LDC4297 hydrochloride

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本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

2319747-14-1

包装与价格：

包装	价格(元)
5mg	电议
10mg	电议
25mg	电议
50mg	电议
100mg	电议
200mg	电议
500mg	电议

产品介绍

LDC4297 hydrochloride 是CDK7的选择性抑制剂，IC₅₀值为 0.13 nM。LDC4297 hydrochloride 抑制人巨细胞病毒 (HCMV) 复制，EC₅₀值为 24.5 nM。LDC4297 hydrochloride 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 hydrochloride 可用于感染的研究。

生物活性

LDC4297 hydrochloride is a selective inhibitor ofCDK7with anIC₅₀value of 0.13 nM. LDC4297 hydrochloride inhibits human cytomegalovirus (HCMV) replication with anEC₅₀value of 24.5 nM. LDC4297 hydrochloride shows broad antiviral activities toHerpesviridae,Adenoviridae,Poxviridae,RetroviridaeandOrthomyxoviridaewithEC₅₀values of 0.02-1.21 μM. LDC4297 hydrochloride can be used for the research ofinfection^[1].

IC₅₀& Target

CDK7

0.13 nM (IC₅₀)

166v VP22-GFP

0.02 μM (EC₅₀)

01-6332

0.27 μM (EC₅₀)

HIV-1 (NL4.3 strain)

1.04 μM (EC₅₀)

4LIG7

1.13 μM (EC₅₀)

体外研究
(In Vitro)

LDC4297 hydrochloride (0-10 μM; 6 d) dose-dependently inhibits HCMV replication with an EC₅₀value of 24.5 nM^[1].
LDC4297 hydrochloride (0-10 μM; 4 d) shows anti-proliferative activity to primary cultures of fibroblasts derived from human (HFF) with a GI₅₀value of 4.5 μM^[1].
LDC4297 hydrochloride (20 μM; 12-96 h) shows anti-HCMV activity through a multifaceted mode of action that involves an interference with virus-induced Rb phosphorylation^[1].
LDC4297 hydrochloride (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 EC₅₀values 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^[1].

Western Blot Analysis^[1]

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 hydrochloride (100 mg/kg; p.o. once) shows promising pharmacokinetic analyses^[1].

Animal Model:	CD1 mice^[1]
Dosage:	100 mg/kg
Administration:	Oral gavage; 100 mg/kg once
Result:	Showed a half-life (t1/2z) of 1.6 h, and the time to a mean peak plasma concentration of 1297.6 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%.

分子量

468.98

性状

Solid

Formula

C₂₃H₂₉ClN₈O

CAS 号

2319747-14-1

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)