JAK-IN-21 (Example 4) 是一种选择性的、有效的JAK抑制剂，对 JAK1、JAK2、J2V617F 和 TYK2 的IC50分别为 1.73、2.04、109 和 62.9 nM。
| 生物活性 | JAK-IN-21 (Example 4) is a selective and potentJAKinhibitor withIC50s of 1.73, 2.04, 109 and 62.9 nM againstJAK1,JAK2, J2V617F andTYK2, respectively[1]. |
| IC50& Target[1] | JAK1 1.73 nM (IC50) | JAK2 2.04 nM (IC50) | Tyk2 62.9 nM (IC50) | JAK2-V617F 109 nM (IC50) |
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体外研究
(In Vitro) | JAK-IN-21 (Example 4) doses not inhibit CYPs and shows good liver microsome stability[1].
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体内研究
(In Vivo) | JAK-IN-21 (Example 4) shows low bioavailability (F=1.9%)[1].
| Animal Model: | SD rats[1] | | Dosage: | 10 mg/kg | | Administration: | Oral gavage (Pharmacokinetic Study) | | Result: | Rat Colon Pharmacokinetic Study[1]
| Compound | Plasma Cmax
(ng/mL) | Plasma AUC
(h*ng/mL) | t1/2(h) | Colon AUC
(h*ng/g) | Colon + Feces AUC
(h*ng/g) | | JAK-IN-21 | 68.8 | 96 | 1.6 | 6,623 | 545,501 |
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| Animal Model: | SD rats[1] | | Dosage: | 1 mg/kg or 2 mg/kg | | Administration: | Intravenous injection (1 mg/kg) or oral gavage (2 mg/kg) (Pharmacokinetic Study) | | Result: | Pharmacokinetic Parameters in Sprague-Dawley Rats by Intravenous Administration and Oral Administration[1]
| Compound | Dose
(mg/kg) | AUC
(h*ng/mL) | T1/2(h) | Cl
(mL/min/kg) | Vd
(L/kg) | Cmax
(ng/mL) | F (%) | | JAK-IN-21 (iv) | 1 | 854.8 | 0.22 | 19.4 | 0.37 | | | | JAK-IN-21 (ig) | 2 | 29.8 | 0.38 | | | 40.4 | 1.9 |
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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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