1. GPCR/G Protein Apoptosis Stem Cell/Wnt TGF-beta/Smad Immunology/Inflammation
  2. PACAP Receptor Caspase Apoptosis PKA Interleukin Related TNF Receptor
  3. Maxadilan

Maxadilan 是一种特异性不可逆 PAC1 受体激动剂,也是一种存在于白蛉唾液腺中的强效血管扩张肽。Maxadilan 在 hADSCs 中表现出抗凋亡活性。Maxadilan 抑制促炎细胞因子 (TNF-α) 并增强抗炎介质 (IL-10)。Maxadilan 可通过 PAC1 受体,活化白细胞和抑制血管通透性。Maxadilan 促进人类脂肪干细胞的神经分化。Maxadilan 可用于研究内毒素休克、动脉粥样硬化和神经退行性疾病。

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Custom Peptide Synthesis

Maxadilan Chemical Structure

Maxadilan Chemical Structure

CAS No. : 135374-80-0

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Maxadilan is a specific irreversible PAC1 receptor agonist and a potent vasodilator peptide present in the salivary glands of sand flies. Maxadilan exhibits anti-apoptotic activity in hADSCs. Maxadilan inhibits pro-inflammatory cytokines (TNF-α) and enhances anti-inflammatory mediators (IL-10). Maxadilan can activate leukocytes and inhibit vascular permeability through PAC1 receptors. Maxadilan promotes neural differentiation of human adipose-derived stem cells. Maxadilan can be used to study endotoxin shock, atherosclerosis, and neurodegenerative diseases[1][2][3][4][5].

IC50 & Target[1][2][3][4][5]

PAC1 Receptor

 

IL-1β

 

Caspase 3

 

Caspase-9

 

TNF-α

 

体外研究
(In Vitro)

Maxadilan (20-200 nM,24 小时) 可增强人脂肪干细胞 (hADSC) 增殖并促进其迁移,并增强 hADSC 中细胞因子诱导的神经细胞再分化为功能性神经元[2]

Maxadilan (80 nM,24-48 小时) 通过 PKA 信号通路介导的 PAC1R 配体依赖性活性和 Wnt/β-catenin 信号通路介导的 PAC1R 二聚体依赖性活性,降低 hADSC 细胞凋亡率[2]

Maxadilan (80 nM) 在化学神经诱导培养基中诱导 hADSC 高效分化为神经样细胞形态[2]

Maxadilan (5-100 ng/mL) 可诱导人中性粒细胞趋化[3]

Maxadilan (134 nM,30 分钟) 可增加小动脉扩张,并伴有仓鼠颊囊内血浆渗漏和白细胞积聚[3]

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

Cell Migration Assay [2]

Cell Line: hADSC
Concentration: 80 nM
Incubation Time: 0 h, 12 h, 24 h
Result: Reduced the wound area by 59.52% in 12 hours, completely reduced the wound area in 24 hours.

Apoptosis Analysis[2]

Cell Line: hADSC
Concentration: 80 nM
Incubation Time: 24 h, 48 h
Result: Reduced the ratio of JC-1-green/red.
Reduced the generation of Cleaved Caspase 3 and Caspase 9.
体内研究
(In Vivo)

Maxadilan (20 nmol/kg,腹腔注射,每周 3 次) 减少 SC 和 CED 下的 ApoE−/− 小鼠的主动脉弓和头臂动脉干的动脉粥样硬化,同时保留或进一步增强高胆固醇血症[1]

Maxadilan (20 nmol/kg,腹腔注射,一次,0-90 分钟) 可升高 NIH 小鼠的血糖[4]

Maxadilan (25-50 nmol/kg,腹腔注射,每日一次,21 天) 可增加 NIH 小鼠的体重,降低基础血糖,并促进血浆胰岛素水平升高[4]

Maxadilan (0.5-10 μg,腹腔注射,一次) 可降低 LPS 诱导的 BALB/c 小鼠死亡率[5]

Maxadilan (3 μg,腹腔注射,一次) 抑制 LPS 诱导的 BALB/c 小鼠血清中 TNF-4 水平,同时升高 IL-6 和IL-10 水平并可以预防 LPS 诱发的血小板减少症[5]

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

Animal Model: ApoE−/− mice[1]
Dosage: 20 nmol/kg
Administration: i.p., 3 times a week
Result: Reduced atherosclerotic plaque frequency in the aortic arch and its branches under SC or CED.
Reduced Lumen Stenosis in BT.
Decreased plasma triglyceride levels and increased total and free cholesterol and body weight/tibia ratio.
Reduced TNF-α, IL-1β and caspase-3, and increased COX-2 areas++++.
Animal Model: Male NIH mice [4]
Dosage: 25 nmol/kg, 50 nmol/kg
Administration: i.p.,once a day, 21 days
Result: Increased body weight, reduced basal blood sugar, and promoted the increase of plasma insulin.
Animal Model: LPS-induced (500 μg, i.p., once) C57BL/6, BALB/c mice (Male 8-week-old) model[5]
Dosage: 0.1 μg, 1 μg, 10 μg,3 μg
Administration: i.p., once
Result: Reduced mortality, does not change in signs of endotoxemia, including piloerection, tremors, and lethargy at a concentration of 10 μg.
Abrogated thethrombocytopenia during the first hours after alethal challenge with LPS, revealed a twofold increase in bleeding time at 30 min at a concentration of 3 μg.
分子量

6865.72

Formula

C291H466N86O94S6

CAS 号
Sequence

Cys-Asp-Ala-Thr-Cys-Gln-Phe-Arg-Lys-Ala-Ile-Asp-Asp-Cys-Gln-Lys-Gln-Ala-His-His-Ser-Asn-Val-Leu-Gln-Thr-Ser-Val-Gln-Thr-Thr-Ala-Thr-Phe-Thr-Ser-Met-Asp-Thr-Ser-Gln-Leu-Pro-Gly-Asn-Ser-Val-Phe-Lys-Glu-Cys-Met-Lys-Gln-Lys-Lys-Lys-Glu-Phe-Lys-Ala-NH2 (Disulfide bridge:Cys1-Cys5, Cys14-Cys51)

Sequence Shortening

CDATCQFRKAIDDCQKQAHHSNVLQTSVQTTATFTSMDTSQLPGNSVFKECMKQKKKEFKA-NH2 (Disulfide bridge:Cys1-Cys5, Cys14-Cys51)

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.

纯度 & 产品资料
参考文献
  • 摩尔计算器

  • 稀释计算器

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

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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.

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Maxadilan
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