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.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit : 98.58%
- CAS. Nr.: 2467732-66-5
- Formel: C33H48FN7O4
- Molecular Weight:625.78
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Speicherung: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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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
Biologische Aktivität
Beschreibung
IC50 & Target
[1]|
IL-17A |
In Vitro
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 |
In Vivo
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.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS. Nr. 2467732-66-5
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Appearance Solid
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Molecular Weight 625.78
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Formel 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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Synonyms
DC-806; LY4100504; S-011806
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Lösungsmittel & Löslichkeit
In Vitro:
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.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Reinheit & Dokumentation
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Data Sheet (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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Handling Instructions (2659 KB)
Verweise
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 |
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