Tyk2-IN-5|cas:1797432-62-2|西域试剂

Tyk2-IN-5,98.87%

产品编号：Bellancom-111745| CAS NO：1797432-62-2| 分子式：C₂₁H₁₉FN₈O₂| 分子量：434.43

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用，

货号	价格	库存与货期
Bellancom-111745	￥4500.00	杭州北京（现货）
Bellancom-111745	￥7500.00	杭州北京（现货）
Bellancom-111745	￥15000.00	杭州北京（现货）
Bellancom-111745	￥22500.00	杭州北京（现货）
Bellancom-111745	￥33500.00	杭州北京（现货）

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Tyk2-IN-5

产品介绍

Tyk2-IN-5 (compound 6) 是一种强效的、具有选择性和口服活性的酪氨酸激酶 2 (Tyk2) 抑制剂，作用于 JH2 结构域。Tyk2-IN-5 对 Tyk2 JH2 的 K_i 值为 0.086 nM，对 IFNα 的 IC₅₀ 值为 25 nM。Tyk2-IN-5 能高效地抑制药效学大鼠模型中 IFNγ 的产生，对大鼠关节炎模型具有完全的疗效。

生物活性

Tyk2-IN-5 (compound 6) is a potent, selective and orally active tyrosine kinase 2 (Tyk2) inhibitor that acts on the JH2 structural domain. Tyk2-IN-5 shows a K_i value of 0.086 nM for Tyk2 JH2 and an IC₅₀ value of 25 nM for IFNα. Tyk2-IN-5 efficiently inhibits the production of IFNγ in a pharmacodynamic rat model and is fully efficacious in a rat model of arthritis.

体外研究

Tyk2-IN-5 inhibits Jak1-3 with IC₅₀ values of >2 μM and displays the Jak1-3 dependent cellular activities of >12.5 μM (IC₅₀ values).

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

体内研究

Tyk2-IN-5 (5, 10 mg/kg; p.o.; twice daily for 20 days) shows highly efficacious in a rat adjuvant arthritis model.
Tyk2-IN-5 (1, 10 mg/kg; p.o.; single) inhibits IL-12/IL-18 induced IFNγ production in a dose-dependent manner.
Tyk2-IN-5 (10 mg/kg; p.o.; single) shows a high oral exposure and bioavailability (114%) in rat.

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

Animal Model:	Lewis male rats (rat adjuvant arthritis model).
Dosage:	5, 10 mg/kg
Administration:	Oral administration; twice daily for 20 days
Result:	Demonstrated full efficacy to prevent the rats′ paw from swelling.

Animal Model:	Lewis male rats (IL-12/IL-18-induced).
Dosage:	1, 10 mg/kg
Administration:	Oral administration; single
Result:	Inhibited IL-12/IL-18 induced IFNγ production by 45% and 77% at doses of 1 and 10 mg/kg, respectively.

Animal Model:

Lewis male rats, mouse.

Dosage:

10 mg/kg

Administration:

Oral administration; single

Result:

1.19 Pharmacokinetic Parameters of Tyk2-IN-5 in mouse and rat.

	PO (10 mg/kg)
	mouse	rat
C_max (μM)	15	9.4
AUC_0-24 (μM•h)	19	57
CL (mL/min/kg)	16	7.8
F (%)	86	114

体内研究

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

Animal Model:	Lewis male rats (rat adjuvant arthritis model).
Dosage:	5, 10 mg/kg
Administration:	Oral administration; twice daily for 20 days
Result:	Demonstrated full efficacy to prevent the rats′ paw from swelling.

Animal Model:	Lewis male rats (IL-12/IL-18-induced).
Dosage:	1, 10 mg/kg
Administration:	Oral administration; single
Result:	Inhibited IL-12/IL-18 induced IFNγ production by 45% and 77% at doses of 1 and 10 mg/kg, respectively.

Animal Model:

Lewis male rats, mouse.

Dosage:

10 mg/kg

Administration:

Oral administration; single

Result:

1.19 Pharmacokinetic Parameters of Tyk2-IN-5 in mouse and rat.

	PO (10 mg/kg)
	mouse	rat
C_max (μM)	15	9.4
AUC_0-24 (μM•h)	19	57
CL (mL/min/kg)	16	7.8
F (%)	86	114

性状

Solid

溶解性数据

In Vitro:

DMSO : 43.33 mg/mL (99.74 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.3019 mL	11.5093 mL	23.0187 mL
5 mM	0.4604 mL	2.3019 mL	4.6037 mL
10 mM	0.2302 mL	1.1509 mL	2.3019 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： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.17 mg/mL (5.00 mM); Clear solution

此方案可获得 ≥ 2.17 mg/mL (5.00 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 21.7 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