Azithromycin

別名：XZ-450,CP-62993

製品コード：S1835 純度：97%

Azithromycin is an antibiotic by inhibiting protein synthesis, used for the treatment of bacterial infections.

CAS No. 83905-01-5

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
50mg	JPY 37000	国内在庫あり
200mg	JPY 73500	国内在庫あり
1g	JPY 145500	国内在庫なし(納期7~10日)

代表番号: 045-509-1970\|電子メール：sales@selleck.co.jp よく尋ねられる質問

文献中Selleckの製品使用例（26）

Proc Natl Acad Sci U S A,2016113(50):14408-14413

質量管理及び製品安全説明書

現在のバッチを見る： 純度：>97%

Azithromycin関連製品

関連化合物ライブラリー	Kinase Inhibitor Library FDA-approved Drug Library Natural Product Library Bioactive Compound Library-I Highly Selective Inhibitor Library	もっと見る

Antibiotics for Mammalian Cell Culture阻害剤の選択性比較

阻害剤	Citation	EGFR/ErbB1	HER2/ErbB2	ErbB3	ErbB4	mutant EGFR	その他
Saracatinib (AZD0530)	299	+++					c-Src,c-YES,LCK
Canertinib (CI-1033)	48	++++	+++
AG-490	132	+					JAK2 (V617F)
CP-724714	108		++
WZ4002	34	++++
Sapitinib (AZD8931)	48	+++	+++	+++
CUDC-101	23	+++	++				HDAC,HDAC1,HDAC6
AG-1478	97	+++
PD153035 HCl	17	++++
Pelitinib (EKB-569)	11	+	+				Src,MEK/ERK,Raf
AEE788 (NVP-AEE788)	13	++++	+++		+		c-Abl,FLT1,c-Fms
AC480 (BMS-599626)	10	++	++		+
AP26113-analog (ALK-IN-1)	4					++	ALK,IGF1R,INSR
WZ3146	2	++++
Allitinib tosylate	16	++++	+++		++++
Rociletinib (CO-1686)	36	++
Varlitinib	8	+++	++++
Icotinib (BPI-2009H)	9	+++
TAK-285	4	++	++		+		MEK1,Aurora B,LCK
WHI-P154	11	+++					Src,VEGFR,JAK3
Daphnetin	4	+					PKA,PKC
PD168393	6	++++
CNX-2006	2	++				++
Tyrphostin 9	1	+					PDGFR
AG-18	1	+
Icotinib Hydrochloride	0	+++
HS-10296 hydrochloride	0					++++
MTX-531	0	++					PI3Kα
Avitinib maleate	0	+++				++++	BTK
limertinib	0					++++
AG 825	0		+				PDGFR
4-AMino-1-phenylpyrazolo[3,4-d]pyriMidine	0	+
AST-1306	0	++++	+++		++++
ErbB2 inhibitor	0		+		+
Tuxobertinib (BDTX-189)	2	++++	++++				RIPK2,BLK
Epertinib hydrochloride	0	++++	+++		+++
JND3229	0	+++				++	EGFR C797S
BI-4020	1					++++
Tyrphostin AG-528	0	+	+
AG 556	0	+
Canertinib dihydrochloride	8	+++	+++
EGFR Inhibitor	3	++					Microtubules
SU5214	0	+					VEGFR2
RG 13022	0	+
TQB3804	0					++++
zipalertinib (TAS6417)	3	+++			+++	++++	TXK,BMX
Pyrotinib dimaleate	4	++	++
PD153035	14	++++
AG 494	0	+
AG 555	0	+
Theliatinib (HMPL-309)	0	+++				++
Avitinib (Abivertinib)	2					++++	JAK3,BTK
Lazertinib	7	++++				++++	Del19,L85R
Lifirafenib (BGB-283)	6	++				+	WT A-RAF,C-RAF (Y340/341D),BRAF(V600E)
Nazartinib (EGF816)	6	++				++
Zorifertinib (AZD3759)	6	++++
CL-387785 (EKI-785)	5	++++
Poziotinib	34	+++	+++		++
AZ5104	4	++++			+++		ACK1,BLK,BRK
AV-412 free base	0	++++	++			++++
HER2-Inhibitor-1	1		✔
WZ8040	2	✔
Genistein	32	✔					topo II
Rezivertinib	0	✔
BDTX-1535	0	✔
Falnidamol	0	✔
BLU-945	0	✔
(S)-Sunvozertinib ((S)-DZD9008)	1	✔
Licochalcone D	0	✔					NF-κB,PARP,Caspase
Alflutinib (Furmonertinib) mesylate	2	✔					CYP3A4
(Rac)-JBJ-04-125-02	0	✔
Tyrphostin AG30 (AG30)	0	✔
AG-1557	0	✔
AG99	0	✔
MTX-211	2	✔					PI3K
RG14620	0	✔					ABCG2
Almonertinib (HS-10296)	2					✔
Cyasterone	1	✔
Norcantharidin	3	✔					c-Met
Naquotinib(ASP8273)	1	✔
EAI045	2					✔
Olmutinib (BI 1482694)	5	✔					BTK
Butein	2	✔
Chrysophanic Acid	3	✔					mTOR
EGCG ((-)-Epigallocatechin Gallate)	41	✔					DNMT,telomerase,FASN

1. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation. 2. "✔" indicates inhibitory effect, but without specific value.

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	活性情報	PMID
Hep2	Antichlamydial assay	4 ug/ml	8 hrs	Anti-Chlamydial activity against Chlamydia trachomatis Serovar LGV-L2 infected in Hep2 cells assessed as reduction in size and number of chlamydial inclusion at 4 ug/ml treated at 8 hrs post-infection and 24 hrs later re-infecting fresh Hep2 cells monolay	32227948
HeLa 299	Antichlamydial assay		44 to 48 hrs	Antichlamydial activity against Chlamydia trachomatis serovar L2 infected in human HeLa 299 cells assessed as reduction in number of inclusion bodies measured after 44 to 48 hrs by DAPI staining-based HCS assay, IC50=0.727μM.	29232584
THP1	Function assay		30 mins	Drug uptake in human THP1 cells at pH 6 to 7 after 30 mins	19564365
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生物活性

製品説明

Azithromycin is an antibiotic by inhibiting protein synthesis, used for the treatment of bacterial infections.

Targets

protein synthesis ^[1]

In Vitro
In vitro	Azithromycin reduces about 40% of IL-8 mRNA and protein expression in cystic fibrosis (CF) cells reaching the levels of non-CF cells. Azithromycin results in 50% and 70% reduction of NF-kappaB and AP-1 DNA binding, respectively, leading to levels of non-CF cells. ^[1] Azithromycin significantly enhances the intensity of a co-stimulatory molecule, CD80, on DCs but not CD86 and CD40 in dendritic cells (DCs). Azithromycin significantly increases the production of IL-10 and Clarithromycin (CAM) significantly inhibits the production of IL-6 by DCs. Azithromycin increases IL-10 and CAM decreases IL-2 productions significantly, when naive T cells derived from spleen are co-cultured with DCs treated in advance with LPS and these macrolides. ^[2] Azithromycin selectively inhibits fluid-phase endocytosis of horseradish peroxidase and lucifer yellow in J774 mouse macrophages. Azithromycin delays sequestration of receptor-bound transferrin and peroxidase-anti-peroxidase immune complexes into cell-surface endocytic pits and vesicles. Azithromycin down-regulates cell surface transferrin receptors, but not Fc gamma receptors, by causing a major delay in the accessibility of internalized transferrin receptors to the recycling route, without slowing down subsequent efflux, resulting in redistribution of the surface pool to an intracellular pool. ^[3] Azithromycin inserts into the DOPC lipid bilayer, so as to decrease its cohesion and to facilitate the merging of DPPC into the DOPC fluid matrix. ^[4]

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
臨床試験 (data from https://clinicaltrials.gov, updated on 2024-05-22)
NCT05972772	Not yet recruiting	Infectious Disease\|Therapeutics	Lao-Oxford-Mahosot Hospital Wellcome Trust Research Unit\|Mahidol Oxford Tropical Medicine Research Unit	March 20 2024	Phase 2\|Phase 3
NCT05796362	Not yet recruiting	Infectious Disease\|Drug Effect\|Clinical Infection	Brigham and Women''s Hospital\|Bill and Melinda Gates Foundation	April 2023	Phase 1

参考
[1] Cigana C, et al. P Biochem Biophys Res Commun, 2006, 350(4), 977-982. [2] Sugiyama K, et al. Clin Exp Immunol, 2007, 147(3), 540-546. [3] Tyteca D, et al. Exp Cell Res, 2002, 281(1), 86-100. [4] Fa N, et al. Biochim Biophys Acta, 2007, 1768(7), 1830-1838. + 展開

参考

[4] Fa N, et al. Biochim Biophys Acta, 2007, 1768(7), 1830-1838.

+ 展開

化学情報

分子量	748.98	化学式	C₃₈H₇₂N₂O₁₂
CAS No.	83905-01-5	SDF	Download Azithromycin SDFをダウンロードする
Smiles	CCC1C(C(C(N(CC(CC(C(C(C(C(C(=O)O1)C)OC2CC(C(C(O2)C)O)(C)OC)C)OC3C(C(CC(O3)C)N(C)C)O)(C)O)C)C)C)O)(C)O
保管	3年-20°C粉	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年-20°C粉	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ケ月-20°Cin solvent

In vitro
Batch:

DMSO : 100 mg/mL ( (133.51 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 : 100 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

Clear solution

5%DMSO 1 40%PEG300 Click to order 2 5%Tween 80 Click to order 3 50%ddH2O

5.0mg/ml (6.68mM)

Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

Clear solution

5% DMSO 1 95% Corn oil

0.83mg/ml (1.11mM)

Taking the 1 mL working solution as an example, add 50 μL of 16.6 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

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。

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