C25-140|cas:1358099-18-9|西域试剂

C25-140,99.84%

产品编号：Bellancom-120934| CAS NO：1358099-18-9| 分子式：C₂₆H₃₁N₇O| 分子量：457.57

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-120934	￥2100.00	杭州北京（现货）
Bellancom-120934	￥3500.00	杭州北京（现货）
Bellancom-120934	￥12500.00	杭州北京（现货）
Bellancom-120934	￥0.00	杭州北京（现货）

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C25-140

产品介绍

C25-140 是一种首创的，具有口服活性和一定选择性的 TRAF6-Ubc13 相互作用的抑制剂，直接与 TRAF6 结合，阻断 TRAF6 和 Ubc13 的相互作用，从而降低 TRAF6 活性，降低 NF-κB 的活性，并对抗自身免疫。

生物活性

C25-140, a first-in-class, orally active, and fairly selective TRAF6-Ubc13 inhibitor, directly binds to TRAF6, and blocks the interaction of TRAF6 with Ubc13. C25-140 lowers TRAF6 activity, reduces NF-κB activation, and combats autoimmunity.

体外研究

C25-140 dose-dependently impedes TRAF6-Ubc13 interaction.
C25-140 (10-30 μM; 2 hours) effectively reduces TRAF6-mediated ubiquitin chain formation.
C25-140 affects TNFα-induced phosphorylation of IκBα as well as NF-κB-induced target gene expression.
C25-140 efficiently inhibits IL-1β- and TNFα-mediated receptor signaling in the context of cytokine activation.

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

Western Blot Analysis

Cell Line:	TRAF6_WT
Concentration:	10 μM, 20 μM, 30 μM
Incubation Time:	2 hours
Result:	Effectively reduced TRAF6-mediated ubiquitin chain formation.

体内研究
(In Vivo)

C25-140 (~1.5 mg/kg; topically to the shaved back and the right ear; twice daily for 6 days) ameliorates symptoms of autoimmune psoriasis in R 837-induced psoriasis mouse model.
C25-140 (6-14 mg/kg; given i.p.; twice daily for 14 days) shows a dose-dependent improvement of RA disease outcome in Collagen-induced arthritis (CIA) model.
C25-140 (10 mg/kg; i.v.) treatment shows that the C_max, AUC, t_1/2 and V_d are 9.7 μg/mL, 274083 ng min/mL, 80.62 min, and 4.13 L/kg, respectively.
. C25-140 (10 mg/kg; p.o.) treatment shows that the C_max, AUC, t_1/2 and V_d are 3.4 μg/mL, 124034 ng min/mL, 127.33 min and 13.3 L/kg, respectively.
C25-140 (10 mg/kg; i.p.) treatment shows that the C_max, AUC, t_1/2 and V_d are 4.2μg/mL, 100000 ng min/mL, 184 min, 25.6 L/kg, respectively.

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

Animal Model:	R 837-induced psoriasis mouse model (male BALB/c mice)
Dosage:	~1.5 mg/kg
Administration:	Topically to the shaved back and the right ear; twice daily for 6 days
Result:	Showed a dose-dependent improvement of RA disease outcome.

Animal Model:	Collagen-induced arthritis (CIA) model in DBA1/J mice
Dosage:	6 mg/kg, 10 mg/kg, 14 mg/kg
Administration:	Given i.p.; twice daily for 14 days
Result:	Ameliorated the arthritic index to almost baseline levels in this efficacy model at doses of 10 and 14 mg/kg. Dose-dependently improved symptoms of RA including inflammation and structural damage.

Animal Model:	BALB/C mice
Dosage:	10 mg/kg
Administration:	I.v. (Pharmacokinetic Analysis)
Result:	The C_max, AUC, t_1/2 and V_d were 9.7 μg/mL, 274083 ng min/mL, 80.62 min, and 4.13 L/kg, respectively.

体内研究

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

Animal Model:	R 837-induced psoriasis mouse model (male BALB/c mice)
Dosage:	~1.5 mg/kg
Administration:	Topically to the shaved back and the right ear; twice daily for 6 days
Result:	Showed a dose-dependent improvement of RA disease outcome.

Animal Model:	Collagen-induced arthritis (CIA) model in DBA1/J mice
Dosage:	6 mg/kg, 10 mg/kg, 14 mg/kg
Administration:	Given i.p.; twice daily for 14 days
Result:	Ameliorated the arthritic index to almost baseline levels in this efficacy model at doses of 10 and 14 mg/kg. Dose-dependently improved symptoms of RA including inflammation and structural damage.

Animal Model:	BALB/C mice
Dosage:	10 mg/kg
Administration:	I.v. (Pharmacokinetic Analysis)
Result:	The C_max, AUC, t_1/2 and V_d were 9.7 μg/mL, 274083 ng min/mL, 80.62 min, and 4.13 L/kg, respectively.

体内研究

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

Animal Model:	R 837-induced psoriasis mouse model (male BALB/c mice)
Dosage:	~1.5 mg/kg
Administration:	Topically to the shaved back and the right ear; twice daily for 6 days
Result:	Showed a dose-dependent improvement of RA disease outcome.

Animal Model:	Collagen-induced arthritis (CIA) model in DBA1/J mice
Dosage:	6 mg/kg, 10 mg/kg, 14 mg/kg
Administration:	Given i.p.; twice daily for 14 days
Result:	Ameliorated the arthritic index to almost baseline levels in this efficacy model at doses of 10 and 14 mg/kg. Dose-dependently improved symptoms of RA including inflammation and structural damage.

Animal Model:	BALB/C mice
Dosage:	10 mg/kg
Administration:	I.v. (Pharmacokinetic Analysis)
Result:	The C_max, AUC, t_1/2 and V_d were 9.7 μg/mL, 274083 ng min/mL, 80.62 min, and 4.13 L/kg, respectively.

性状

Solid

溶解性数据

In Vitro:

DMSO : 41.67 mg/mL (91.07 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.1855 mL	10.9273 mL	21.8546 mL
5 mM	0.4371 mL	2.1855 mL	4.3709 mL
10 mM	0.2185 mL	1.0927 mL	2.1855 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: ≥ 2.08 mg/mL (4.55 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (4.55 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 (4.55 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (4.55 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 (4.55 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (4.55 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。