Etrasimod
Based on 1 publication(s) in Google Scholar
Etrasimod (APD334) is a potent, selective and orally available antagonist of the sphingosine-1-phosphate-1 (S1P1) receptor with an IC50 value of 1.88 nM in CHO cells.
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- 純度: 99.91%
- CAS 番号: 1206123-37-6
- 分子式: C26H26F3NO3
- 分子量:457.48
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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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
- プロトコル
- 純度とドキュメンテーション
- 参考文献
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MedChemExpress（MCE）の使用を引用している文献 Etrasimod
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生物活性
IC50: 1.88 nM (S1P1)[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO | IC50 |
1.88 nM
Compound: (R)-4, APD334
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Induction of internalization of HA-tagged human S1P1 receptor expressed in CHO cells
Induction of internalization of HA-tagged human S1P1 receptor expressed in CHO cells
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[PMID: 25516790] |
| THP-1 | CC50 |
57.7 μM
Compound: 1; Etra
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Cytotoxicity against human THP-1 cells assessed as reduction in cell viability incubated for 24 hrs by resazurin staining based analysis
Cytotoxicity against human THP-1 cells assessed as reduction in cell viability incubated for 24 hrs by resazurin staining based analysis
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[PMID: 37948883] |
APD334 is a structurally novel, selective, functional antagonist of S1P1. In CHO cells expressing HA tagged S1P1, APD334 is found to have an IC50 value of 1.88 nM. Moderate agonism at human S1P4 and S1P5 is observed but is reduced relative to S1P1, both in terms of potency and efficacy. APD334 is devoid of any agonism or antagonism at human S1P2 and S1P3. APD334 achieves good central exposure following oral dosing and possesses a favorable pharmacokinetic profile in multiple preclinical species. S1P1 activity is maintained in mice (EC50=0.44 nM), rats (EC50=0.32 nM), dogs (EC50=0.34 nM) and monkeys (EC50=0.32 nM)[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.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 1206123-37-6
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性状 Solid
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分子量 457.48
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分子式 C26H26F3NO3
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Color White to khaki
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SMILES
FC(F)(F)C1=CC(COC2=CC=C(NC3=C4CC[C@@H]3CC(O)=O)C4=C2)=CC=C1C5CCCC5
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別名
APD334
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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 2 years -20°C 1 year
Publications (1)
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Journal Impact Factor
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Most Recent
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Heliyon
Development and validation of stability-indicating method of etrasimod by HPLC/DAD/MS/MS technique with greenness profiling. [Abstract]2024 Jul 4;10(13):e34066. PMID: 39071639
溶剤 & 溶解度
DMSO : 116.67 mg/mL (255.03 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
プロトコル
Rats: APD334 induced effects on blood lymphopenia are determined in male Sprague-Dawley rats. Briefly, male rats are given a 0 (vehicle only), 0.03 (mice only), 0.1, 0.3 or 1 mg/kg oral dose of APD334 formulated in 0.5% methylcellulose (MC) in water. Rat blood samples are collected at 0, 1, 3, 5, 8, 16, 24, 32, 48 and 72 hours post-dose[1].
Mice: APD334 induced effects on blood lymphopenia are determined in male BALB/c mice. Briefly, male mice are given a 0 (vehicle only), 0.03 (mice only), 0.1, 0.3 or 1 mg/kg oral dose of APD334 formulated in 0.5% methylcellulose (MC) in water. Mouse blood samples are taken at 0, 1, 3, 5, 8, 16, 24 and 32 hours post-dose[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
純度とドキュメンテーション
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データシート (273 KB)
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SDS (393 KB)
- English - EN (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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.1859 mL | 10.9294 mL | 21.8589 mL | 54.6472 mL |
| 5 mM | 0.4372 mL | 2.1859 mL | 4.3718 mL | 10.9294 mL | |
| 10 mM | 0.2186 mL | 1.0929 mL | 2.1859 mL | 5.4647 mL | |
| 15 mM | 0.1457 mL | 0.7286 mL | 1.4573 mL | 3.6431 mL | |
| 20 mM | 0.1093 mL | 0.5465 mL | 1.0929 mL | 2.7324 mL | |
| 25 mM | 0.0874 mL | 0.4372 mL | 0.8744 mL | 2.1859 mL | |
| 30 mM | 0.0729 mL | 0.3643 mL | 0.7286 mL | 1.8216 mL | |
| 40 mM | 0.0546 mL | 0.2732 mL | 0.5465 mL | 1.3662 mL | |
| 50 mM | 0.0437 mL | 0.2186 mL | 0.4372 mL | 1.0929 mL | |
| 60 mM | 0.0364 mL | 0.1822 mL | 0.3643 mL | 0.9108 mL | |
| 80 mM | 0.0273 mL | 0.1366 mL | 0.2732 mL | 0.6831 mL | |
| 100 mM | 0.0219 mL | 0.1093 mL | 0.2186 mL | 0.5465 mL |
Etrasimod 関連分類
HY-12789 関連分類
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