YM-341619 AS1617612|cas:643082-52-4|西域试剂

YM-341619 AS1617612,99.06%

产品编号：Bellancom-134771| CAS NO：643082-52-4| 分子式：C₂₂H₂₁F₃N₆O₂| 分子量：458.44

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货号	包装	价格	库存与货期	购买量	操作
Bellancom-134771		￥8200.00	杭州北京（现货）
Bellancom-134771		￥13000.00	杭州北京（现货）

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YM-341619 AS1617612

产品介绍

YM-341619 (AS1617612) 是一种有效的口服 STAT6 抑制剂，IC₅₀ 为 0.70 nM。YM-341619 可抑制 IL-4 诱导的小鼠脾脏 T 细胞 Th2 分化 (IC₅₀=0.28 nM)，但不影响 Th1 细胞的分化。YM-341619 是一种很有希望的化合物，可用于过敏性疾病研究的化合物，如过敏性哮喘。

生物活性

YM-341619 (AS1617612) is a potent and orally active STAT6 inhibitor with an IC₅₀ of 0.70 nM. YM-341619 inhibits Th2 differentiation in mouse spleen T cells induced by IL-4 (IC₅₀=0.28 nM) without affecting Th1 cell differentiation. YM-341619 is a promising compound for the the research of allergic diseases, such as allergic asthma.

体外研究

YM-341619 (0.1-100 nM; pretreatment 30 min before IL-4) inhibits IL-4-increased STAT6 luciferase gene activity in a concentration dependent manner, exhibiting an IC₅₀ value of 1.5 nM in FW4 cells.
YM-341619 (0.1-10 nM; pretreatment 30 min before IL-4) concentration-dependently decreases the production of IL-4 and the expression of GATA-3 mRNA in T cells cultured with IL-4. And it has no effects on the production of IFN-γ or the expression of T-bet (a Th1 transcription factor) mRNA in T cells cultured with IL-12.

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

RT-PCR

Cell Line:	T cells
Concentration:	0.1 nM, 1 nM, 10 nM
Incubation Time:	Pretreatment 30 min before IL-4, then IL-4 treated for 16 hours
Result:	Decreased IL-4 and GATA-3 mRNA expression.

体内研究
(In Vivo)

YM-341619 (intravenous injection; 1 mg/kg) exhibits CL_tot, t_1/2, V_d values of 36.1 mL/min/kg, 1.0 hour, 3117 mL/kg, respectively. And it exhibits C_max, T_max, AUC, and F% values of 80 ng/mL, 0.5h, 114 ng h/mL and 25%, respectively in 8-week-old female balb/c mice.
YM-341619 (oral administration; 0.003-0.03 mg/kg) suppresses the IgE level in a dose-dependent manner, but not the IgG2a level, and the ED₅₀ value of YM-341619 for the suppression of IgE production is 0.026 mg/kg. YM-341619 tends to decrease IL-4 production and decrease IL-13 production in a dose-dependent manner (both 57%), but does not affect IFN-γ production in DNP-Ascaris-sensitized rats.

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

Animal Model:	DNP-Ascaris-sensitized rats
Dosage:	0.003-0.03 mg/kg
Administration:	Oral administration; 0.003-0.03 mg/kg
Result:	Suppressed IL-4 and IL-13 production in splenocytes derived from DNP-ascaris-sensitized rats without reducing IFN-γ production.

体内研究

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

Animal Model:	DNP-Ascaris-sensitized rats
Dosage:	0.003-0.03 mg/kg
Administration:	Oral administration; 0.003-0.03 mg/kg
Result:	Suppressed IL-4 and IL-13 production in splenocytes derived from DNP-ascaris-sensitized rats without reducing IFN-γ production.

体内研究

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

Animal Model:	DNP-Ascaris-sensitized rats
Dosage:	0.003-0.03 mg/kg
Administration:	Oral administration; 0.003-0.03 mg/kg
Result:	Suppressed IL-4 and IL-13 production in splenocytes derived from DNP-ascaris-sensitized rats without reducing IFN-γ production.

性状

Solid

溶解性数据

In Vitro:

DMSO : 50 mg/mL (109.07 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	2.1813 mL	10.9066 mL	21.8131 mL
5 mM	0.4363 mL	2.1813 mL	4.3626 mL
10 mM	0.2181 mL	1.0907 mL	2.1813 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: 2.5 mg/mL (5.45 mM); Suspended solution; Need ultrasonic

此方案可获得 2.5 mg/mL (5.45 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。
以 1 mL 工作液为例，取 100 μL 25.0 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: ≥ 2.5 mg/mL (5.45 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.45 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 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: ≥ 2.5 mg/mL (5.45 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.45 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 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。