Brepocitinib P-Tosylate PF-06700841 P-Tosylate|cas:2140301-96-6|西域试剂

Brepocitinib P-Tosylate PF-06700841 P-Tosylate,99.86%

产品编号：Bellancom-112708A| CAS NO：2140301-96-6| 分子式：C₂₅H₂₉F₂N₇O₄S| 分子量：561.60

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货号	价格	库存与货期
Bellancom-112708A	￥990.00	杭州北京（现货）
Bellancom-112708A	￥1700.00	杭州北京（现货）
Bellancom-112708A	￥6600.00	杭州北京（现货）
Bellancom-112708A	￥11500.00	杭州北京（现货）

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Brepocitinib P-Tosylate PF-06700841 P-Tosylate

产品介绍

Brepocitinib (PF-06700841) P-Tosylate 是一种有效的 JAK1 和 TYK2 双重抑制剂， IC₅₀ 值分别为 17 nM 和 23 nM。Brepocitinib P-Tosylate 还分别以 IC₅₀值为 77 nM 和 6.49 μM 抑制 JAK2和 JAK3。

生物活性

Brepocitinib (PF-06700841) P-Tosylate is a potent dual Janus kinase 1 (JAK1) and TYK2 inhibitor with IC₅₀s of 17 nM and 23 nM, respectively. Brepocitinib P-Tosylate also inhibits JAK2 and JAK3 with IC₅₀s of 77 nM and 6.49 μM, respectively.

体外研究

Brepocitinib (Compound 23) potently inhibits TYK2/JAK2 mediated IL-12/pSTAT4 and IL-23/pSTAT3 (human whole blood (HWB) IC₅₀s of 65 and 120 nM, respectively). Brepocitinib has good potency against IL6/pStat1 in the CD3⁺ cellular subset (IC₅₀ of 81 nM), but lower inhibition of IL6/pSTAT3, again in the CD3⁺ cellular subset (IC₅₀ of 641 nM). Brepocitinib also inhibits the JAK1/JAK3 driven γ-common chain cytokines, represented by IL-15/pStat5 and IL-21/pSTAT3 with reasonable potency (HWB IC₅₀s of 238 and 204 nM, respectively). Brepocitinib inhibits EPO/pSTAT5 (JAK2 homodimer) in HWB spiked with CD34⁺ progenitor cells (IC₅₀ of 577 nM). IL10/pSTAT3 (TYK2/JAK1) and IL27/pSTAT3 (JAK1/JAK2/TYK2) are also inhibited by Brepocitinib with IC₅₀s of 305 nM and 86 nM, respectively.

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

体内研究

Brepocitinib (Compound 23; 3-30 mg/kg; oral administration; for 7 consecutive days; female Lewis rats) treatment significantly reduces paw volume increase in a dose-dependent manner. The plasma concentrations in animals dosed with Brepocitinib at peak (30 min) and trough (24 h) time intervals post final dose respectively are as follows: 3 mg/kg, 3.54 μM, 0.0221 μM; 10 mg/kg, 10.95 μM, 0.06 μM; and 30 mg/kg, 23.89 μM, 0.06 μM.

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

Animal Model:	Female Lewis rats with induced arthritis
Dosage:	3 mg/kg, 10 mg/kg, or 30 mg/kg
Administration:	Oral administration; for 7 consecutive days
Result:	Increased in paw volume was significantly lower and dose-dependent.

体内研究

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

Animal Model:	Female Lewis rats with induced arthritis
Dosage:	3 mg/kg, 10 mg/kg, or 30 mg/kg
Administration:	Oral administration; for 7 consecutive days
Result:	Increased in paw volume was significantly lower and dose-dependent.

性状

Solid

溶解性数据

In Vitro:

DMSO : 50 mg/mL (89.03 mM; ultrasonic and warming and heat to 60°C)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.7806 mL	8.9031 mL	17.8063 mL
5 mM	0.3561 mL	1.7806 mL	3.5613 mL
10 mM	0.1781 mL	0.8903 mL	1.7806 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 (sealed storage, away from moisture)。-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： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.08 mg/mL (3.70 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (3.70 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.08 mg/mL (3.70 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (3.70 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.08 mg/mL (3.70 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (3.70 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。