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JAK-IN-21
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
JAK-IN-21图片
CAS NO:2445499-20-5
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品介绍
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)

体外研究
(In Vitro)

JAK-IN-21 (Example 4) doses not inhibit CYPs and shows good liver microsome stability[1].

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]
CompoundPlasma Cmax
(ng/mL)
Plasma AUC
(h*ng/mL)
t1/2(h)Colon AUC
(h*ng/g)
Colon + Feces AUC
(h*ng/g)
JAK-IN-2168.8961.66,623545,501
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]
CompoundDose
(mg/kg)
AUC
(h*ng/mL)
T1/2(h)Cl
(mL/min/kg)
Vd
(L/kg)
Cmax
(ng/mL)
F (%)
JAK-IN-21 (iv)1854.80.2219.40.37
JAK-IN-21 (ig)229.80.3840.41.9
分子量

372.38

Formula

C19H16N8O

CAS 号

2445499-20-5

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.