IDO1/TDO-IN-4|cas:461424-21-5|西域试剂

IDO1/TDO-IN-4,99.23%

产品编号：Bellancom-151108| CAS NO：461424-21-5| 分子式：C₁₄H₁₀N₄| 分子量：234.26

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货号	价格	库存与货期
Bellancom-151108	￥1300.00	杭州北京（现货）
Bellancom-151108	￥2350.00	杭州北京（现货）
Bellancom-151108	￥4200.00	杭州北京（现货）
Bellancom-151108	￥6200.00	杭州北京（现货）
Bellancom-151108	￥9400.00	杭州北京（现货）

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IDO1/TDO-IN-4

产品介绍

IDO1/TDO-IN-4 是一种有效的 IDO1/TDO 双重抑制剂，IC₅₀ 值为 3.53 μM (IDO1) 和 1.15 μM (TDO)。IDO1/TDO-IN-4 可与 IDO1 形成氢键，与 TDO 产生 π-π 堆积相互作用。 IDO1/TDO-IN-4 可用于抑郁症、以及抑郁引起的感染性疾病、代谢性疾病和自身免疫性疾病的研究。

生物活性

IDO1/TDO-IN-4 is a potent IDO1/TDO dual inhibitor, with IC₅₀ values of 3.53 μM (IDO1) and 1.15 μM (TDO). IDO1/TDO-IN-4 forms hydrogen bond with IDO1, and π−π stacking interaction with TDO. IDO1/TDO-IN-4 can be used in the research of depression, and depression-induced infectious, metabolic, and autoimmune disorders.

体外研究

IDO1/TDO-IN-4 (compound 28, 0-2 μM, 1 h) inhibits the LPS-induced activation of BV2 microglial cells (determined by morphological changes).
IDO1/TDO-IN-4 (0-2 μM, 1 h) inhibits the generation of pro-inflammatory factors and promotes the expression of IL-10.
IDO1/TDO-IN-4 (0-2 μM, 1 h) decreases the expression of IDO1 and prevents the excessive degradation of tryptophan via the kynurenine pathway.

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

RT-PCR

Cell Line:	100 ng/mL LPS-induced BV2 microglial cells
Concentration:	0, 0.25, 0.5, 1, 2 μM
Incubation Time:	1 h
Result:	Inhibited the generation of COX2, iNOS, TNF-α, and IL-1β. Increased the level of IL-10.

体内研究
(In Vivo)

IDO1/TDO-IN-4 (compound 28, i.p., 20 mg/kg, at day 1, 2, 3) rescues LPS-induced neuroinflammation and depressive-like behavior in mice.
IDO1/TDO-IN-4 (I.p. or i.v., 20 mg/kg) displays high exposure and a high volume of distribution at the steady state in normal mice.

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

Animal Model:	2 mg/kg LPS-induced depressive mice
Dosage:	20 mg/kg
Administration:	Intraperitoneal injection (i.p.), at day 1, 2, 3.
Result:	Attenuated microglial activation significantly. Decreased inflammatory factors in the hippocampus, such as TNF-α, IL-1β, and iNOS. Downregulated LPS-induced overexpression of IDO1.

Animal Model:

Male C57BL/6J mice (pharmacokinetic assay)

Dosage:

20 mg/kg

Administration:

Intraperitoneal injection and intravenous injection

Result:

Pharmacokinetic profile of IDO1/TDO-IN-4 (compound 28)

pharmacokinetic property	T_1/2 (h)	T_max (h)	C_max (ng/mL)	bioavailability F (%)
i.v./i.p.	2.31/0.77	0.25	5543.99/3878	52.55

体内研究

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

Animal Model:	2 mg/kg LPS-induced depressive mice
Dosage:	20 mg/kg
Administration:	Intraperitoneal injection (i.p.), at day 1, 2, 3.
Result:	Attenuated microglial activation significantly. Decreased inflammatory factors in the hippocampus, such as TNF-α, IL-1β, and iNOS. Downregulated LPS-induced overexpression of IDO1.

Animal Model:

Male C57BL/6J mice (pharmacokinetic assay)

Dosage:

20 mg/kg

Administration:

Intraperitoneal injection and intravenous injection

Result:

Pharmacokinetic profile of IDO1/TDO-IN-4 (compound 28)

pharmacokinetic property	T_1/2 (h)	T_max (h)	C_max (ng/mL)	bioavailability F (%)
i.v./i.p.	2.31/0.77	0.25	5543.99/3878	52.55

体内研究

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

Animal Model:	2 mg/kg LPS-induced depressive mice
Dosage:	20 mg/kg
Administration:	Intraperitoneal injection (i.p.), at day 1, 2, 3.
Result:	Attenuated microglial activation significantly. Decreased inflammatory factors in the hippocampus, such as TNF-α, IL-1β, and iNOS. Downregulated LPS-induced overexpression of IDO1.

Animal Model:

Male C57BL/6J mice (pharmacokinetic assay)

Dosage:

20 mg/kg

Administration:

Intraperitoneal injection and intravenous injection

Result:

Pharmacokinetic profile of IDO1/TDO-IN-4 (compound 28)

pharmacokinetic property	T_1/2 (h)	T_max (h)	C_max (ng/mL)	bioavailability F (%)
i.v./i.p.	2.31/0.77	0.25	5543.99/3878	52.55

性状

Solid

溶解性数据

In Vitro:

DMSO : 125 mg/mL (533.60 mM; ultrasonic and warming and heat to 60°C)

Methanol : 16.67 mg/mL (71.16 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	4.2688 mL	21.3438 mL	42.6876 mL
5 mM	0.8538 mL	4.2688 mL	8.5375 mL
10 mM	0.4269 mL	2.1344 mL	4.2688 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 90% (20% SBE-β-CD in saline)
Solubility: 2.08 mg/mL (8.88 mM); Suspended solution; Need ultrasonic

此方案可获得 2.08 mg/mL (8.88 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 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