LY310762
Based on 1 publication(s) in Google Scholar
LY310762 is a selective 5-HT1D receptor antagonist (Ki=249 nM) with a weak affinity for 5-HT1B receptor. LY310762 effectively abolishes the renal vasodilatory effects of 5-HTSumatriptan (HY-B0121B)-induced decrease in excitatory postsynaptic potential (EPSC) amplitude.
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- Reinheit: 98.89%
- CAS. Nr.: 192927-92-7
- Formel: C24H28ClFN2O2
- Molecular Weight:430.94
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Speicherung:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
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Publications Citing Use of MedChemExpress (MCE) LY310762
MoreAlle 5-HT Receptor Isoform-spezifische Produkte anzeigen
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Biologische Aktivität
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5-HT1B Receptor |
5-HT1D Receptor |
5-HT1D Receptor 249 nM (Ki) |
LY310762 (0.01-1 μM) shows potentiation of potassium-induced [3H]5-HT outflow from guinea pig cortical slices with an EC50 value of 31 nM[1].
LY310762 (10 μM) significantly but not completely blocks the extent of sumatriptan-induced decrease in EPSCs (excitatory postsynaptic potential)[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
LY310762 (1 mg/kg; i.v.; single) abolishes 5-HT vasodilator effects in phenylephrine-infusion rats model[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Dunkin Hartley guinea pigs (female; 350-400 g, Harlan)[1].
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Dosage:10 mg/kg
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Administration:Intraperitoneal injection; single
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Result:Produced a further significant enhancement in the 5-HT response to fluoxetine.
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Animal Model:Male Wistar rats (270-330 g; phenylephrine-infusion rats model)[2].
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Dosage:1 mg/kg
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Administration:Intravenous injection; single
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Result:Completely abolished 5-HT vasodilator effects.
Chemical Information
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CAS. Nr. 192927-92-7
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Appearance Solid
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Molecular Weight 430.94
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Formel C24H28ClFN2O2
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Color White to off-white
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SMILES
O=C1N(CCN2CCC(C(C3=CC=C(F)C=C3)=O)CC2)C4=C(C=CC=C4)C1(C)C.[H]Cl
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (1)
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Journal Impact Factor
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Most Recent
Lösungsmittel & Löslichkeit
DMSO : 18.33 mg/mL (42.53 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 1.83 mg/mL (4.25 mM); Clear solution
This protocol yields a clear solution of ≥ 1.83 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (18.3 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 1.83 mg/mL (4.25 mM); Clear solution
This protocol yields a clear solution of ≥ 1.83 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (18.3 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Reinheit & Dokumentation
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Data Sheet (279 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
Verweise
[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. [Content Brief]
[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. [Content Brief]
[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. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.3205 mL | 11.6025 mL | 23.2051 mL | 58.0127 mL |
| 5 mM | 0.4641 mL | 2.3205 mL | 4.6410 mL | 11.6025 mL | |
| 10 mM | 0.2321 mL | 1.1603 mL | 2.3205 mL | 5.8013 mL | |
| 15 mM | 0.1547 mL | 0.7735 mL | 1.5470 mL | 3.8675 mL | |
| 20 mM | 0.1160 mL | 0.5801 mL | 1.1603 mL | 2.9006 mL | |
| 25 mM | 0.0928 mL | 0.4641 mL | 0.9282 mL | 2.3205 mL | |
| 30 mM | 0.0774 mL | 0.3868 mL | 0.7735 mL | 1.9338 mL | |
| 40 mM | 0.0580 mL | 0.2901 mL | 0.5801 mL | 1.4503 mL |
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