Navepdekinra
Based on 1 Customer Validation
Navepdekinra (DC-806) is an orally active, potent interleukin-17A (IL-17A) inhibitor (IC50 = 10.81 nM). Navepdekinra disrupts the IL-17A protein-receptor interaction, suppressing the downstream pro-inflammatory signaling pathway. Navepdekinra inhibits arthritis in a collage-induced arthritis (CIA) rat model. Navepdekinra can be used for psoriasis, psoriatic arthritis, and ankylosing spondylitis.
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 : 98.58%
- CAS 番号: 2467732-66-5
- 分子式: C33H48FN7O4
- 分子量:625.78
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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
製品説明
IC50 & Target
[1]|
IL-17A |
体外実験
Navepdekinra (1 μM, 0-60 min) shows metabolic stability in rat liver microsomes (RLM) but exhibits moderate metabolic clearance in human liver microsomes (HLM)[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Parmacokinetics
| Species | Dose | Route | T1/2 | Tmax | Cmax | AUCinf |
|---|---|---|---|---|---|---|
| Rat[3] | 25 mg/kg | p.o. | 2.66 h | 0.75 h | 614 ng/mL | 1869 ng·h/mL |
体内実験
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male Wistar rats (6 weeks old) intradermally injected with emulsified Collagen II (CII) in Complete Freund's Adjuvant (CFA) on both day 0 and day 7[3]
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Dosage:25 mg/kg
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Administration:p.o., b.i.d. for 9 days
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Result:Showed 28.10% inhibition of arthritis.
臨床実験
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 2467732-66-5
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性状 Solid
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分子量 625.78
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分子式 C33H48FN7O4
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Color white
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SMILES
O=C(C1=CC=NN1CC)N[C@@H]([C@@]2([H])CC[C@@H](CC2)C)C(NC3=C(C=C(C=C3)[C@H](C)[C@@H](NC(CC)=O)C(N4CCN(CC4)C)=O)F)=O
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別名
DC-806; LY4100504; S-011806
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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
体外:
DMSO : 100 mg/mL (159.80 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)
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 (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (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 | 1.5980 mL | 7.9900 mL | 15.9801 mL | 39.9501 mL |
| 5 mM | 0.3196 mL | 1.5980 mL | 3.1960 mL | 7.9900 mL | |
| 10 mM | 0.1598 mL | 0.7990 mL | 1.5980 mL | 3.9950 mL | |
| 15 mM | 0.1065 mL | 0.5327 mL | 1.0653 mL | 2.6633 mL | |
| 20 mM | 0.0799 mL | 0.3995 mL | 0.7990 mL | 1.9975 mL | |
| 25 mM | 0.0639 mL | 0.3196 mL | 0.6392 mL | 1.5980 mL | |
| 30 mM | 0.0533 mL | 0.2663 mL | 0.5327 mL | 1.3317 mL | |
| 40 mM | 0.0400 mL | 0.1998 mL | 0.3995 mL | 0.9988 mL | |
| 50 mM | 0.0320 mL | 0.1598 mL | 0.3196 mL | 0.7990 mL | |
| 60 mM | 0.0266 mL | 0.1332 mL | 0.2663 mL | 0.6658 mL | |
| 80 mM | 0.0200 mL | 0.0999 mL | 0.1998 mL | 0.4994 mL | |
| 100 mM | 0.0160 mL | 0.0799 mL | 0.1598 mL | 0.3995 mL |