MRGPRX1 agonist 1
Based on 1 Customer Validation
MRGPRX1 agonist 1 is a highly potent MRGPRX1 agonist (EC50=50 nM) with greater than 50-fold selectivity for δ, μ, and κ opioid receptors. MRGPRX1 agonist 1 is inactive against MRGPRC11. MRGPRC11 inhibits high voltage-activated (HVA) Ca2+ currents, reduces neurotransmitter release, and mitigates nociceptive transmission in the spinal cord. MRGPRX1 agonist 1 is useful for the study of chronic pain, especially neuropathic pain.
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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: 99.95%
- CAS 番号: 2377379-39-8
- 分子式: C23H21N3O4S
- 分子量:435.50
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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
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生物活性
EC50: 50 nM (MRGPRX1)[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | EC50 |
0.05 μM
Compound: 16
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Agonist activity at human MrgprX1 expressed in HEK293 cells incubated for 2 mins by Fluo4AM dye based FLIPR assay
Agonist activity at human MrgprX1 expressed in HEK293 cells incubated for 2 mins by Fluo4AM dye based FLIPR assay
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[PMID: 31498617] |
MRGPRX1 agonist 1 (compound 16) is an agonist of MRGPRX1. MRGPRX1 agonist 1 shows the binding affinity (Kis) for the δ-Opioid Receptor is 2.47 μM, for the μ-opioid receptor is 3.73 μM, and for the κ-opioid receptor is 12.10 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
化学情報
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CAS 番号 2377379-39-8
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性状 Solid
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分子量 435.50
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分子式 C23H21N3O4S
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Color White to yellow
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SMILES
O=S(C1=CC=CC=C1OC)(NC2=CC=C(C)C=C2OC3=CC4=C(C(N)=NC=C4)C=C3)=O
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
溶剤 & 溶解度
DMSO : 125 mg/mL (287.03 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. 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. 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)
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: ≥ 2.08 mg/mL (4.78 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (4.78 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
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 (280 KB)
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SDS (251 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. 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 | 2.2962 mL | 11.4811 mL | 22.9621 mL | 57.4053 mL |
| 5 mM | 0.4592 mL | 2.2962 mL | 4.5924 mL | 11.4811 mL | |
| 10 mM | 0.2296 mL | 1.1481 mL | 2.2962 mL | 5.7405 mL | |
| 15 mM | 0.1531 mL | 0.7654 mL | 1.5308 mL | 3.8270 mL | |
| 20 mM | 0.1148 mL | 0.5741 mL | 1.1481 mL | 2.8703 mL | |
| 25 mM | 0.0918 mL | 0.4592 mL | 0.9185 mL | 2.2962 mL | |
| 30 mM | 0.0765 mL | 0.3827 mL | 0.7654 mL | 1.9135 mL | |
| 40 mM | 0.0574 mL | 0.2870 mL | 0.5741 mL | 1.4351 mL | |
| 50 mM | 0.0459 mL | 0.2296 mL | 0.4592 mL | 1.1481 mL | |
| 60 mM | 0.0383 mL | 0.1914 mL | 0.3827 mL | 0.9568 mL | |
| 80 mM | 0.0287 mL | 0.1435 mL | 0.2870 mL | 0.7176 mL | |
| 100 mM | 0.0230 mL | 0.1148 mL | 0.2296 mL | 0.5741 mL |
MRGPRX1 agonist 1 関連分類
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