MS-553
Based on 1 Customer Validation
MS-553 is a potent, ATP-competitive and reversible inhibitor of conventional PKC enzymes with Kis of 5.3 and 10.4 nM for human PKCβ and PKCα, and IC50s of 2.3, 8.1, 7.6, 25.6, 57.5, 314, 808 nM for PKCα, PKCβI, PKCβII, PKCθ, PKCγ, PKC mu and PKCε, respectively.
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: 99.79%
- CAS 番号: 1046787-18-1
- 分子式: C25H37FN8O2
- 分子量:500.61
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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
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
- プロトコル
- 純度とドキュメンテーション
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生物活性
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Human PKCα 2.3 nM (IC50) |
Human PKCβII 7.6 nM (IC50) |
Human PKCβI 8.1 nM (IC50) |
Human PKCθ 25.6 nM (IC50) |
Human PKCγ 57.5 nM (IC50) |
Human PKC mu 314 nM (IC50) |
Human PKCε 808 nM (IC50) |
Human PKCβ 5.3 nM (Ki) |
Human PKCα 10.4 nM (Ki) |
MS-553 (Compound A) is a potent, ATP-competitive and reversible of conventional PKC enzymes with Kis of 5.3 and 10.4 nM for human PKCβ and PKCα, and IC50s of 2.3, 8.1, 7.6, 25.6, 57.5, 314, 808 nM for PKCα, PKCβI, PKCβII, PKCθ, PKCγ, PKC mu and PKCε, respectively[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
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 1046787-18-1
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性状 Solid
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分子量 500.61
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分子式 C25H37FN8O2
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Color White to off-white
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SMILES
O=C(N1[C@@H](C)CN(CC2CCOCC2)[C@H](C)C1)N(C3)C(C)(C)C4=C3C(NC5=NC(C)=NC=C5F)=NN4
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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
溶剤 & 溶解度
DMSO : 200 mg/mL (399.51 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[1]
MS-553 is tested in the experimental autoimmune encephalitis (EAE) model in Lewis rats. EAE is induced by MBP69-88/CFA immunization and pertussis toxin injection in Lewis rats. MS-553 is prepared as an oral suspension and dosed orally, twice per day (BID) at three doses, 7.5 and 15 and 30 mg/kg for total daily doses of 15, 30 and 60 mg/kg. The efficacy is compared to animals that receive the positive control FTY720 dosed once per day at a dose of 0.5 mg/kg. The treatment starts on Day 8, when 48% of the rats have signs of EAE[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 (274 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (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, 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 | 1.9976 mL | 9.9878 mL | 19.9756 mL | 49.9391 mL |
| 5 mM | 0.3995 mL | 1.9976 mL | 3.9951 mL | 9.9878 mL | |
| 10 mM | 0.1998 mL | 0.9988 mL | 1.9976 mL | 4.9939 mL | |
| 15 mM | 0.1332 mL | 0.6659 mL | 1.3317 mL | 3.3293 mL | |
| 20 mM | 0.0999 mL | 0.4994 mL | 0.9988 mL | 2.4970 mL | |
| 25 mM | 0.0799 mL | 0.3995 mL | 0.7990 mL | 1.9976 mL | |
| 30 mM | 0.0666 mL | 0.3329 mL | 0.6659 mL | 1.6646 mL | |
| 40 mM | 0.0499 mL | 0.2497 mL | 0.4994 mL | 1.2485 mL | |
| 50 mM | 0.0400 mL | 0.1998 mL | 0.3995 mL | 0.9988 mL | |
| 60 mM | 0.0333 mL | 0.1665 mL | 0.3329 mL | 0.8323 mL | |
| 80 mM | 0.0250 mL | 0.1248 mL | 0.2497 mL | 0.6242 mL | |
| 100 mM | 0.0200 mL | 0.0999 mL | 0.1998 mL | 0.4994 mL |
MS-553 関連分類
HY-16903 関連分類
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