Cl
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| InChi Key |
OKUHLSYESBLBCP-PKLMIRHRSA-N
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| InChi Code |
InChI=1S/C21H22FN3O.ClH/c1-25(2)16-8-10-20-18(12-16)17-11-15(7-9-19(17)24-20)23-21(26)13-3-5-14(22)6-4-13;/h3-7,9,11,16,24H,8,10,12H2,1-2H3,(H,23,26);1H/t16-;/m1./s1
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| Chemical Name |
N-[(6R)-6-(dimethylamino)-6,7,8,9-tetrahydro-5H-carbazol-3-yl]-4-fluorobenzamide;hydrochloride
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| Synonyms |
LY-344864; LY 344864; LY344864; LY-344864 free base
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| HS Tariff Code |
2934.99.9001
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| 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)
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| Solubility (In Vitro) |
DMSO: ~100 mg/mL (~284.6 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.11 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (7.11 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (7.11 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.8455 mL | 14.2276 mL | 28.4552 mL | |
| 5 mM | 0.5691 mL | 2.8455 mL | 5.6910 mL | |
| 10 mM | 0.2846 mL | 1.4228 mL | 2.8455 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.
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