Alisporivir (Synonyms: Debio-025; DEB-025)

Name: Alisporivir
Brand: MedChemExpress
SKU: HY-12559
Rating: 5.0 (16 reviews)

製品番号: HY-12559 純度: 99.03%: Data Sheet SDS COA 取扱説明書
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Alisporivir (Debio-025) is a cyclophilin inhibitor molecule with potent anti-hepatitis C virus (HCV) activity.

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Alisporivir 構造式

CAS 番号 : 254435-95-5

容量	価格（税別）	在庫状況	数量
1 mg	$700	在庫あり	Estimated Time of Arrival: December 31
5 mg	$1400	在庫あり	Estimated Time of Arrival: December 31
10 mg	$2000	在庫あり	Estimated Time of Arrival: December 31
25 mg	$3250	在庫あり	Estimated Time of Arrival: December 31
50 mg	$4550	在庫あり	Estimated Time of Arrival: December 31
100 mg	$6400	在庫あり	Estimated Time of Arrival: December 31
200 mg		お問い合わせ
500 mg		お問い合わせ

or バルクお問い合わせ

* アイテムを追加する前、数量をご選択ください

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カスタマーレビュー

Based on 16 publication(s) in Google Scholar

顧客検証

Cyclophilin アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示

Cyclophilin A Cyclophilin B Cyclophilin C Cyclophilin D Cyclophilin G Cyclophilin E

生物活性
プロトコル
純度とドキュメンテーション
参考文献
カスタマーレビュー

製品説明

Alisporivir (Debio-025) is a cyclophilin inhibitor molecule with potent anti-hepatitis C virus (HCV) activity.

Cellular Effect

Cell Line	Type	Value	Description	References
CHO	IC₅₀	0.8 μM Compound: 3	Inhibition of OATP1B1 (unknown origin) expressed in CHO cells using 8-fluorescein-cAMP substrate by fluorescent photometry Inhibition of OATP1B1 (unknown origin) expressed in CHO cells using 8-fluorescein-cAMP substrate by fluorescent photometry	[PMID: 25310383]
Caco-2	CC₅₀	> 20 μM Compound: ALISPORIVIR	Toxicity against Caco-2 cells determined at 48 hours by intracellular ATP concentration using the CellTiter-Glo Luminescent Cell Viability Assay Toxicity against Caco-2 cells determined at 48 hours by intracellular ATP concentration using the CellTiter-Glo Luminescent Cell Viability Assay	10.21203/rs.3.rs-23951/v1
Caco-2	IC₅₀	3.1 μM Compound: ALISPORIVIR	Determination of IC50 values for inhibition of SARS-CoV-2 induced cytotoxicity of Caco-2 cells after 48 hours by high content imaging Determination of IC50 values for inhibition of SARS-CoV-2 induced cytotoxicity of Caco-2 cells after 48 hours by high content imaging	10.21203/rs.3.rs-23951/v1
HEK293	IC₅₀	0.11 μM Compound: 3	Inhibition of BSEP (unknown origin) expressed in HEK293 cells using [3H]taurocholic acid substrate Inhibition of BSEP (unknown origin) expressed in HEK293 cells using [3H]taurocholic acid substrate	[PMID: 25310383]
HEK293	IC₅₀	0.18 μM Compound: 3	Inhibition of OATP1B1 (unknown origin) expressed in HEK293 cells using [3H]estradiol-17beta-glucuronide substrate Inhibition of OATP1B1 (unknown origin) expressed in HEK293 cells using [3H]estradiol-17beta-glucuronide substrate	[PMID: 25310383]
HEK293	IC₅₀	0.22 μM Compound: 3	Inhibition of OATP1B3 (unknown origin) expressed in HEK293 cells using [3H]estradiol-17beta-glucuronide substrate Inhibition of OATP1B3 (unknown origin) expressed in HEK293 cells using [3H]estradiol-17beta-glucuronide substrate	[PMID: 25310383]
HeLa	IC₅₀	> 8.2 μM Compound: Debio-025	Antiviral activity against RSV infected in human HeLa cells assessed as inhibition of viral replication Antiviral activity against RSV infected in human HeLa cells assessed as inhibition of viral replication	[PMID: 18212100]
Huh-5-2	CC₅₀	> 3 μM Compound: Debio-025	Cytotoxicity against human Huh5-2 cells after 3 days by MTT assay Cytotoxicity against human Huh5-2 cells after 3 days by MTT assay	[PMID: 18625766]
Huh-5-2	EC₅₀	0.06 μM Compound: Debio-025	Antiviral activity against Hepatitis C virus genotype 1b infected in human Huh5-2 cells assessed as reduction in replicon RNA after 4 days by luciferase assay Antiviral activity against Hepatitis C virus genotype 1b infected in human Huh5-2 cells assessed as reduction in replicon RNA after 4 days by luciferase assay	[PMID: 18625766]
Huh-7	EC₅₀	116 nM Compound: 3	Antiviral activity against HCV subtype 1b in human Huh7.5 cells expressing subgenomic HCV replicons and coexpressing luciferase reporter gene in presence of 40% human serum Antiviral activity against HCV subtype 1b in human Huh7.5 cells expressing subgenomic HCV replicons and coexpressing luciferase reporter gene in presence of 40% human serum	[PMID: 25310383]
Huh-7	EC₅₀	46 nM Compound: 3	Antiviral activity against HCV subtype 1b in human Huh7.5 cells expressing subgenomic HCV replicons and coexpressing luciferase reporter gene Antiviral activity against HCV subtype 1b in human Huh7.5 cells expressing subgenomic HCV replicons and coexpressing luciferase reporter gene	[PMID: 25310383]
Huh-7	EC₅₀	70 nM Compound: 3	Antiviral activity against HCV subtype 1a in human Huh7.5 cells expressing subgenomic HCV replicons and coexpressing luciferase reporter gene Antiviral activity against HCV subtype 1a in human Huh7.5 cells expressing subgenomic HCV replicons and coexpressing luciferase reporter gene	[PMID: 25310383]
MDCK	IC₅₀	> 25 μM Compound: Debio-025	Antiviral activity against BVDV infected in MDCK cells assessed as inhibition of viral replication Antiviral activity against BVDV infected in MDCK cells assessed as inhibition of viral replication	[PMID: 18212100]
MDCK	IC₅₀	> 9.9 μM Compound: Debio-025	Antiviral activity against Influenza A virus H1N1 infected in MDCK cells assessed as inhibition of viral replication Antiviral activity against Influenza A virus H1N1 infected in MDCK cells assessed as inhibition of viral replication	[PMID: 18212100]
MDCK	IC₅₀	> 9.9 μM Compound: Debio-025	Antiviral activity against Influenza A virus H3N2 infected in MDCK cells assessed as inhibition of viral replication Antiviral activity against Influenza A virus H3N2 infected in MDCK cells assessed as inhibition of viral replication	[PMID: 18212100]
MDCK	IC₅₀	> 9.9 μM Compound: Debio-025	Antiviral activity against influenza B virus infected in MDCK cells assessed as inhibition of viral replication Antiviral activity against influenza B virus infected in MDCK cells assessed as inhibition of viral replication	[PMID: 18212100]
MT4	CC₅₀	20 μM Compound: 3	Cytotoxicity against human MT4 cells by CDCF probe based assay Cytotoxicity against human MT4 cells by CDCF probe based assay	[PMID: 25310383]
MT4	EC₅₀	63 nM Compound: 7, [D-Ala]3[EtVal]4CsA	Antiviral activity against HIV1 3B infected in human MT4 cells assessed as reduction in virus-induced cytopathogenicity after 5 to 6 days by MTT assay Antiviral activity against HIV1 3B infected in human MT4 cells assessed as reduction in virus-induced cytopathogenicity after 5 to 6 days by MTT assay	[PMID: 23849880]
MT4	IC₅₀	0.099 μM Compound: Debio-025	Antiviral activity against HIV-1 3B infected in human MT4 cells assessed as inhibition of virus induced cytopathic effect by MTT assay Antiviral activity against HIV-1 3B infected in human MT4 cells assessed as inhibition of virus induced cytopathic effect by MTT assay	[PMID: 18212100]
PBMC	IC₅₀	0.5 μM Compound: 3	Cytotoxicity against PHA-stimulated human PBMC by 5-bromo-2'-deoxyuridine incorporation assay Cytotoxicity against PHA-stimulated human PBMC by 5-bromo-2'-deoxyuridine incorporation assay	[PMID: 25310383]
PBMC	IC₅₀	0.82 μM Compound: Debio-025	Antiproliferative activity against mouse PBMC with MLR assessed as inhibition of [3H]thymidine incorporation after 18 hrs Antiproliferative activity against mouse PBMC with MLR assessed as inhibition of [3H]thymidine incorporation after 18 hrs	[PMID: 18212100]
PBMC	IC₅₀	840 nM Compound: Alisporivir, DEBIO-025	Immunosuppressive activity in human PBMC isolated from two individuals assessed as inhibition of proliferation using [3H]thymidine by mixed lymphocyte reaction assay Immunosuppressive activity in human PBMC isolated from two individuals assessed as inhibition of proliferation using [3H]thymidine by mixed lymphocyte reaction assay	10.1039/C1MD00227A
Sf9	IC₅₀	18 μM Compound: 3	Inhibition of human MRP2 expressed in Sf9 cells inside out vesicles using CDCF substrate Inhibition of human MRP2 expressed in Sf9 cells inside out vesicles using CDCF substrate	[PMID: 25310383]
Vero	IC₅₀	7.7 μM Compound: Debio-025	Antiviral activity against SARS coronavirus infected in african green monkey Vero cells assessed as inhibition of viral replication Antiviral activity against SARS coronavirus infected in african green monkey Vero cells assessed as inhibition of viral replication	[PMID: 18212100]
Vero	IC₅₀	> 16.6 μM Compound: Debio-025	Antiviral activity against Yellow fever virus 17D infected in african green monkey Vero cells assessed as inhibition of viral replication Antiviral activity against Yellow fever virus 17D infected in african green monkey Vero cells assessed as inhibition of viral replication	[PMID: 18212100]
Vero	IC₅₀	> 25 μM Compound: Debio-025	Antiviral activity against Coxsackie B3 infected in african green monkey Vero cells assessed as inhibition of viral replication Antiviral activity against Coxsackie B3 infected in african green monkey Vero cells assessed as inhibition of viral replication	[PMID: 18212100]
Vero	IC₅₀	> 25 μM Compound: Debio-025	Antiviral activity against Parainfluenza 3 infected in african green monkey Vero cells assessed as inhibition of viral replication Antiviral activity against Parainfluenza 3 infected in african green monkey Vero cells assessed as inhibition of viral replication	[PMID: 18212100]

体外実験

DEB025 binds to CypA, a peptidyl-prolyl cis-trans isomerase which is a crucial cofactor for HCV replication^[1]. Alisporivir (Debio-025) represents the prototype of a new class of non-immunosuppressive cyclophilin inhibitors. Alisporivir prevents HCV protein-mediated collapse of the respiration-driven mitochondrial membrane potential. Alisporivir prevents HCV protein-mediated mitochondrial dysfunction outside the context of apoptosis, calcium overload, production of ROS, dysfunction^[2]. In cell culture models, low-micromolar doses of alisporivir block SARS-CoV and MERS-CoV replication. Combination treatment with Alisporivir and ICN-1229 increases the anti-MERS-CoV activity in cell culture^[3]. Alisporivir pretreatment stimulates antigen presentation by hepatoma target cells, leading to enhancement of antigen-specific CD8+ T cell activation by 40%. Alisporivir induces an increase of MHC-I and beta-2 microglobulin on the surface of several cell lines^[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

体内実験

Combination treatment with Alisporivir and ICN-1229 does not protect against SARS-CoV infection in a mouse model^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

臨床実験

分子量

1216.64

分子式

C₆₃H₁₁₃N₁₁O₁₂

CAS 番号

254435-95-5

Appearance

Solid

Color

White to off-white

Sequence

Cyclo({N-Me-Bmt(E)}-{Abu}-{d-N-Me-Ala}-{N-Et-Val)-Val-{N-Me-Leu}-Ala-{d-Ala}-{N-Me-Leu}-{N-Me-Leu}-{N-Me-Val})

Sequence Shortening

Cyclo({N-Me-Bmt(E)}-{Abu}-{d-N-Me-Ala}-{N-Et-Val)-V-{N-Me-Leu}-A-{d-Ala}-{N-Me-Leu}-{N-Me-Leu}-{N-Me-Val})

輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

polypeptide, stored under nitrogen, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (polypeptide, stored under nitrogen, away from moisture)

溶剤 & 溶解度

体外:

DMSO : 50 mg/mL (41.10 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	0.8219 mL	4.1097 mL	8.2194 mL
5 mM	0.1644 mL	0.8219 mL	1.6439 mL
10 mM	0.0822 mL	0.4110 mL	0.8219 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

一般には略語で表示されます：C₁V₁ = C₂V₂

濃度 _（開始）

体積 _（開始）

濃度 _（終了）

体積 _（終了）

体内:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 5% DMSO 40% PEG300 5% Tween-80 50% Saline
Solubility: ≥ 2.62 mg/mL (2.15 mM); Clear solution
Protocol 2

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (2.05 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen, away from moisture)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

純度とドキュメンテーション

純度: 99.03%

Select Batch:

データシート (281 KB) SDS (557 KB)

COA (253 KB) HNMR (501 KB) RP-HPLC (246 KB) LCMS (78 KB)

取扱説明書 (2659 KB)

参考文献

[1]. Coelmont L, et al. DEB025 (Alisporivir) inhibits hepatitis C virus replication by preventing a cyclophilin A induced cis-trans isomerisation in domain II of NS5A. PLoS One. 2010 Oct 27;5(10):e13687. [Content Brief]

[2]. Quarato G, et al. The cyclophilin inhibitor alisporivir prevents hepatitis C virus-mediated mitochondrial dysfunction. Hepatology. 2012 May;55(5):1333-43. [Content Brief]

[3]. de Wilde AH, et al. Alisporivir inhibits MERS- and SARS-coronavirus replication in cell culture, but not SARS-coronavirus infection in a mouse model. Virus Res. 2017 Jan 15;228:7-13. [Content Brief]

[4]. Esser-Nobis K, et al. The cyclophilin-inhibitor alisporivir stimulates antigen presentation thereby promoting antigen-specific CD8(+) T cell activation. J Hepatol. 2016 Jun;64(6):1305-14. [Content Brief]

細胞実験
^[2]

Alisporivir is prepared in DMSO at 4 mM and diluted in cell culture medium at the indicated concentrations (0.1, 0.2, 0.3, 0.4, 0.5 μM). UHCV-32 and UHCVcon-57.3 are U-2 OS human osteosar coma-derived cell lines inducibly expressing the entire open reading frame derived from the HCV H77 prototype and consensus clones, respectively. Cell viability is measured by trypan blue exclusion analysis^[2].

MedChemExpress (MCE) はこれらの方法の精度を確認していません。こちらは参照専用です。

参考文献

[1]. Coelmont L, et al. DEB025 (Alisporivir) inhibits hepatitis C virus replication by preventing a cyclophilin A induced cis-trans isomerisation in domain II of NS5A. PLoS One. 2010 Oct 27;5(10):e13687. [Content Brief]

[2]. Quarato G, et al. The cyclophilin inhibitor alisporivir prevents hepatitis C virus-mediated mitochondrial dysfunction. Hepatology. 2012 May;55(5):1333-43. [Content Brief]

[3]. de Wilde AH, et al. Alisporivir inhibits MERS- and SARS-coronavirus replication in cell culture, but not SARS-coronavirus infection in a mouse model. Virus Res. 2017 Jan 15;228:7-13. [Content Brief]

[4]. Esser-Nobis K, et al. The cyclophilin-inhibitor alisporivir stimulates antigen presentation thereby promoting antigen-specific CD8(+) T cell activation. J Hepatol. 2016 Jun;64(6):1305-14. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	0.8219 mL	4.1097 mL	8.2194 mL	20.5484 mL
	5 mM	0.1644 mL	0.8219 mL	1.6439 mL	4.1097 mL
	10 mM	0.0822 mL	0.4110 mL	0.8219 mL	2.0548 mL
	15 mM	0.0548 mL	0.2740 mL	0.5480 mL	1.3699 mL
	20 mM	0.0411 mL	0.2055 mL	0.4110 mL	1.0274 mL
	25 mM	0.0329 mL	0.1644 mL	0.3288 mL	0.8219 mL
	30 mM	0.0274 mL	0.1370 mL	0.2740 mL	0.6849 mL
	40 mM	0.0205 mL	0.1027 mL	0.2055 mL	0.5137 mL

Alisporivir Related Classifications

Infection

Molarity Calculator
Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

質量		濃度		体積		分子量 *
	=		×		×

The dilution calculator equation

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

一般には略語で表示されます：C₁V₁ = C₂V₂

濃度 _（開始）	×	体積 _（開始）	=	濃度 _（終了）	×	体積 _（終了）
	×		=		×
C1		V1		C2		V2

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Alisporivir254435-95-5Debio-025 DEB-025Debio025Debio 025DEB025DEB 025DEB-025CyclophilinHCVHepatitis C virusInhibitorinhibitorinhibit

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Alisporivir (Synonyms: Debio-025; DEB-025)

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•関連小分子:

•関連タンパク質:

Cyclophilin アイソフォーム固有の製品をすべて表示:

生物活性

プロトコル

純度とドキュメンテーション

参考文献

カスタマーレビュー

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Alisporivir Related Classifications

Molarity Calculator

Dilution Calculator

The molarity calculator equation

The dilution calculator equation

Keywords:

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Alisporivir (Synonyms: Debio-025; DEB-025)

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Alisporivir 関連抗体

顧客検証

おすすめ

•関連スクリーニングライブラリ:

•関連小分子:

•関連タンパク質:

Cyclophilin アイソフォーム固有の製品をすべて表示:

生物活性

プロトコル

純度とドキュメンテーション

参考文献

カスタマーレビュー

Alisporivir 関連抗体

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Alisporivir Related Classifications

Molarity Calculator

Dilution Calculator

The molarity calculator equation

The dilution calculator equation

Keywords:

最近チェックした製品:

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