TM-25659|cas:260553-97-7|西域试剂

TM-25659,99.65%

产品编号：Bellancom-112920| CAS NO：260553-97-7| 分子式：C₃₀H₂₈N₈| 分子量：500.60

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货号	价格	库存与货期
Bellancom-112920	￥1600.00	杭州北京（现货）
Bellancom-112920	￥2500.00	杭州北京（现货）
Bellancom-112920	￥5700.00	杭州北京（现货）
Bellancom-112920	￥9800.00	杭州北京（现货）

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TM-25659

产品介绍

TM-25659是 具有PDZ结合基序的转录共激活子 (TAZ) 的调制剂。抗骨质疏松和抗肥胖活性。

生物活性

TM-25659 is a transcriptional co-activator with PDZ-binding motif (TAZ) modulator. Anti-osteoporotic and anti-obesity activities.

体外研究

TM-25659 (2, 10, 20, 100 μM) enhances nuclear TAZ localization in a dose-dependent manner and attenuates PPARγ-mediated adipocyte differentiation by facilitating PPARγ suppression activity of TAZ.

TM-25659 (2, 10, 50 μM) enhances osteogenic gene expression and thereby increases osteoblast differentiation.

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

Cell Proliferation Assay

Cell Line:	3T3-L1 cells
Concentration:	2, 10, 20, 100 μM
Incubation Time:	6 days
Result:	Acted as a suppressor of PPARγ-dependent adipocyte differentiation.

体内研究
(In Vivo)

TM-25659 (50 mg/kg, i.p., every other day for 2 weeks) suppresses bone loss in vivo and decreases weight gain in an obesity model.

TM-25659 has a favourable pharmacokinetic profile in rats. The plasma concentration of TM-25659 declines with an approximate t_1/2 of 7 or 10 h following i.v or p.o. administration respectively. The systemic clearance (CL) is 0.21 L×h^-1×kg^-1 and the volume of distribution at steady-state (1.91 L×h^-1×kg^-1) is larger than the volume of total body fluids.

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

Animal Model:	C57BL6 mice (4- to 6-week-old )
Dosage:	50 mg/kg
Administration:	I.p., every other day for 2 weeks
Result:	Attenuated weight gain in these obese mice.

Animal Model:	Adult male Sprague-Dawley rats
Dosage:	10 mg/kg
Administration:	I.v. (2, 10 and 30 min), oral (15 and 30 min, and 1, 2, 4 and 8 h)
Result:	Oral administration for 4 weeks moderately but significantly attenuated weight gain and partly restored BMD in the OVX rats.

体内研究

TM-25659 (50 mg/kg, i.p., every other day for 2 weeks) suppresses bone loss in vivo and decreases weight gain in an obesity model.

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

Animal Model:	C57BL6 mice (4- to 6-week-old )
Dosage:	50 mg/kg
Administration:	I.p., every other day for 2 weeks
Result:	Attenuated weight gain in these obese mice.

Animal Model:	Adult male Sprague-Dawley rats
Dosage:	10 mg/kg
Administration:	I.v. (2, 10 and 30 min), oral (15 and 30 min, and 1, 2, 4 and 8 h)
Result:	Oral administration for 4 weeks moderately but significantly attenuated weight gain and partly restored BMD in the OVX rats.

体内研究

TM-25659 (50 mg/kg, i.p., every other day for 2 weeks) suppresses bone loss in vivo and decreases weight gain in an obesity model.

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

Animal Model:	C57BL6 mice (4- to 6-week-old )
Dosage:	50 mg/kg
Administration:	I.p., every other day for 2 weeks
Result:	Attenuated weight gain in these obese mice.

Animal Model:	Adult male Sprague-Dawley rats
Dosage:	10 mg/kg
Administration:	I.v. (2, 10 and 30 min), oral (15 and 30 min, and 1, 2, 4 and 8 h)
Result:	Oral administration for 4 weeks moderately but significantly attenuated weight gain and partly restored BMD in the OVX rats.

性状

Solid

溶解性数据

In Vitro:

DMSO : ≥ 135 mg/mL (269.68 mM)

* "≥" means soluble, but saturation unknown.

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.9976 mL	9.9880 mL	19.9760 mL
5 mM	0.3995 mL	1.9976 mL	3.9952 mL
10 mM	0.1998 mL	0.9988 mL	1.9976 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: ≥ 2.25 mg/mL (4.49 mM); Clear solution

此方案可获得 ≥ 2.25 mg/mL (4.49 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 22.5 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: 2.25 mg/mL (4.49 mM); Suspended solution; Need ultrasonic

此方案可获得 2.25 mg/mL (4.49 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 22.5 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: ≥ 2.25 mg/mL (4.49 mM); Clear solution

此方案可获得 ≥ 2.25 mg/mL (4.49 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 22.5 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。