Dalcetrapib | RO4607381 | CETP Inhibitor | AmBeed-信号通路专用抑制剂

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Dalcetrapib/达塞曲匹 {[allProObj[0].p_purity_real_show]}

货号：A162985 同义名： RO4607381; JTT-705

Dalcetrapib is a rhCETP inhibitor with IC50 of 0.2 μM.

Dalcetrapib/达塞曲匹化学结构
CAS号：211513-37-0

Dalcetrapib/达塞曲匹 3D分子结构
CAS号：211513-37-0

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Dalcetrapib/达塞曲匹纯度/质量文件产品仅供科研

货号：A162985 标准纯度： {[allProObj[0].p_purity_real_show]} 产品说明书

批次查询：批次纯度: COA SDS NMR HPLC CNMR LC-MS

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EGFR 亚型比较
CETP 亚型比较

产品名称	EGFR/ErbB1 ↓ ↑	ErbB3 ↓ ↑	ErbB4 ↓ ↑	HER2/ErbB2 ↓ ↑	mutant EGFR ↓ ↑	其他靶点	纯度
WZ-3146	++++ EGFR (E746_A750), IC50: 2 nM EGFR (E746_A750/T790M), IC50: 14 nM						99%+
Daphnetin	+ EGFR, IC50: 7.67 μM					PKC,PKA	95%
Lifirafenib	++ EGFR, IC50: 29 nM				+ EGFR(T790M/L858R), IC50: 495 nM		98%
PD168393	++++ EGFR, IC50: 0.70 nM						99%+
Nazartinib	++ mutant EGFR, Ki: 0.031 μM				++ mutant EGFR, Ki: 0.031 μM		98%
Norcantharidin	✔						98%
CL-387785	++++ EGFR, IC50: 370 pM						98%
WHI-P154	+++ EGFR, IC50: 4 nM					VEGFR,Src	98%
Tyrphostin A9	+ EGFR, IC50: 460 μM					PDGFR	98%
AG 555	+ EGFR, IC50: 0.7 μM						98%
AG 494	+ EGFR, IC50: 1.2 μM						99%+
AG-556	+ EGFR, IC50: 5 μM						98%
RG13022	+ EGFR, IC50: 4 μM						99%+
Tyrphostin RG 14620	✔						99%+
Vandetanib	+ EGFR, IC50: 500 nM						99%
CNX-2006	++ mutant EGFR, IC50: <20 nM				++ mutant EGFR, IC50: <20 nM		99%
AZD3759	++++ EGFR (L858R), IC50: 0.2 nM EGFR (WT), IC50: 0.3 nM						98%
Erlotinib	++++ EGFR, IC50: 2 nM						95%
Saracatinib	+++ EGFR (L861Q), IC50: 4 nM EGFR, IC50: 5 nM						99%+
AG1557	✔						99%
Rociletinib	++ EGFR (L858R/T790M), Ki: 21.5 nM EGFR (wt), Ki: 303.3 nM						98%
AG490	+ EGFR, IC50: 0.1 μM						98%
Cetuximab	++++ EGFR, Kd: 0.39 nM						99%
Osimertinib	++ WT EGFR, IC50: 12.92 nM L858R/T790M EGFR, IC50: 11.44 nM						98%
Osimertinib mesylate	✔						98% (Content MsOH 15.2-18.2%)
Chrysophanol	✔					mTOR	98%
PD153035	++++ EGFR, Ki: 5.2 pM						99%+
Olmutinib	✔					BTK	99%+
WZ4002	++++ EGFR (L858R), IC50: 2 nM EGFR (L858R/T790M), IC50: 8 nM						99%+
Icotinib	+++ EGFR, IC50: 5 nM						99%
Desmethyl Erlotinib HCl	++++ EGFR, IC50: 2 nM						99%
Cyasterone	✔						99%+
PP 3	+ EGFR tyrosine kinase, IC50: 2.7 μM						98%
WZ8040	✔						99%+
(-)-Epigallocatechin Gallate	✔						99%
AG 18	+ EGFR, IC50: 35 μM						99%+
O-Desmethyl gefitinib	++ EGFR, IC50: 36 nM						99%
Falnidamol	✔						99%+
AZ-5104	++++ EGFR (L858R), IC50: 6 nM EGFR (L861Q) , IC50: <1 nM		+++ ErbB4, IC50: 7 nM			BRK	99%+
Butein	✔						95%
Genistein	✔						98%
SU5214	+ EGFR, IC50: 36.7 μM						99%+
Naquotinib	✔						99%+
Gefitinib	++ EGFR, IC50: 15.5 nM				+ EGFR (858R/T790M), IC50: 823.3 nM		98%
Theliatinib	+++ WT EGFR, IC50: 3 nM				++ EGFR T790M/L858R, IC50: 22 nM		99%
Lazertinib	++++ WT EGFR, IC50: 76 nM L858R/T790M EGFR, IC50: 2 nM				++++ Del19/T790M, IC50: 1.7 nM		99%+
Gefitinib-based PROTAC 3	++ EGFR, DC50: 22.3 nM						99%+
MTX-211	✔					PI3K	98%
(E)-AG 99	✔						99%+
Licochalcone D	✔					PARP,Caspase	99%
Zipalertinib	+++ EGFR (L861Q), IC50: 4.1 nM EGFR WT, IC50: 8 nM		+++ HER4, IC50: 4 nM		++++ EGFR(d746-750), IC50: 1.4 nM EGFR L858R, IC50: 2 nM		97%
JND3229	+++ EGFR WT, IC50: 6.8 nM				++ EGFR L858R/T790M, IC50: 30.5 nM		99%+
Firmonertinib mesylate	✔						99%+
Tyrphostin AG30	✔						99%+
EGFR-IN-12	++ EGFR, IC50: 21 nM						99%+
Mobocertinib	✔						98%
(Rac)-JBJ-04-125-02	✔						99%
(S)-Sunvozertinib	✔						99%
BLU-945	✔						95%
Poziotinib	+++ HER1, IC50: 3.2 nM		++ HER4, IC50: 23.5 nM	+++ HER2, IC50: 5.3 nM			98%
TAK-285	++ EGFR/HER1, IC50: 23 nM		+ HER4, IC50: 260 nM	++ HER2, IC50: 17 nM			99%+
ARRY-380 analog				✔			99%
Canertinib	++++ EGFR, IC50: 1.5 nM			+++ ErbB2, IC50: 9.0 nM			99%+
Dacomitinib	+++ EGFR, IC50: 6.0 nM		+ ErbB4, IC50: 73.7 nM	+ ErbB2, IC50: 45.7 nM			98%
EGFR/ErbB-2/ErbB-4 inhibitor-2			+ ErbB4, IC50: 1.91 μM	+ ErbB2, IC50: 0.08 μM			99%+
(E/Z)-CP-724714				++ HER2/ErbB2, IC50: 10 nM			95%
Lapatinib	++ EGFR, IC50: 10.8 nM		+ ErbB4, IC50: 367 nM	+++ ErbB2, IC50: 9.2 nM			98%
AEE788	++++ EGFR, IC50: 2 nM		+ HER4/ErbB4, IC50: 160 nM	+++ HER2/ErbB2, IC50: 6 nM		c-Fms	98+%
AV-412 free base	++++ EGFR, IC50: 0.75 nM			++ ErbB2, IC50: 19 nM	++++ EGFR^T790M, IC50: 0.79 nM EGFR^L858R/T790M, IC50: 0.51 nM		98+%
Neratinib	+ EGFR, IC50: 92 nM			+ HER2, IC50: 59 nM		Src	98%
BMS-599626	++ HER1, IC50: 20 nM		+ HER4, IC50: 190 nM	++ HER2, IC50: 30 nM			98%
Tucatinib				+++ ErbB2, IC50: 8 nM			98%
Allitinib	++++ EGFR, IC50: 0.5 nM		++++ ErbB4, IC50: 0.8 nM	+++ ErbB2, IC50: 3.0 nM			99%
Pelitinib	+ EGFR, IC50: 38.5 nM			+ ErbB2, IC50: 1.255 μM		Raf,Src	99%+
Sapitinib	+++ EGFR, IC50: 4 nM	+++ ErbB3, IC50: 4 nM		+++ ErbB2, IC50: 3 nM			99%+
CUDC-101	+++ EGFR, IC50: 2.4 nM			++ HER2, IC50: 15.7 nM		HDAC	99%+
Varlitinib	+++ ErbB1, IC50: 7 nM			++++ ErbB2, IC50: 2 nM			99%+
Afatinib dimaleate	++++ EGFR (wt), IC50: 0.5 nM EGFR (L858R/T790M), IC50: 0.4 nM			++ HER2, IC50: 14 nM			98%
Canertinib 2HCl	+++ EGFR, IC50: 7.4 nM			+++ ErbB2, IC50: 9 nM			99%
Allitinib tosylate	++++ EGFR (T790M/L858R), IC50: 12 nM EGFR, IC50: 0.5 nM		++++ ErbB4, IC50: 0.8 nM	+++ ErbB2, IC50: 3.0 nM			99%
Tyrphostin AG 528	+ EGFR, IC50: 4.9 μM			+ HER2, IC50: 2.1 μM			97%
Afatinib	++++ EGFR (wt), IC50: 0.5 nM EGFR (L858R), IC50: 10 nM		++++ ErbB4, IC50: 1 nM	++ HER2, IC50: 14 nM			99%
Pyrotinib dimaleate	++ EGFR, IC50: 0.013 μM			++ HER2, IC50: 0.038 μM			98%
Epertinib HCl	++++ EGFR, IC50: 1.48 nM		+++ HER4, IC50: 2.49 nM	+++ HER2, IC50: 7.15 nM			99%
Tuxobertinib	++++ EGFR, Kd: 0.2 nM			++++ HER2, Kd: 0.76 nM			99%
ALK-IN-1					++ EGFR(C797S/del19), IC50: 138.6 nM EGFR(del19), IC50: 36.8 nM	ALK	99%
Brigatinib					+ EGFR(del19), IC50: 39.9 nM EGFR(C797S/T790M/del19), IC50: 67.2 nM	FLT3,ALK	98%
Avitinib					++++ EGFR L858R/T790M, IC50: 0.18 nM	BTK	99%+
EAI045					✔		97%
Almonertinib					✔		99%
BI-4020					++++ EGFR^{del19 T790M C797S}, IC50: 0.2 nM		99%+
EGFR-IN-7					++++ EGFR^{d746-750/T790M/C797S}, IC50: 0.26 nM EGFR^L858R/T790M, IC50: 0.19 nM		99%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

产品名称	CETP ↓ ↑	纯度
Torcetrapib	++ CETP, IC50: 37 nM	95%
Anacetrapib	+++ Mutant CETP (C13S), IC50: 11.8 nM rhCETP, IC50: 7.9 nM	98%
Dalcetrapib	+ rhCETP, IC50: 0.2 μM	98%
Evacetrapib	++++ CETP, IC50: 5.5 nM	98%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

Dalcetrapib/达塞曲匹生物活性

靶点

CETP

rhCETP, IC50:0.2 μM

描述

Cholesteryl ester transfer protein (CETP) promotes the transfer of cholesteryl esters from high-density lipoprotein (HDL) to very low-density lipoprotein and low-density lipoprotein (LDL). Therefore, CETP inhibition raises high-density lipoprotein cholesterol (HDL-C) levels and decreases LDL-C levels^[7]. Dalcetrapib is a CETP inhibitor with IC₅₀ of 0.2 μM that increases the plasma HDL cholesterol^[8]. Dalcetrapib induces a conformational change in CETP, when added to human plasma. CETP-induced pre-β-HDL formation in human plasma is unchanged by dalcetrapib ≤3 μM and increased at 10 μM. Dalcetrapib statistically and significantly increases pre-β-HDL formation^[8]. Dalcetrapib achieves 50% inhibition of CETP activity in human plasma at a concentration of 9 μM^[9]. Dalcetrapib inhibits the CETP activity of media in HepG2 in a dose-dependent manner^[10]. Treatment with Dalcetrapib leads to significant increases in HDL-C levels. In hamsters injected with [³H]cholesterol-labeled autologous macrophages. dalcetrapib significantly increases fecal elimination of both [³H]neutral sterols and [³H]bile acids. Dalcetrapib increases plasma HDL-[³H]cholesterol^[8]. Dalcetrapib increases the plasma HDL cholesterol level by 27% and 54%, respectively, when given at oral doses of 30 mg/kg or 100 mg/kg once a day for 3 days to male Japanese white rabbits^[9].

Dalcetrapib/达塞曲匹动物研究

Dose

Rat: 100 mg/kg^[3] (p.o.); 10 mg/kg^[3] (i.v.) Monkey: 100 mg/kg^[3] (p.o.); 10 mg/kg^[3] (i.v.) Hamsters: 200 mg/kg^[4] (p.o., BID) Rabbit: 10 mg/kg - 100 mg/kg^[5] (p.o.) Male cynomolgus monkey: 50 mg/kg^[6] (p.o.)

Administration

p.o., i.v.

Pharmacokinetics

Animal	Rats^[3]	Monkeys^[3]
Dose	10 mg/kg (i.v.) 100 mg/kg (p.o.)	10 mg/kg (i.v.) 100 mg/kg (p.o.)
Administration	i.v. p.o.	i.v. p.o.
F	26.9 ± 7.0% (p.o.)	18.0% (p.o.)
T_max	1.7 ± 0.6 h (p.o.)	4 h (p.o.)
t_t1/2β		12.5 h (i.v.) 8.4 h (p.o.)
AUC_inf		19.41 μg·Eq·h/ml (i.v.) 35.03 μg·Eq·h/ml (p.o.)
AUC_0-inf	6.75 ± 1.09 μg·Eq·h/ml (i.v.) 18.16 ± 4.71 μg·Eq·h/ml (p.o.)
C₀	14.17 ± 4.99 μg Eq/ml (i.v.)	7.94 μg Eq/ml (i.v.)
Vss	5.18 ± 0.97 L/kg (i.v.)	6.25 L/kg (i.v.)
T_1/2β	5.5 ± 1.3 h (i.v.) 4.0 ± 0.3 h (p.o.)
C_max	2.80 ± 0.75 μg Eq/ml (p.o.)	2.16 μg Eq/ml (p.o.)
CL	1.51 ± 0.26 L/h/kg (i.v.)	0.52 L/h/kg (i.v.)
T_1/2α	0.15 ± 0.09 h (i.v.)

Dalcetrapib/达塞曲匹参考文献

[1]Niesor EJ, Magg C, et al. Modulating cholesteryl ester transfer protein activity maintains efficient pre-β-HDL formation and increases reverse cholesterol transport. J Lipid Res. 2010 Dec;51(12):3443-54.

[2]Shinkai H, Maeda K, et al. bis(2-(Acylamino)phenyl) disulfides, 2-(acylamino)benzenethiols, and S-(2-(acylamino)phenyl) alkanethioates as novel inhibitors of cholesteryl ester transfer protein. J Med Chem. 2000 Sep 21;43(19):3566-72.

[3]Takubo H, Ishikawa T, et al. Pharmacokinetics and disposition of dalcetrapib in rats and monkeys. Xenobiotica. 2014 Dec;44(12):1117-26.

[4]Briand F, Thieblemont Q, et al. Anacetrapib and dalcetrapib differentially alters HDL metabolism and macrophage-to-feces reverse cholesterol transport at similar levels of CETP inhibition in hamsters. Eur J Pharmacol. 2014 Oct 5;740:135-43.

[5]Shinkai H, Maeda K, et al. bis(2-(Acylamino)phenyl) disulfides, 2-(acylamino)benzenethiols, and S-(2-(acylamino)phenyl) alkanethioates as novel inhibitors of cholesteryl ester transfer protein. J Med Chem. 2000 Sep 21;43(19):3566-72.

[6]Kuhlmann O, Heinig K, et al. Dalcetrapib pharmacokinetics and metabolism in the cynomolgus monkey. Xenobiotica. 2011 May;41(5):430-6.

[7]Kosmas CE, DeJesus E, Rosario D, Vittorio TJ. CETP Inhibition: Past Failures and Future Hopes. Clin Med Insights Cardiol. 2016 Mar 13;10:37-42. doi: 10.4137/CMC.S32667. PMID: 26997876; PMCID: PMC4790583.

[8]Niesor EJ, Magg C, Ogawa N, Okamoto H, von der Mark E, Matile H, Schmid G, Clerc RG, Chaput E, Blum-Kaelin D, Huber W, Thoma R, Pflieger P, Kakutani M, Takahashi D, Dernick G, Maugeais C. Modulating cholesteryl ester transfer protein activity maintains efficient pre-β-HDL formation and increases reverse cholesterol transport. J Lipid Res. 2010 Dec;51(12):3443-54. doi: 10.1194/jlr.M008706. Epub 2010 Sep 22. PMID: 20861162; PMCID: PMC2975716.

[9]Shinkai H, Maeda K, Yamasaki T, Okamoto H, Uchida I. bis(2-(Acylamino)phenyl) disulfides, 2-(acylamino)benzenethiols, and S-(2-(acylamino)phenyl) alkanethioates as novel inhibitors of cholesteryl ester transfer protein. J Med Chem. 2000 Sep 21;43(19):3566-72. doi: 10.1021/jm000224s. PMID: 11000011.

[10]Huang Z, Inazu A, Kawashiri MA, Nohara A, Higashikata T, Mabuchi H. Dual effects on HDL metabolism by cholesteryl ester transfer protein inhibition in HepG2 cells. Am J Physiol Endocrinol Metab. 2003 Jun;284(6):E1210-9. doi: 10.1152/ajpendo.00453.2002. Epub 2003 Feb 25. PMID: 12604506.

Dalcetrapib/达塞曲匹实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

2.57mL

0.51mL

0.26mL

12.83mL

2.57mL

1.28mL

25.67mL

5.13mL

2.57mL

Dalcetrapib/达塞曲匹技术信息

CAS号	211513-37-0
分子式	C₂₃H₃₅NO₂S
分子量	389.59
SMILES Code	CC(C)C(SC1=CC=CC=C1NC(C2(CC(CC)CC)CCCCC2)=O)=O
MDL No.	MFCD06407886

别名	RO4607381; JTT-705
运输	蓝冰
InChI Key	YZQLWPMZQVHJED-UHFFFAOYSA-N
Pubchem ID	6918540

存储条件

In solvent -20°C:3-6个月-80°C:12个月

Pure form Sealed in dry, store in freezer, under -20°C

溶解方案

细胞实验：

DMSO: 50 mg/mL(128.34 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

动物实验：请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的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

方案一

方案二

动物实验配方

0.5% methylcellulose+water 30 mg/mL suspension

Dalcetrapib/达塞曲匹 {[allProObj[0].p_purity_real_show]}

Dalcetrapib/达塞曲匹纯度/质量文件产品仅供科研

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Dalcetrapib/达塞曲匹生物活性

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Dalcetrapib/达塞曲匹参考文献

Dalcetrapib/达塞曲匹实验方案

Dalcetrapib/达塞曲匹技术信息

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Dalcetrapib/达塞曲匹 质控信息

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最近浏览的产品

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摩尔计算器

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总药量计算器

工作液计算器

细胞研究

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Dalcetrapib/达塞曲匹纯度/质量文件产品仅供科研

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Dalcetrapib/达塞曲匹参考文献

Dalcetrapib/达塞曲匹实验方案

Dalcetrapib/达塞曲匹技术信息