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Delgocitinib
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。
Delgocitinib图片
CAS NO:1263774-59-9
包装与价格:
包装价格(元)
10 mM * 1 mL in DMSO电议
1mg电议
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议
200mg电议
500mg电议

产品名称
JTE-052
产品介绍
Delgocitinib (JTE-052) 是一种特异性的JAK抑制剂,对 JAK1, JAK2, JAK3 和 Tyk2 的IC50值分别为 2.8,2.6,13 和 58 nM。
生物活性

Delgocitinib (JTE-052) is a specificJAKinhibitor withIC50s of 2.8, 2.6, 13 and 58 nM forJAK1,JAK2,JAK3andTyk2, respectively[1].

IC50& Target[1]

JAK1

2.8 nM (IC50)

JAK2

2.6 nM (IC50)

JAK3

13 nM (IC50)

Tyk2

58 nM (IC50)

体外研究
(In Vitro)

In the enzymatic assays, Delgocitinib potently inhibits all of the JAK subtypes with IC50values of 2.8±0.6, 2.6±0.2, 13±0 and 58±9 nM for JAK1, JAK2, JAK3 and Tyk2, respectively. Lineweaver-Burk plots show that the inhibition mode of Delgocitinib toward all JAKs is competitive with ATP with Kivalues of 2.1±0.3, 1.7±0.0, 5.5±0.3 and 14±1 nM for JAK1, JAK2, JAK3 and Tyk2, respectively. In these cell-based cytokine signaling assays, Delgocitinib inhibits the phosphorylation of Stat proteins induced by IL-2, IL-6, IL-23, GM-CSF, and IFN-α with IC50values of 40±9, 33±14, 84±11, 304±22 and 18±3 nM, respectively. Delgocitinib also inhibits IL-2-induced proliferation of T cells in a concentration-dependent manner (IC50=8.9±3.6 nM), and its potency is similar to that of CP-690550 (IC50=16 nM)[1].

体内研究
(In Vivo)

Delgocitinib decreases the IFN-γ production, but the potency of the 1-h prior administration is higher than that of the 6-h prior administration (ED50=0.24 versus 1.3 mg/kg). In the administration from day 1, Delgocitinib prevents the development of hind paw swelling and histological changes of inflammatory cell infiltration and synovial cell hyperplasia. Delgocitinib inhibits radiographic and histological changes of bone destruction and cartilage destruction. In the administration from day 15, Delgocitinib decreases the paw swelling in a dose-dependent manner. In addition, Delgocitinib ameliorates the inflammatory cell infiltration, synovial cell hyperplasia, and cartilage/bone destructions in the histological and radiographic examinations at the end of the study[1].

Clinical Trial
分子量

310.35

性状

Solid

Formula

C16H18N6O

CAS 号

1263774-59-9

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder-20°C3 years
4°C2 years
In solvent-80°C6 months
-20°C1 month
溶解性数据
In Vitro: 

DMSO : ≥ 58 mg/mL(186.89 mM)

*"≥" means soluble, but saturation unknown.

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM3.2222 mL16.1108 mL32.2217 mL
5 mM0.6444 mL3.2222 mL6.4443 mL
10 mM0.3222 mL1.6111 mL3.2222 mL
*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80℃, 6 months; -20℃, 1 month。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 5% DMSO    40%PEG300   5%Tween-80   50% saline

    Solubility: ≥ 2.5 mg/mL (8.06 mM); Clear solution

  • 2.

    请依序添加每种溶剂: 5% DMSO    95% (20%SBE-β-CDin saline)

    Solubility: ≥ 2.5 mg/mL (8.06 mM); Clear solution

  • 3.

    请依序添加每种溶剂: 1% DMSO    99% saline

    Solubility: ≥ 0.5 mg/mL (1.61 mM); Clear solution

*以上所有助溶剂都可在本网站选购。