标签归档：alisporivir

Alisporivir intermediate-1

发表于由

Alisporivir intermediate-1;

Alisporivir intermediate-1 是合成 Alisporivir 的中间体。Alisporivir 可用于研究炎症和病毒性疾病。

Alisporivir intermediate-1amp;;

Alisporivir intermediate-1 Chemical Structure

CAS No. : 882506-05-0

规格 价格 是否有货
1 mg ￥1900 询问价格 货期
5 mg ￥5900 询问价格 货期

* Please select Quantity before adding items.

生物活性

Alisporivir intermediate-1 is an intermediate in the synthesis of Alisporivir. Alisporivir is used for the treatment of inflammatory and viral diseases.

分子量

1461.91

Formula

C74H132N12O17
CAS 号

882506-05-0
Sequence Shortening

{d-Ala}-VVLA-{d-Ala}-LLV-{Aaa}-{Abu}
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
Solvent Solubility
In Vitro:;

H2O

Peptide Solubility and Storage Guidelines:

1.;;Calculate the length of the peptide.

2.;;Calculate the overall charge of the entire peptide according to the following table:

; Contents Assign value
Acidic amino acid Asp (D), Glu (E), and the C-terminal -COOH. -1
Basic amino acid Arg (R), Lys (K), His (H), and the N-terminal -NH2 +1
Neutral amino acid Gly (G), Ala (A), Leu (L), Ile (I), Val (V), Cys (C), Met (M), Thr (T), Ser (S), Phe (F), Tyr (Y), Trp (W), Pro (P), Asn (N), Gln (Q) 0

3.;;Recommended solution:

Overall charge of peptide Details
Negative (lt;0) 1.;;Try to dissolve the peptide in water first.
2.;;If water fails, add NH4OH (lt;50 μL).
3.;;If the peptide still does not dissolve, add DMSO (50-100 μL) to solubilize the peptide.
Positive (gt;0) 1.;;Try to dissolve the peptide in water first.
2.;;If water fails, try dissolving the peptide in a 10%-30% acetic acid solution.
3.;;If the peptide still does not dissolve, try dissolving the peptide in a small amount of DMSO.
Zero (=0) 1.;;Try to dissolve the peptide in organic solvent (acetonitrile, methanol, etc.) first.
2.;;For very hydrophobic peptides, try dissolving the peptide in a small amount of DMSO, and then dilute the solution with water to the desired concentration.
参考文献

  • [1]. Werkmeister S, et al. Hydrogenation of esters to alcohols with a well-defined iron complex. Angew Chem Int Ed Engl. 2014 Aug 11;53(33):8722-6.

Alisporivir(Synonyms: Debio-025 DEB-025)

发表于由

Alisporivir;(Synonyms: Debio-025; DEB-025) 纯度: 98.15%

Alisporivir (Debio-025) 是亲环蛋白抑制剂，具有高效的抗丙型肝炎病毒 (HCV) 活性的。

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

Alisporivir Chemical Structure

CAS No. : 254435-95-5

规格 价格 是否有货 数量
1 mg ￥7000 In-stock
5 mg ￥21000 In-stock
10 mg ; 询价 ;
50 mg ; 询价 ;

* Please select Quantity before adding items.

Alisporivir 相关产品

bull;相关化合物库:

  • Drug Repurposing Compound Library Plus
  • Clinical Compound Library Plus
  • Bioactive Compound Library Plus
  • Macrocyclic Compound Library
  • Peptide Library

生物活性

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

体外研究
(In Vitro)

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究
(In Vivo)

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

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial

分子量

1216.64

Formula

C63H113N11O12
CAS 号

254435-95-5
中文名称

阿拉泊韦
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Stored under nitrogen

Powder -80deg;C 2 years
-20deg;C 1 year

*In solvent : -80deg;C, 6 months; -20deg;C, 1 month (stored under nitrogen)
溶解性数据
In Vitro:;

DMSO : ≥ 100 mg/mL (82.19 mM)

* “≥” means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 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

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (stored under nitrogen)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 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，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制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

  • 1.

    请依序添加每种溶剂：;5% DMSO ;; 40% PEG300 ;; 5% Tween-80 ;; 50% saline

    Solubility: ≥ 2.62 mg/mL (2.15 mM); Clear solution

  • 2.

    请依序添加每种溶剂：;10% DMSO ;; 40% PEG300 ;; 5% Tween-80 ;; 45% saline

    Solubility: ≥ 2.5 mg/mL (2.05 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (2.05 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

*以上所有助溶剂都可在 MCE 网站选购。
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.

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

    [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.

    [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.
Cell Assay
[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].

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

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

    [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.

    [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.