Atorvastatin

製品コード：S5715 純度：99.51%

Atorvastatin is a lipid lowering agent. It is a competitive inhibitor of hydroxymethylglutaryl-coenzyme A (HMG-CoA) reductase, the rate-determining enzyme in cholesterol biosynthesis via the mevalonate pathway. Atorvastatin activates autophagy.

CAS No. 134523-00-5

サイズ	価格(税別)	在庫状況
10mM (1mL in DMSO)	JPY 29500	国内在庫あり
25mg	JPY 22000	国内在庫あり
100mg	JPY 44500	国内在庫あり
1g	JPY 130500	国内在庫なし(納期7~10日)

代表番号: 045-509-1970\|電子メール：[email protected] よく尋ねられる質問

文献中Selleckの製品使用例（22）

製品安全説明書

現在のバッチを見る：純度： 99.51%

99.51

Atorvastatin関連製品

関連製品	Simvastatin Lovastatin Fluvastatin Sodium Pitavastatin calcium Rosuvastatin calcium Atorvastatin Calcium Pravastatin sodium Pravastatin Mevastatin SR-12813 Clinofibrate	もっと見る
関連化合物ライブラリー	Metabolism Compound Library Anti-cancer Metabolism Compound Library Glutamine Metabolism Compound Library Carbohydrate Metabolism Compound Library Lipid Metabolism Compound Library	もっと見る

シグナル伝達経路

HMG-CoA Reductaseシグナル伝達経路

HMG-CoA Reductase阻害剤の選択性比較

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	活性情報	PMID
hepatocytes	Function assay	0.1 to 10 uM	up to 90 mins	Drug metabolism in Sprague-Dawley rat hepatocytes assessed per 10'6 cells at 0.1 to 10 uM up to 90 mins by media-loss method, Km=0.43μM	22593038
hepatocytes	Function assay	0.1 to 10 uM	up to 90 mins	Drug metabolism in Sprague-Dawley rat hepatocytes assessed per 10'6 cells at 0.1 to 10 uM up to 90 mins by conventional assay, Km=1.3μM	22593038
Hep3G	Function assay	25 uM	48 hrs	Inhibition of HMG CoA reductase in human Hep3G cells assessed as increase in LDL receptor expression at 25 uM incubated for 48 hrs by immunofluorescence method	31005367
C2C12	Function assay	1 uM		Induction of cell differentiation in mouse C2C12 cells assessed as myosin heavy chain expression at 1 uM	20081855
HepG2	Function assay	1 uM		Upregulation of LDL receptor expression in human HepG2 cells at 1 uM in presence of ARH-specific siRNA	20356098
HepG2	Function assay	10 uM		Induction of SREBP2 maturation in human HepG2 cells at 10 uM after overnight incubation by immunoblot analysis	26784936
A549	Cytotoxicity assay		72 hrs	Cytotoxicity against human A549 cells after 72 hrs by MTT assay, IC50=8.7μM	23570542
HS68	Cytotoxicity assay		72 hrs	Cytotoxicity against human HS68 cells after 72 hrs by MTT assay, IC50=22.7μM	23570542
MEF	Cytotoxicity assay		72 hrs	Cytotoxicity against mouse MEF cells after 72 hrs by MTT assay, IC50=30.7μM	23570542
human red blood cells	Antiplasmodial assay		48 hrs	Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum W2 infected in human red blood cells after 48 hrs by SYBR test, IC50=10.3μM	26988303
HEK293	Function assay			TP_TRANSPORTER: uptake in OATP1B1-expressing HEK293 cells, Km=12.4μM	15970799
L6	Function assay			Inhibition of cholesterol synthesis in rat L6 cells assessed as incorporation of [14C]acetate into cholesterol, IC50=0.078μM	18412317
HEK293	Function assay			Activity at human liver OATP1B3 expressed in HEK293 Flp-In cells, Km=0.73μM	22541068
HEK293	Function assay			Activity at human liver OATP1B1 expressed in HEK293 Flp-In cells, Km=0.77μM	22541068
HEK293	Function assay			Activity at human liver OATP2B1 expressed in HEK293 Flp-In cells, Km=2.84μM	22541068
HEK293	Function assay			Inhibition of OATP1B1 (unknown origin) expressed in HEK293 cells using estradiol-17beta-glucuronide substrate, IC50=0.6μM	22587986
HEK293	Function assay			Inhibition of OATP1B1 (unknown origin) expressed in HEK293 cells using pitavastatin substrate, IC50=0.8μM	22587986
HEK293	Function assay			Inhibition of OATP1B1 (unknown origin) expressed in HEK293 cells using estrone-3-sulfate substrate, IC50=1.6μM	22587986
A549	Function assay			Reductase Activity Assay: The HMGR activity was performed using HMG-CoA reductase assay kit from Sigma-Aldrich with the human recombinant protein or 100 μg total cell lysates from A549 cells. Lovastatin was used as a positive control, and SAHA as a negati, IC50=0.0116μM	ChEMBL
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生物活性

製品説明	Atorvastatin is a lipid lowering agent. It is a competitive inhibitor of hydroxymethylglutaryl-coenzyme A (HMG-CoA) reductase, the rate-determining enzyme in cholesterol biosynthesis via the mevalonate pathway. Atorvastatin activates autophagy.

In Vitro
In vitro	Atorvastatin, one of the statins, inhibits the c-Myc pathway in chronic myeloid leukemia (CML) cells, demonstrating that c-Myc is a target of statins.^[1]
細胞実験	細胞株	murine CML-KLS⁺ cells, OP-9 stromal cells
	濃度	2 μM
	反応時間	3 days
	実験の流れ	CML cKit+Lineage Sca1+ (KLS) cells are isolated from CML mice. Thereafter, the effect of statins on the colony-forming capacity of CML-KLS cells is determined. Freshly isolated CML-KLS cells are co-cultured with OP-9 stromal cells in the presence of IM (1 M), DA (0.5 M), and rosuvastatin (2 M) or atorvastatin (2 M) for 72 h. Thereafter, the cells are washed with PBS and transferred to semi-solid medium. The number of colonies is counted under the microscope.
実験結果図	Methods	Biomarkers	結果図	PMID
	Growth inhibition assay	Cell viability		24815071
	Western blot	PDX-1 / BETA2 / NeuroD		30863781

In Vivo
In Vivo	ATV-Exos activates AKT/eNOS signaling pathway to augment the angiogenesis of endothelial cells via upregulating miR-211-3p, thereby resulting in accelerated wound regeneration of the diabetic rats.^[2]
動物実験	動物モデル	Sprague-Dawley rats ofdiabetes models
	投与量	50 μg/mL
	投与経路	s.c

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
臨床試験 (data from https://clinicaltrials.gov, updated on 2024-01-11)
NCT04915183	Not yet recruiting	Hearing Loss\|Head and Neck Cancer	National Institute on Deafness and Other Communication Disorders (NIDCD)\|National Institutes of Health Clinical Center (CC)	January 12 2024	Phase 3
NCT06191991	Active not recruiting	Healthy Volunteers	Aligos Therapeutics	November 3 2023	Phase 1

参考
[1] Jang HJ, et al. Cancers (Basel). 2021;13(21):5543. [2] Yu M, et al. Stem Cell Res Ther. 2020;11(1):350.

参考

化学情報

分子量	558.64	化学式	C₃₃H₃₅FN₂O₅
CAS No.	134523-00-5	SDF	--
Smiles	CC(C)C1=C(C(=C(N1CCC(CC(CC(=O)O)O)O)C2=CC=C(C=C2)F)C3=CC=CC=C3)C(=O)NC4=CC=CC=C4
保管	3 years -20°C powder	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	1年-80°Cin solvent
保管	3 years -20°C powder	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	1个月-20°Cin solvent

In vitro
Batch:

DMSO : 100 mg/mL ( (179.0 mM)；吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。)

Ethanol : 17 mg/mL

Water : Insoluble

モル濃度計算器

in vivo
Batch:

Add solvents to the product individually and in order.

投与溶液組成計算機

実験計算

モル濃度計算器

質量	濃度	体積	分子量
=	×	×

希釈計算器分子量計算器

投与溶液組成計算機(クリア溶液)

ステップ１：実験データを入力してください。（実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します）

投与量 mg/kg 動物平均体重 g 投与体積（動物毎）μL 動物数匹

ステップ２：投与溶媒の組成を入力してください。（ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください）

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

計算結果：

投与溶媒濃度： mg/ml;

DMSOストック溶液調製方法： mg 試薬を μL DMSOに溶解する（濃度 mg/mL, 注：濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )

投与溶媒調製方法：Take μL DMSOストック溶液に μL PEG300，を加え、完全溶解後μL Tween 80，を加えて完全溶解させた後 μL ddH₂O，を加え完全に溶解させます。

投与溶媒調製方法：μL DMSOストック溶液に μL Corn oil，を加え、完全溶解。

注意：１.ストック溶液に沈殿、混濁などがないことをご確認ください；
２.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。

技術サポート

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Handling Instructions

他に質問がある場合は、お気軽にお問い合わせください。

* 必須

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):