Maxadilan
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].
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- No. CAS: 135374-80-0
- Fòrmula: C291H466N86O94S6
- Peso molecular:6865.72
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Almacenamiento:
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Actividad biológica
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Chemical Information
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Actividad biológica
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PAC1 Receptor |
IL-1β |
Caspase 3 |
Caspase-9 |
TNF-α |
Maxadilan (20-200 nM, 24 h) 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) 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) induces an efficient differentiation of hADSCs into neural-like cell morphology in chemical neural induction medium[2].
Maxadilan (5-100 ng/mL) induces human neutrophil chemotaxis[3].
Maxadilan (134 nM, 30 min) 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) 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) increases blood sugar in NIH mice[4].
Maxadilan (0.172-0.343 mg/kg, i.p., once a day, 21 days) 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) reduces LPS (HY-D1056)-induced mortality in BALB/c mice[5].
Maxadilan (3 μg, i.p., once) 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.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 135374-80-0
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Peso molecular 6865.72
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Fòrmula C291H466N86O94S6
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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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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
[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 Related Classifications
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