JAK-IN-20 是一种有效的，广泛的，具有口服活性的JAK抑制剂，对 JAK1，JAK2，JAK3 的IC50值分别为 7 nM、5 nM、14 nM。JAK-IN-20 在体内表现出优异的药代动力学和抗炎功效。
| 生物活性 | JAK-IN-20 is a potent, pan and orally activeJAKinhibitor with anIC50s of 7 nM, 5 nM, 14 nM forJAK1,JAK2,JAK3, respectively. JAK-IN-20 shows excellent pharmacokinetics and displays anti-inflammatory efficacy in vivo[1]. |
| IC50& Target | JAK1 7 nM (IC50) | JAK2 5 nM (IC50) | JAK3 14 nM (IC50) |
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体内研究
(In Vivo) | JAK-IN-20 (compound 32) (3 mg/kg for p.o.; 1 mg/kg for i.v.) shows excellent pharmacokinetics in rats[1].
JAK-IN-20 (10 mg/kg; p.o.; once a day for 3 days) shows anti-inflammatory effect[1].
Pharmacokinetic Parameters of JAK-IN-20 in female Sprague Dawley rats[1].
| parameter | 32 | | PO Dose (mg/kg) | 3 | | Tmax(h) | 0.63(0.25-6) | | Cmax(μg/mL) | 7.82±3.68 | | AUC0-t(μg.h/mL) | 80.18±35.44 | | T1/2,po (h) | 4.77±1.84 | | MRT (h) | 7.54±2.52 | | IV Dose (mg/kg) | 1 | | C0(μg/mL) | 4.70±2.50 | | AUC0-t(μg.h/mL) | 18.89±1.76 | | Vss(L/kg) | 0.32±0.14 | | CL (mL/min/kg) | 0.85±0.13 | | T1/2,iv (h) | 5.16±3.83 | | MRT (h) | 6.69±4.03 | | %F | 100 |
Wistar rats; 3 mg/kg; p.o. (1% Tween 80 + 99% (0.5%) methyl cellulose in water); 1 mg/kg; i.v. (5% NMP + 5% solutol + 90% normal saline) [1]
| Animal Model: | 7-10 weeks, 250-300g, male wistar rats[1] | | Dosage: | | | Administration: | 3 mg/kg for p.o.; 1 mg/kg for i.v. | | Result: | Showed fast oral absorption, higher plasma exposure, extended oral half-life and excellent oral bioavailability of 100%. |
| Animal Model: | Female Sprague Dawley rats ( PGPS rat model)[1] | | Dosage: | 10 mg/kg | | Administration: | P.o.; once a day; 3 days | | Result: | Showed anti-inflammatory effect. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
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