JAK3 covalent inhibitor-2
JAK3 covalent inhibitor-2 (compound J1b) is a selective, orally potent JAK3 inhibitor (IC50=7.2 nM) with low toxicity, anti-inflammatory activity and good bioavailability.
For research use only. We do not sell to patients.
- CAS No.: 2664050-97-7
- Formula: C20H20N6O3
- Molecular Weight:392.41
-
Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biological Activity
-
Chemical Information
- Purity & Documentation
- References
-
Help & FAQs
Biological Activity
|
JAK3 7.2 nM (IC50) |
JAK3 covalent inhibitor-2 shows low cytotoxicity among HEK293, LO2, chondrocytes and RAW264.7 with IC50s (72 h) of 86.82 μM (HEK293), 61.79 μM (LO2), >32 μM (chondrocytes) and >32 μM (RAW264.7) respectively[1].
JAK3 covalent inhibitor-2 (100 mM; 90 min) shows t1/2 of 13.1 min and 43.9 min in human and rat liver microsomes, respectively. And the clean rate of 132.5 mL/min/kg and mL/min/kg, resepectively[1].
JAK3 covalent inhibitor-2 ((0.125-8 μM; 48 h)) dose-dependently induces T lymphocytes apoptosis[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Cell Line:CD4+ T cells , CD8[1] T cells
-
Concentration:0.125, 0.5, 1, 2, 4, 8 μM
-
Incubation Time:48 h
-
Result:Dose-dependently led to apoptosis among CD4+ and CD8+ T cells
Toxicity: JAK3 covalent inhibitor-2 (2 g/kg, p.o.; single dose) Liver and kidney appeare to be similar to those of normal mice, no weight loss or other adverse effects are observed[1].
Pharmacokinetics: JAK3 covalent inhibitor-2 (5 mg/kg; p.o.), clearance (Cl) 7.37 l/h/kg, oral half-life (t1/2=3.77 h), and bioavailability (F = 31.69%)[1].
Pharmacokinetic parameters of compound JAK3 covalent inhibitor-2 in SD rats[1]
Pharmacokinetic Analysis[1]
| Route | Dose (mg/kg) | Cmax (mg/L) | tmax (h) | t1/2 (h) | AUC0-t (mg/L·h) | V<, V/F (L/kg) | Cl, Cl/F (L/h/kg) | F (%) |
| i.v. | 5 | 4497.32 | 0.08 | 2.63 | 2161.38 | 8.98 (V) | 2.32V (Cl) | 31.69 |
| p.o. | 5 | 501.8 | 0.25 | 3.77 | 684.87 | 39.89 (V/F) | 7.37 (Cl/F) | / |