Maxadilan TFA
Based on 1 Customer Validation
Maxadilan TFA is a specific irreversible PAC1 receptor agonist and a potent vasodilator peptide present in the salivary glands of sand flies. Maxadilan TFA exhibits anti-apoptotic activity in hADSCs. Maxadilan TFA inhibits pro-inflammatory cytokines (TNF-α) and enhances anti-inflammatory mediators (IL-10). Maxadilan TFA can activate leukocytes and inhibit vascular permeability through PAC1 receptors. Maxadilan TFA promotes neural differentiation of human adipose-derived stem cells. Maxadilan TFA can be used to study endotoxin shock, atherosclerosis, and neurodegenerative diseases[1][2][3][4][5].
연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.
- Purity: 96.35%
- 화학식: C291H466N86O94S6·xC2HF3O2
- 분자량:6865.72 (free base)
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보관:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
Biological Activity
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PAC1 Receptor |
IL-1β |
Caspase 3 |
Caspase-9 |
TNF-α |
Maxadilan (20-200 nM, 24 h) TFA enhances the proliferation and migration of human adipose-derived stem cells (hADSCs), and enhances cytokine-induced neural redifferentiation of hADSCs into functional neurons[2].
Maxadilan (80 nM, 24-48 h) TFA decreases the ratio of apoptosis with serum withdrawal treatment in hADSCs through PAC1R ligand-dependent activity mediated by the PKA signaling pathway and PAC1R dimer-dependent activity mediated by the Wnt/β-catenin signaling pathway[2].
Maxadilan (80 nM, 1-3 days) TFA induces an efficient differentiation of hADSCs into neural-like cell morphology in chemical neural induction medium[2].
Maxadilan (5-100 ng/mL) TFA induces human neutrophil chemotaxis[3].
Maxadilan (134 nM, 30 min) TFA increases arteriolar dilation, associated with plasma leakage and leukocyte accumulation in one hamster cheek pouch[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:hADSC
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Concentration:80 nM
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Incubation Time:0 h, 12 h, 24 h
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Result:Reduced the wound area by 59.52% in 12 hours, completely reduced the wound area in 24 hours.
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Cell Line:hADSC
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Concentration:80 nM
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Incubation Time:24 h, 48 h
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Result:Reduced the ratio of JC-1-green/red.
Reduced the generation of Cleaved Caspase 3 and Caspase 9.
Maxadilan (0.137 mg/kg, i.p., 3 times a week) TFA reduces atherosclerosis in the aortic arch and brachiocephalic trunk of ApoE−/− mice under SC and CED with preserved or further enhanced hypercholesterolemia[1].
Maxadilan (0.137 mg/kg, i.p., once, 0-90 min) TFA increases blood sugar in NIH mice[4].
Maxadilan (0.172-0.343 mg/kg, i.p., once a day, 21 days) TFA increases body weight, reduces basal blood sugar, and promotes the increase of plasma insulin in NIH mice[4].
Maxadilan (0.5-10 μg, i.p., once) TFA reduces LPS (HY-D1056)-induced mortality in BALB/c mice[5].
Maxadilan (3 μg, i.p., once) TFA inhibits serum levels of TNF-4 while elevates IL-6 and IL-10 levels and prevents LPS-induced thrombocytopenia in LPS-induced BALB/c mice[5].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:ApoE−/− mice[1]
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Dosage:0.137 mg/kg
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Administration:i.p., 3 times a week
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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++++.
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Animal Model:Male NIH mice [4]
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Dosage:0.172 mg/kg, 0.343 mg/kg
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Administration:i.p., once a day, 21 days
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Result:Increased body weight, reduced basal blood sugar, and promoted the increase of plasma insulin.
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Animal Model:LPS-induced (500 μg, i.p., once) C57BL/6, BALB/c mice (Male 8-week-old) model[5]
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Dosage:0.1 μg, 1 μg, 10 μg, 3 μg
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Administration:i.p., once
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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.
Chemical Information
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Appearance Solid
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분자량 6865.72 (free base)
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화학식 C291H466N86O94S6·xC2HF3O2
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Color White to off-white
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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)
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Sequence Shortening
CDATCQFRKAIDDCQKQAHHSNVLQTSVQTTATFTSMDTSQLPGNSVFKECMKQKKKEFKA-NH2 (disulfide bridge:Cys1-Cys5, Cys14-Cys51)
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
용액&용해도
DMSO : 100 mg/mL (Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL; 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL; 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 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
순도&문서
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Data Sheet (313 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
[1]. Mey L, et al. PAC1 Agonist Maxadilan Reduces Atherosclerotic Lesions in Hypercholesterolemic ApoE-Deficient Mice. Int J Mol Sci. 2024 Dec 10;25(24):13245. [Content Brief]
[2]. Guo X, et al.PAC1R agonist maxadilan enhances hADSC viability and neural differentiation potential. J Cell Mol Med. 2016 May;20(5):874-90. [Content Brief]
[3]. Svensjö E, et al.Maxadilan, the Lutzomyia longipalpis vasodilator, drives plasma leakage via PAC1-CXCR1/2-pathway. Microvasc Res. 2012 Mar;83(2):185-93. [Content Brief]
[4]. .Yu R, et al. Long-term administration of maxadilan improves glucose tolerance and insulin sensitivity in mice. Peptides. 2008 Aug;29(8):1347-53. [Content Brief]
[5]. Bozza M, S et al The PACAP-type I receptor agonist maxadilan from sand fly saliva protects mice against lethal endotoxemia by a mechanism partially dependent on IL-10. Eur J Immunol. 1998 Oct;28(10):3120-7. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Maxadilan TFA Related Classifications
HY-P3483A Related Classifications
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