CS-2100
Based on 1 Customer Validation
CS-2100 (Compound 10b) is a potent, selective, orally active and S1P3-sparing S1P1 agonist with an EC50 of 4.0 nM for human S1P1. CS-2100 shows in vivo immunosuppressive efficacy in rats with an ID50 (infective dose) of 0.407 mg/kg for HvGR.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
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: 99.12%
- CAS 番号: 913827-99-3
- 分子式: C25H23N3O4S
- 分子量:461.53
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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
生物活性
EC50: 4.0 nM (human S1P1)[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO-K1 | EC50 |
1.5 nM
Compound: 8, CS-2100
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Agonist activity at rat S1P1 receptor expressed in CHO-K1 cells assessed as induction of GTPgammaS binding
Agonist activity at rat S1P1 receptor expressed in CHO-K1 cells assessed as induction of GTPgammaS binding
|
[PMID: 22405291] |
| CHO-K1 | EC50 |
4 nM
Compound: 8, CS-2100
|
Agonist activity at human S1P1 receptor expressed in CHO-K1 cells assessed as induction of GTPgammaS binding
Agonist activity at human S1P1 receptor expressed in CHO-K1 cells assessed as induction of GTPgammaS binding
|
[PMID: 22405291] |
| CHO-K1 | EC50 |
7400 nM
Compound: 8, CS-2100
|
Agonist activity at rat S1P3 receptor expressed in CHO-K1 cells assessed as induction of GTPgammaS binding
Agonist activity at rat S1P3 receptor expressed in CHO-K1 cells assessed as induction of GTPgammaS binding
|
[PMID: 22405291] |
| CHO-K1 | EC50 |
>20000 nM
Compound: 8, CS-2100
|
Agonist activity at human S1P3 receptor expressed in CHO-K1 cells assessed as induction of GTPgammaS binding
Agonist activity at human S1P3 receptor expressed in CHO-K1 cells assessed as induction of GTPgammaS binding
|
[PMID: 22405291] |
化学情報
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CAS 番号 913827-99-3
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性状 Solid
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分子量 461.53
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分子式 C25H23N3O4S
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Color Off-white to light yellow
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SMILES
O=C(C1CN(CC2=CC(CC)=C(C3=NOC(C4=CC=C(OC5=CC=CC=C5)C=C4)=N3)S2)C1)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 : 12.5 mg/mL (27.08 mM; ultrasonic and warming and heat to 60°C; 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: ≥ 1.25 mg/mL (2.71 mM); Clear solution
This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 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.
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 (269 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
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- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Portuguese - PT (254 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 | 2.1667 mL | 10.8335 mL | 21.6671 mL | 54.1677 mL |
| 5 mM | 0.4333 mL | 2.1667 mL | 4.3334 mL | 10.8335 mL | |
| 10 mM | 0.2167 mL | 1.0834 mL | 2.1667 mL | 5.4168 mL | |
| 15 mM | 0.1444 mL | 0.7222 mL | 1.4445 mL | 3.6112 mL | |
| 20 mM | 0.1083 mL | 0.5417 mL | 1.0834 mL | 2.7084 mL | |
| 25 mM | 0.0867 mL | 0.4333 mL | 0.8667 mL | 2.1667 mL |