Delgocitinib JTE-052|cas:1263774-59-9|西域试剂

Delgocitinib JTE-052,99.76%

产品编号：Bellancom-109053| CAS NO：1263774-59-9| 分子式：C₁₆H₁₈N₆O| 分子量：310.35

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货号	价格	库存与货期
Bellancom-109053	￥1840.00	杭州北京（现货）
Bellancom-109053	￥5510.00	杭州北京（现货）
Bellancom-109053	￥9120.00	杭州北京（现货）
Bellancom-109053	￥16720.00	杭州北京（现货）
Bellancom-109053	￥26750.00	杭州北京（现货）

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Delgocitinib 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 specific JAK inhibitor with IC₅₀s of 2.8, 2.6, 13 and 58 nM for JAK1, JAK2, JAK3 and Tyk2, respectively.

体外研究

In the enzymatic assays, Delgocitinib potently inhibits all of the JAK subtypes with IC₅₀ values 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 K_i values 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 IC₅₀ values 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).

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究

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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

性状

Solid

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 mg	5 mg	10 mg

1 mM	3.2222 mL	16.1108 mL	32.2217 mL
5 mM	0.6444 mL	3.2222 mL	6.4443 mL
10 mM	0.3222 mL	1.6111 mL	3.2222 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°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 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-CD in 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