LDC4297|cas:1453834-21-3|西域试剂

LDC4297,98.25%

产品编号：Bellancom-12653| CAS NO：1453834-21-3| 分子式：C₂₃H₂₈N₈O| 分子量：432.52

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-12653	￥850.00	杭州北京（现货）
Bellancom-12653	￥1440.00	杭州北京（现货）
Bellancom-12653	￥3000.00	杭州北京（现货）
Bellancom-12653	￥5000.00	杭州北京（现货）

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LDC4297

产品介绍

LDC4297 是 CDK7 的选择性抑制剂，IC₅₀ 值为 0.13 nM。LDC4297 抑制人巨细胞病毒 (HCMV) 复制，EC₅₀ 值为 24.5 nM。LDC4297 具有广谱的抗病毒活性，对疱疹病毒，腺病毒，痘病毒，逆转录病毒和正粘病毒的 EC₅₀ 值为 0.02-1.21 μM。LDC4297 可用于感染的研究。

生物活性

LDC4297 is a selective inhibitor of CDK7 with an IC₅₀ value of 0.13 nM. LDC4297 inhibits human cytomegalovirus (HCMV) replication with an EC₅₀ value of 24.5 nM. LDC4297 shows broad antiviral activities to Herpesviridae, Adenoviridae, Poxviridae, Retroviridae and Orthomyxoviridae with EC₅₀ value of 0.02-1.21 μM. LDC4297 can be used for the research of infection.

体外研究

LDC4297 (0-10 μM; 6 d) dose-dependently inhibits HCMV replication with an EC₅₀ value of 24.5 nM.
LDC4297 (0-10 μM; 4 d) shows anti-proliferative activity to primary cultures of fibroblasts derived from human (HFF) with a GI₅₀ value of 4.5 μM.
LDC4297 (20 μM; 12-96 h) shows anti-HCMV activity through a multifaceted mode of action that involves an interference with virus-induced Rb phosphorylation.
LDC4297 (0-10 μM; 7 d) shows broad antiviral activities to HCMV, GPCMV, MCMV, HVV-6A, HSV-1, HSV-2, VZV, EBV, HAdV-2, Vaccinia virus, HIV-1 (nl4-3), HIV-1 (4LIG7) and Influenza A virus with EC₅₀ values of 0.02, 0.05, 0.07, 0.04, 0.02, 0.27, 0.06, 1.21, 0.25, 0.77, 1.04, 1.13 and 0.99 μM, respectively.

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

Western Blot Analysis

Cell Line:	Primary cultures of fibroblasts derived from human (HFF) with virus infection
Concentration:	20 μM
Incubation Time:	12, 24, 48 and 96 hours
Result:	Showed inhibitory effect towards viral protein synthesis at the stage of immediate early (IE) gene expression and the drug-mediated reduction of IE1p72 levels partially recovered over time. Exerted an inhibitory effect on human cytomegalovirus (HCMV) induced an up-regulation of protein expression or protein phosphorylation, and reduced Rb expression in the uninfected control cells at 24 h.

体内研究
(In Vivo)

LDC4297 (100 mg/kg; p.o. once) shows promising pharmacokinetic analyses.

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

Animal Model:	CD1 mice
Dosage:	100 mg/kg
Administration:	Oral gavage; 100 mg/kg once
Result:	Showed a half-life of 1.6 h, and the time to a mean peak plasma concentration of 1,297.6 ng/mL is reached 0.5 h after administration with a continued presence in plasma for at least 8 h and a bioavailability of 97.7%.

体内研究

LDC4297 (100 mg/kg; p.o. once) shows promising pharmacokinetic analyses.

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

Animal Model:	CD1 mice
Dosage:	100 mg/kg
Administration:	Oral gavage; 100 mg/kg once
Result:	Showed a half-life of 1.6 h, and the time to a mean peak plasma concentration of 1,297.6 ng/mL is reached 0.5 h after administration with a continued presence in plasma for at least 8 h and a bioavailability of 97.7%.

体内研究

LDC4297 (100 mg/kg; p.o. once) shows promising pharmacokinetic analyses.

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

Animal Model:	CD1 mice
Dosage:	100 mg/kg
Administration:	Oral gavage; 100 mg/kg once
Result:	Showed a half-life of 1.6 h, and the time to a mean peak plasma concentration of 1,297.6 ng/mL is reached 0.5 h after administration with a continued presence in plasma for at least 8 h and a bioavailability of 97.7%.

性状

Solid

溶解性数据

In Vitro:

DMSO : ≥ 60 mg/mL (138.72 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	2.3120 mL	11.5602 mL	23.1203 mL
5 mM	0.4624 mL	2.3120 mL	4.6241 mL
10 mM	0.2312 mL	1.1560 mL	2.3120 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: ≥ 2.5 mg/mL (5.78 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.78 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 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: ≥ 2.5 mg/mL (5.78 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.78 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 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: ≥ 2.5 mg/mL (5.78 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.78 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 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。