RAI-20
Based on 1 Customer Validation
RAI-20 (H018) is an orally active JAK1/JAK2 dual inhibitor (IC50=15.1 and 22.7 nM). RAI-20 exhibits excellent pharmacokinetic properties, including plasma stability, systemic exposure, and a long half-life. In a collagen-induced arthritis rat model, RAI-20 shows significant anti-inflammatory and anti-arthritic activities, effectively reducing paw swelling volume and arthritis index. RAI-20 can be used for research on the pathogenesis of rheumatoid arthritis.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit : 98.66%
- CAS. Nr.: 2549180-90-5
- Formel: C20H21FN4O3S2
- Molecular Weight:448.53
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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
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JAK2 22.7 nM (IC50) |
JAK1 15.1 nM (IC50) |
In Vitro
RAI-20 (3×10- serial dilutions; under standard cell culture conditions) potently inhibits Ba/F3 cell proliferation with an IC50 of 1.21 μM[1].
RAI-20 (serial dilutions; 10 min compound pre-incubation, 10 min IL-6 stimulation) inhibits IL-6-induced pSTAT1 expression in human whole blood cells with an IC50 of 1.45 μM[1].
RAI-20 (up to 10 μM (CYP inhibition), serial dilutions (other assays); incubated to measure T1/2 (plasma stability, hepatic microsomal stability)) exhibits favorable in vitro pharmacokinetic properties including prolonged human plasma stability, moderate hepatic microsomal metabolism, high plasma protein binding, no significant CYP inhibition, and hERG inhibition with an IC50 of 11.5 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Ba/F3 cell
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Concentration:3x serial dilutions
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Incubation Time:under standard cell culture conditions
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Result:Inhibited Ba/F3 cell proliferation with an IC50 of 1.21 μM.
Parmacokinetics
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Lewis rats (immunized with type II collagen intradermally at the base of the tail on day 0, followed by a booster immunization on day 7)[1]
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Dosage:2 mg/kg; 3 mg/kg; 5 mg/kg; 10 mg/kg
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Administration:p.o.; daily; 14 days
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Result:Exhibited dose-dependent reductions in arthritis index, with scores of 8.63, 9.25, 8.00, and 7.25 for the 2 mg/kg, 3 mg/kg, 5 mg/kg, and 10 mg/kg doses, respectively.
Showed lower hind paw volume (3.826 ± 0.075 cm3 at day 28) and arthritis index at every time point from day 17 to day 28 in the 10 mg/kg group compared to other control drugs.
Demonstrated a trend of body weight recovery in all dose groups during days 24-28.
Chemical Information
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CAS. Nr. 2549180-90-5
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Appearance Solid
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Molecular Weight 448.53
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Formel C20H21FN4O3S2
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Color Light yellow to yellow
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SMILES
O=C([C@H]1[C@H](F)C1)NC2=CN3C(C4=CC=C(CN5CCS(CC5)(=O)=O)S4)=CC=CC3=N2
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Synonyms
H018
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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 : 50 mg/mL (111.48 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 (283 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 |
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| DMSO | 1 mM | 2.2295 mL | 11.1475 mL | 22.2951 mL | 55.7376 mL |
| 5 mM | 0.4459 mL | 2.2295 mL | 4.4590 mL | 11.1475 mL | |
| 10 mM | 0.2230 mL | 1.1148 mL | 2.2295 mL | 5.5738 mL | |
| 15 mM | 0.1486 mL | 0.7432 mL | 1.4863 mL | 3.7158 mL | |
| 20 mM | 0.1115 mL | 0.5574 mL | 1.1148 mL | 2.7869 mL | |
| 25 mM | 0.0892 mL | 0.4459 mL | 0.8918 mL | 2.2295 mL | |
| 30 mM | 0.0743 mL | 0.3716 mL | 0.7432 mL | 1.8579 mL | |
| 40 mM | 0.0557 mL | 0.2787 mL | 0.5574 mL | 1.3934 mL | |
| 50 mM | 0.0446 mL | 0.2230 mL | 0.4459 mL | 1.1148 mL | |
| 60 mM | 0.0372 mL | 0.1858 mL | 0.3716 mL | 0.9290 mL | |
| 80 mM | 0.0279 mL | 0.1393 mL | 0.2787 mL | 0.6967 mL | |
| 100 mM | 0.0223 mL | 0.1115 mL | 0.2230 mL | 0.5574 mL |
RAI-20 Related Classifications
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