Size | Price | Stock | Qty |
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5mg |
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10mg |
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50mg |
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Other Sizes |
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ln Vitro |
In guinea pig cortical slices, LY310762 (0.01-1 µM) exhibits potassium-induced increase of [3H]5-HT efflux, with an EC50 value of 31 nM [1]. The decrease in excitatory postsynaptic potential (EPSC) caused by sumatriptan is largely, albeit not fully, blocked by LY310762 (10 µM) [3].
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ln Vivo |
Fluoxetine, a selective serotonin reuptake inhibitor, produces extracellular 5-HT concentrations in vivo. LY310762 (10 mg/kg; i.p.; single dose) greatly boosts these concentrations [1]. In a rat model of phenylephrine infusion, LY310762 (1 mg/kg; intravenous injection; single dosage) completely eliminates the vasodilatory effects of 5-HT [2].
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Animal Protocol |
Animal/Disease Models: Dunkin Hartley guinea pig (female; 350-400 g, Harlan) [1].
Doses: 10 mg/kg Route of Administration: intraperitoneal (ip) injection; Single Experimental Results:Further significant enhancement of 5-HT response to fluoxetine. Animal/Disease Models: Male Wistar rat (270-330 g; phenylephrine infusion rat model) [2]. Doses: 1 mg/kg Route of Administration: intravenous (iv) (iv)injection; Single Experimental Results:Complete elimination of the vasodilatory effect of 5-HT. |
References |
[1]. Pullar IA, et al. The role of the 5-HT1D receptor as a presynaptic autoreceptor in the guinea pig. Eur J Pharmacol. 2004 Jun 16;493(1-3):85-93.
[2]. García-Pedraza JÁ, et al. Pharmacological evidence that 5-HT1D activation induces renal vasodilation by NO pathway in rats. Clin Exp Pharmacol Physiol. 2015 Jun;42(6):640-7. [3]. Choi IS, Cho JH, An CH, Jung JK, Hur YK, Choi JK, Jang IS. 5-HT(1B) receptors inhibit glutamate release from primary afferent terminals in rat medullary dorsal horn neurons. Br J Pharmacol. 2012 Sep;167(2):356-67. |
Molecular Formula |
C24H28CLFN2O2
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Molecular Weight |
430.94
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Exact Mass |
430.18
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CAS # |
192927-92-7
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Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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SMILES |
CC1(C2=CC=CC=C2N(C1=O)CCN3CCC(CC3)C(=O)C4=CC=C(C=C4)F)C.Cl
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Synonyms |
LY-310762; LY 310762; LY310762
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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 Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
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 : ~18.33 mg/mL (~42.53 mM)
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1.83 mg/mL (4.25 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 18.3 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: ≥ 1.83 mg/mL (4.25 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 18.3 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: ≥ 1.83 mg/mL (4.25 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 | 2.3205 mL | 11.6025 mL | 23.2051 mL | |
5 mM | 0.4641 mL | 2.3205 mL | 4.6410 mL | |
10 mM | 0.2321 mL | 1.1603 mL | 2.3205 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.