LY310762
Based on 1 publication(s) in Google Scholar
LY310762 is a selective 5-HT1D receptor antagonist with a Ki value of 249 nM for the guinea pig receptor. LY310762 blocks presynaptic 5-HT1D autoreceptors and enhances potassium-stimulated [3H]5-HT outflow from guinea pig cortical slices. LY310762 abolishes the inhibitory effect of 5-CT (HY-135555)/L-694,247 (HY-101208) on sympathetic nerve-induced renal vasoconstriction mediated by prejunctional 5-HT1D receptors. LY310762 potentiates the increase in extracellular 5-HT concentration induced by Fluoxetine (HY-B0102). LY310762 is used in research related to depression and diabetic nephropathy.
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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度 : 98.89%
- CAS 番号: 192927-92-7
- 分子式: C24H28ClFN2O2
- 分子量:430.94
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保管条件:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
MedChemExpress（MCE）の使用を引用している文献 LY310762
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生物活性
製品説明
IC50 & Target
[1]|
5-HT1D Receptor 249 nM (Ki) |
体外実験
LY310762 (1000 nM) shows preferential affinity for the guinea pig 5-HT1D receptor (Ki = 249 nM) over the guinea pig 5-HT1B receptor[1].
LY310762 potentiates potassium-stimulated [3H]5-HT release from guinea pig cortical slices with an EC50 of 31 nM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. .
体内実験
LY310762 (1 mg/kg; i.v.) alone does not alter electrically stimulated-induced pressor responses in Fluoxetine-treated decerebrate rats[3].
LY310762 (1 mg/kg; i.v.) blocks the sympathoinhibitory effect of the 5-HT1D agonist L-694,247 (HY-101208), confirming the involvement of presynaptic 5-HT1D receptors in Fluoxetine-treated rats[3].
LY310762 (1 mg/kg; i.v.) , when combined with the 5-HT1A antagonist WAY-100,635, eliminates 5-HT-induced sympathoinhibition in Fluoxetine-treated rats, confirming the involvement of both presynaptic 5-HT1A and 5-HT1D receptors[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Dunkin Hartley (female, 350-400 g)[1]
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Dosage:10 mg/kg (after Fluoxetine); 10 mg/kg (alone)
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Administration:i.p.; single administration
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Result:Increased extracellular 5-HT levels from 312% to a maximum of 683% in fluoxetine-treated animals.
Increased basal 5-HT levels to a maximum of 258% when administered alone.
化学情報
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CAS 番号 192927-92-7
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性状 Solid
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分子量 430.94
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分子式 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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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
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
溶剤 & 溶解度
体外:
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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
体内:
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.
In Vivo Dissolution Calculator
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.
純度とドキュメンテーション
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データシート (279 KB)
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SDS (393 KB)
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取扱説明書 (2659 KB)
参考文献
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 |
LY310762 関連分類
HY-13527 関連分類
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