标签归档：pol

Balixafortide TFA(Synonyms: POL6326 TFA)

发表于由

Balixafortide TFA;(Synonyms: POL6326 TFA) 纯度: 98.19%

Balixafortide TFA (POL6326 TFA) 是一种有效的，选择性的，耐受性好的肽类 CXCR4 拮抗剂，其 IC50 小于 10 nM。Balixafortide TFA 对 CXCR4 的选择性比包括 CXCR7 在内的许多受体高出 1000 倍。Balixafortide TFA 以 IC50 < 10 nM 阻断 β-arrestin 募集和钙通量。Balixafortide TFA 还是一种有效的造血干细胞和祖细胞 (HSPC) 动员剂，并具有抗癌作用。

Balixafortide TFAamp;;(Synonyms: POL6326 TFA)

Balixafortide TFA Chemical Structure

规格 价格 是否有货 数量
5 mg ￥1700 In-stock
25 mg ￥6200 In-stock
50 mg ￥10500 In-stock
100 mg ; 询价 ;
200 mg ; 询价 ;

* Please select Quantity before adding items.

Balixafortide TFA 相关产品

bull;相关化合物库:

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

生物活性

Balixafortide TFA (POL6326 TFA) is a potent, selective, well-tolerated peptidic CXCR4 antagonist with an IC50 < 10 nM. Balixafortide TFA shows 1000-fold selective for CXCR4 than a large panel of receptors including CXCR7. Balixafortide TFA blocks β-arrestin recruitment and calcium flux with IC50s < 10 nM. Balixafortide TFA is also a potent hematopoietic stem and progenitor cell (HSPC) mobilizing agent. Anti-cancer effects[1][2].

IC50 Target[1]

CXCR4

lt;10 nM (IC50)

体外研究
(In Vitro)

Balixafortide potently inhibits pERK / pAKT signaling in the lymphoma lines Namalwa (IC50< 200 nM) and Jurkat (IC50 < 400 nM). Balixafortide efficiently blocks SDF-1 dependent chemotaxis of MDA MB 231 breast cancer cells (IC50 < 20 nM), Namalwa and Jurkat cells (IC50 < 10 nM)[1].

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

Balixafortide is optimized for favorable mouse absorption, distribution, metabolism and excretion (ADME) properties with balanced plasma protein binding, greater plasma and microsomal stability[1].

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

分子量

1978.16

Formula

C86H119F3N24O23S2
Sequence

Cyclo(Ala-Cys-Ser-Ala-Pro-{Dab}-Arg-Tyr-Cys-Tyr-Gln-Lys-Pro-Pro-Tyr-His)(Disulfide bridge: Cys2-Cys9)
Sequence Shortening

Cyclo(ACSAP-{Dab}-RYCYQKPPYH)(Disulfide bridge: Cys2-Cys9)
运输条件

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

Sealed storage, away from moisture and light

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

*In solvent : -80deg;C, 6 months; -20deg;C, 1 month (sealed storage, away from moisture and light)
溶解性数据
In Vitro:;

H2O : 100 mg/mL (50.55 mM; Need ultrasonic)

DMSO : 100 mg/mL (50.55 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 0.5055 mL 2.5276 mL 5.0552 mL
5 mM 0.1011 mL 0.5055 mL 1.0110 mL
10 mM 0.0506 mL 0.2528 mL 0.5055 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 (sealed storage, away from moisture and light)。-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：;10% DMSO ;; 40% PEG300 ;; 5% Tween-80 ;; 45% saline

    Solubility: ≥ 2.5 mg/mL (1.26 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (1.26 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

  • 2.

    请依序添加每种溶剂：;10% DMSO ;; 90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (1.26 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (1.26 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 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
  • 3.

    请依序添加每种溶剂：;10% DMSO ;; 90% corn oil

    Solubility: ≥ 2.5 mg/mL (1.26 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (1.26 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在 MCE 网站选购。
参考文献

  • [1]. Zimmermann J, et al. Anti-tumor cell activity and in vitro profile of the next generation CXCR4 antagonist Balixafortide. Ann Oncol. 2018 Oct;29 Suppl 8:viii103.

    [2]. Karpova D, et al. Mobilization of hematopoietic stem cells with the novel CXCR4 antagonist POL6326 (balixafortide) in healthy volunteers-results of a dose escalation trial. J Transl Med. 2017 Jan 3;15(1):2.

Murepavadin TFA(Synonyms: POL7080 TFA)

发表于由

Murepavadin TFA;(Synonyms: POL7080 TFA) 纯度: 99.07%

Murepavadin TFA (POL7080 TFA) 是一种14氨基酸环肽，是一种强效、特异性的抗生素，可用于 Pseudomonas aeruginosa 引起的细菌感染的研究。Murepavadin TFA 靶向作用于脂多糖转运蛋白 portin D。

Murepavadin TFA&nbsp;(Synonyms: POL7080 TFA)

Murepavadin TFA Chemical Structure

规格 价格 是否有货 数量
5 mg ￥3500 In-stock
10 mg ￥5500 In-stock
50 mg ￥16500 In-stock
100 mg ￥22500 In-stock
200 mg ; 询价 ;
500 mg ; 询价 ;

* Please select Quantity before adding items.

Murepavadin TFA 相关产品

•相关化合物库:

  • Drug Repurposing Compound Library Plus
  • Clinical Compound Library Plus
  • Bioactive Compound Library Plus
  • Anti-Infection Compound Library
  • Clinical Compound Library
  • Drug Repurposing Compound Library
  • Antibacterial Compound Library
  • Anti-COVID-19 Compound Library
  • Antibiotics Library
  • Peptide Library

生物活性

Murepavadin (TFA), a 14-amino-acid cyclic peptide, is a highly potent, specific antibiotic for the treatment of bacterial infections caused by Pseudomonas aeruginosa. Murepavadin (TFA) targets the lipopolysaccharide transport portin D [1].

IC50 & Target

P. aeruginosa[1].
Clinical Trial

分子量

1667.83

Formula

C73H112N22O16.C2HF3O2
Sequence Shortening

Cyclo(AS-{d-Pro}-PTWI-{Dab}-{Orn}-{d-Dab}-{Dab}-W-{Dab}-{Dab})
运输条件

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

Sealed storage, away from moisture

Powder -80°C 2 years
-20°C 1 year

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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 (<0) 1.;;Try to dissolve the peptide in water first.
2.;;If water fails, add NH4OH (<50 μL).
3.;;If the peptide still does not dissolve, add DMSO (50-100 μL) to solubilize the peptide.
Positive (>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]. Matteo Bassetti, et al. New antibiotics for ventilator-associated pneumonia. Curr Opin Infect Dis. 2018 Jan 13.

Lonodelestat(Synonyms: POL6014)

发表于由

Lonodelestat;(Synonyms: POL6014)

Lonodelestat (POL6014) 是有效的、具有口服活性的、选择性的人中性粒细胞弹性蛋白酶(hNE) 的肽类抑制剂。

Lonodelestatamp;;(Synonyms: POL6014)

Lonodelestat Chemical Structure

CAS No. : 906547-89-5

规格 是否有货
100 mg ; 询价 ;
250 mg ; 询价 ;
500 mg ; 询价 ;

* Please select Quantity before adding items.

生物活性

Lonodelestat (POL6014) is a potent, orally active and selective peptide inhibitor of human neutrophil elastase (hNE)[1][2].

体内研究
(In Vivo)

Lonodelestat (POL6014) significantly and efficiently reduced the inflammatory processes of ALI in HNE treated mice[1].
Lonodelestat (POL6014, 0.1, 0.5, 2 and 10 mg/kg, intranasally administered) dose-dependently and significantly reduces the number of macrophages, epithelial cells, neutrophils and lymphocytes recovered in BAL. The maximum inhibition was reached at 2 mg/kg in reducing neutrophils by 65% (p<0.001), epithelial cells by 68% (p<0.001), macrophages by 33% (p<0.001) and lymphocytes by 77% (p<0.001)[1].

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

Animal Model: Ten-week-old male C57BL/6j mice[1].
Dosage: 0.05, 0.2, 0.5 and 5 mg/kg.
Administration: Administered intranasally (i.n.) 15 minutes before HNE (30 UI, i.n.).
Result: Reduced the inflammatory processes of ALI in HNE treated mice.

分子量

1478.73

Formula

C71H111N15O19
CAS 号

906547-89-5
Sequence Shortening

cyclo[ASIPPQKYPPNle(bu)ET]
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.
参考文献

  • [1]. Lagente V, et al. A novel Protein Epitope Mimetic (PEM) neutrophil elastase (NE) inhibitor, POL6014, inhibits human NE-induced acute lung injury in mice. ATS, San Diego, May 15-20, 2009.

    [2]. Odile Sellier-Kessler, et al. Inhibition of lung inflammation by a protein epitope mimetic (PEM) neutrophil elastase inhibitor, POL6014, in a sub-chronic tobacco smoke (TS) model in mice. European Respiratory Journal 2013 42: 1762.

Balixafortide(Synonyms: POL6326)

发表于由

Balixafortide;(Synonyms: POL6326)

Balixafortide (POL6326) 是一种有效的，选择性的，耐受性好的肽类 CXCR4 拮抗剂，其 IC50 小于 10 nM。Balixafortide 对 CXCR4 的选择性比包括 CXCR7 在内的许多受体高出 1000 倍。Balixafortide 以 IC50 < 10 nM 阻断 β-arrestin 募集和钙通量。Balixafortide 还是一种有效的造血干细胞和祖细胞 (HSPC) 动员剂，并具有抗癌作用。

Balixafortideamp;;(Synonyms: POL6326)

Balixafortide Chemical Structure

CAS No. : 1051366-32-5

规格 是否有货
100 mg ; 询价 ;
250 mg ; 询价 ;
500 mg ; 询价 ;

* Please select Quantity before adding items.

Balixafortide 的其他形式现货产品:

Balixafortide TFA

生物活性

Balixafortide (POL6326) is a potent, selective, well-tolerated peptidic CXCR4 antagonist with an IC50 < 10 nM. Balixafortide shows 1000-fold selective for CXCR4 than a large panel of receptors including CXCR7. Balixafortide blocks β-arrestin recruitment and calcium flux with IC50s < 10 nM. Balixafortide is also a potent hematopoietic stem and progenitor cell (HSPC) mobilizing agent. Anti-cancer effects[1][2].

IC50 Target[1]

CXCR4

lt;10 nM (IC50)

体外研究
(In Vitro)

Balixafortide potently inhibits pERK / pAKT signaling in the lymphoma lines Namalwa (IC50< 200 nM) and Jurkat (IC50 < 400 nM). Balixafortide efficiently blocks SDF-1 dependent chemotaxis of MDA MB 231 breast cancer cells (IC50 < 20 nM), Namalwa and Jurkat cells (IC50 < 10 nM)[1].

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

Balixafortide is optimized for favorable mouse absorption, distribution, metabolism and excretion (ADME) properties with balanced plasma protein binding, greater plasma and microsomal stability[1].

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

分子量

1864.14

Formula

C84H118N24O21S2
CAS 号

1051366-32-5
Sequence

Cyclo(Ala-Cys-Ser-Ala-Pro-{Dab}-Arg-Tyr-Cys-Tyr-Gln-Lys-Pro-Pro-Tyr-His) (Disulfide bridge: Cys2-Cys9)
Sequence Shortening

Cyclo(ACSAP-{Dab}-RYCYQKPPYH) (Disulfide bridge: Cys2-Cys9)
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.
参考文献

  • [1]. Zimmermann J, et al. Anti-tumor cell activity and in vitro profile of the next generation CXCR4 antagonist Balixafortide. Ann Oncol. 2018 Oct;29 Suppl 8:viii103.

    [2]. Karpova D, et al. Mobilization of hematopoietic stem cells with the novel CXCR4 antagonist POL6326 (balixafortide) in healthy volunteers-results of a dose escalation trial. J Transl Med. 2017 Jan 3;15(1):2.