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DDD85646

Name: DDD85646
Brand: TargetMol
SKU: T27135
Price: 927 CNY
Availability: InStock
Rating: 5 (10 reviews)

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很棒

纯度: 99.76%

货号 T27135Cas号 1215010-55-1

别名 DDD-85646, DDD 85646

DDD85646 是 T. brucei N-myristoyltransferase 的抑制剂，Ki 为 1.44 nM，IC50 为 2 nM，EC50 为 2 nM。 hNMT 的 IC50 为 4 nM。

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DDD85646

一键复制产品信息

很棒

纯度: 99.76%

货号 T27135 别名 DDD-85646, DDD 85646Cas号 1215010-55-1

DDD85646 是 T. brucei N-myristoyltransferase 的抑制剂，Ki 为 1.44 nM，IC50 为 2 nM，EC50 为 2 nM。 hNMT 的 IC50 为 4 nM。

规格	价格	库存
1 mg	¥ 927	现货
5 mg	¥ 2,650	现货
10 mg	¥ 3,960	现货
25 mg	¥ 6,250	现货
50 mg	¥ 8,430	现货
100 mg	¥ 11,300	现货
200 mg	¥ 15,300	现货
1 mL x 10 mM (in DMSO)	¥ 2,890	现货

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产品介绍

DDD85646 AI Summary

DDD85646 exhibits potent inhibitory activity against N-myristoyltransferases from Trypanosoma brucei, Leishmania major, and Trypanosoma cruzi with IC50 values ranging from 2.0 to 3.0 nM. It also effectively inhibits human N-myristoyltransferase 1 and 2 with similar IC50 values. The compound has demonstrated strong antitrypanosomal activity with EC50 values down to 2.0 nM against Trypanosoma brucei BSF427 expressing VSG118, as well as significant efficacy in Trypanosoma brucei brucei s427 and Trypanosoma brucei rhodesiense infected mouse models with median effective doses (MED) of 12.5 and 50.0 mg/kg, respectively. Additionally, DDD85646 shows anti-leishmanial activity against Leishmania infantum and anti-trypanosomal activity against Trypanosoma cruzi. It also displays antimicrobial activity, cytotoxicity towards human MRC5 cells with an EC50 of 300.0 nM, and exhibits a moderate oral bioavailability of 19-20% in NMRI mice. Pharmacokinetic properties in mice include low blood clearance and volume of distribution, short half-life, and a brain-to-blood ratio of less than 0.1. The compound shows low inhibition of cytochrome P450 enzymes and human ERG at 1 uM, with inhibition levels below or equal to 10.0%, indicating minimal off-target effects. DDD85646 has a maximal tolerated dose of 100.0 mg/kg in orally twice-daily dosed mice and demonstrates moderate to low cytotoxicity against various cell lines, indicating a broad therapeutic potential..

Note: Summary generated by AI. Data source: ChEMBL

生物活性

产品描述	DDD85646 is an inhibitor of T. brucei N-myristoyltransferase with a Ki of 1.44 nM, an IC50 of 2 nM and an EC50 of 2 nM. The IC50 of hNMT is 4 nM.
靶点活性	NMT:1.44 nM(Ki, T. brucei), NMT:2 nM(EC50, T. brucei), NMT:2 nM(T. brucei), NMT:4 nM(human)
别名	DDD-85646, DDD 85646

化学信息

分子量	495.43
分子式	C₂₁H₂₄Cl₂N₆O₂S
CAS No.	1215010-55-1
Smiles	Cc1nn(C)c(C)c1NS(=O)(=O)c1c(Cl)cc(cc1Cl)-c1ccnc(c1)N1CCNCC1
密度	1.48 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: 95 mg/mL (191.75 mM), Sonication is recommended.

体内实验配方

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 3.3 mg/mL (6.66 mM), Sonication is recommended.

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	2.0184 mL	10.0922 mL	20.1845 mL	100.9224 mL
5 mM	0.4037 mL	2.0184 mL	4.0369 mL	20.1845 mL
10 mM	0.2018 mL	1.0092 mL	2.0184 mL	10.0922 mL
20 mM	0.1009 mL	0.5046 mL	1.0092 mL	5.0461 mL
50 mM	0.0404 mL	0.2018 mL	0.4037 mL	2.0184 mL
100 mM	0.0202 mL	0.1009 mL	0.2018 mL	1.0092 mL