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T863

Name: T863
Brand: TargetMol
SKU: T4681
Price: 322 CNY
Availability: InStock
Rating: 5 (10 reviews)

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很棒

纯度: 99.88%

货号 T4681Cas号 701232-20-4

别名 DGAT-3, DGAT-1 inhibitor

T863 (DGAT-3) 是口服有效的二酰基甘油酰基转移酶1 选择性抑制剂。T863结合DGAT1的酰基辅酶A 结合位点，抑制三酰甘油在细胞内的合成。

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T863

一键复制产品信息

很棒

纯度: 99.88%

货号 T4681 别名 DGAT-3, DGAT-1 inhibitorCas号 701232-20-4

T863 (DGAT-3) 是口服有效的二酰基甘油酰基转移酶1 选择性抑制剂。T863结合DGAT1的酰基辅酶A 结合位点，抑制三酰甘油在细胞内的合成。

规格	价格	库存
1 mg	¥ 322	现货
2 mg	¥ 449	现货
5 mg	¥ 712	现货
10 mg	¥ 1,230	现货
25 mg	¥ 2,430	现货
50 mg	¥ 3,590	现货
100 mg	¥ 5,120	现货
200 mg	¥ 7,250	现货
1 mL x 10 mM (in DMSO)	¥ 617	现货

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纯度: 98.66%

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COA LCMS HNMR 产品操作手册

产品介绍

T863 AI Summary

T863 inhibits human recombinant DGAT1 with an IC50 of 15.0 nM and rat microsomal DGAT1 with an IC50 of 19.0 nM. It effectively inhibits triacylglycerol synthesis in human HuTu 80 cells with an IC50 of 4.0 nM and in HT-29 cells with an IC50 of 8.0 nM. It shows low inhibitory activity on human DGAT2 and moderate inhibition of human ACAT1 with an IC50 of 12000.0 nM. Pharmacokinetic studies reveal that T863 has high oral bioavailability (>100%) in rats and dogs with moderate to low clearance rates and varying half-lives. In human liver microsomes, it has an apparent clearance of less than 8.0 mL.min-1.kg-1. The compound demonstrates 100% inhibition of plasma triglyceride accumulation at 10 mg/kg in Sprague-Dawley rats and shows significant reductions in plasma triglyceride levels in other animal models. T863 also displays a favorable distribution coefficient (LogD7.4 = 1.32) and good solubility in pH 7.4 buffer. Additionally, it shows potential anti-viral activity by inhibiting SARS-CoV-2 protease activity at 20 µM and demonstrates cell type-dependent effects on cell growth rates and protein stability. However, at high doses, it exhibits toxicity, such as body weight loss in mice and elevated liver enzyme levels in cynomolgus monkeys..

Note: Summary generated by AI. Data source: ChEMBL

生物活性

产品描述	T-863(DGAT-1 inhibitor) is an orally active, selective and potent DGAT1 (Acyl-CoA:diacylglycerol acyltransferase 1) inhibitor that interacts with the acyl-CoA binding site of DGAT1, and inhibits triacylglycerol synthesis in cells. IC50 value: Target: DGAT1 T863 (DGAT-3) causes weight loss, reduction in serum and liver triglycerides, and improved insulin sensitivity in obese mice.
别名	DGAT-3, DGAT-1 inhibitor

化学信息

分子量	394.47
分子式	C₂₂H₂₆N₄O₃
CAS No.	701232-20-4
Smiles	CC1(C)Oc2ncnc(N)c2N=C1c1ccc(cc1)[C@H]1CC[C@H](CC(O)=O)CC1
密度	1.36 g/cm3 (Predicted)

储存&溶解度

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

溶解度信息

DMSO: 41.67 mg/mL (105.64 mM), Sonication is recommended.

体内实验配方

10% DMSO+90% Corn Oil: 2 mg/mL (5.07 mM), Sonication is recommeded.

请按顺序添加溶剂，在添加下一种溶剂之前，尽可能使溶液澄清。如有必要，可通过加热、超声、涡旋处理进行溶解。工作液建议现配现用。以上配方仅供参考，体内配方并不是绝对的，请根据不同情况进行调整。

溶液配制表

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.5350 mL	12.6752 mL	25.3505 mL	126.7524 mL
5 mM	0.5070 mL	2.5350 mL	5.0701 mL	25.3505 mL
10 mM	0.2535 mL	1.2675 mL	2.5350 mL	12.6752 mL
20 mM	0.1268 mL	0.6338 mL	1.2675 mL	6.3376 mL
50 mM	0.0507 mL	0.2535 mL	0.5070 mL	2.5350 mL
100 mM	0.0254 mL	0.1268 mL	0.2535 mL	1.2675 mL