UCUF-965
UCUF-965 is a CXCR4 positive allosteric modulator. UCUF-965 potentiates CXCL12-induced β-arrestin recruitment and cAMP signaling, activates lymphoblast migration, induces calcium flux, and does not bind CXCR4’s orthosteric CXCL12 site. UCUF-965 reduces miR-15b and miR-29a levels, increases miR-146a levels in fibroblasts. UCUF-965 enhances angiogenesis and reduces wound healing time in diabetic mice. UCUF-965 can be used for the research of diabetic wound healing impairment.
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- CAS No.: 2965316-77-0
- Formule: C22H23N5OS
- Masse moléculaire:405.52
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
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Activité biologique
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CXCR4 |
UCUF-965 (0.1-10 μM) promotes β-arrestin recruitment with an EC50 of 0.02 μM[1].
UCUF-965 acts as a partial agonist of CXCR4-mediated cAMP inhibition in CXCR4-overexpressing CHO cells, with an EC50 of 0.05 μM[1].
UCUF-965 (0.4 μM; 3 h) induces migration of CEM-CCRF human lymphoblast cells via CXCR4 activation, with an EC50 of 0.4 μM[1].
UCUF-965 (10 μM) induces CXCR4-mediated calcium flux in CEM-CCRF human lymphoblast cells[1].
UCUF-965 (0.1-10 μM; 24 h) modulates the expression of wound healing-related microRNAs in murine diabetic and non-diabetic fibroblasts, reducing miR-15b and miR-29a levels and increasing miR-146a levels[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:CEM-CCRF human lymphoblast cells
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Concentration:0.4 μM
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Incubation Time:3 h
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Result:Induced CEM-CCRF cell migration with an EC50 of 0.4 μM and an average Eₘₐₓ of 31%.
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Cell Line:murine diabetic (Db/Db) fibroblasts; murine non-diabetic (HZ) fibroblasts
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Concentration:0.1, 1, 10 μM
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Incubation Time:24 h
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Result:Decreased the expression of miR-15b in both diabetic and non-diabetic fibroblasts in a dose-dependent manner.
Decreased miR-29a levels and increased miR-146a levels in both cell types, with responses observed at concentrations as low as 0.1 μM.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Db/Db mice (10-week-old female, diabetic model)[1]
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Dosage:10 μM
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Administration:intradermal injection; single dose (immediately after wounding)
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Result:Reduced wound surface area compared to controls starting at post-injury day 6.
Achieved full wound closure at day 14, representing a 36% reduction in wound healing time compared to day 22 in PBS-treated controls.
Showed a significant increase in CD31-positive endothelial cells at day 7 post-wounding, reaching levels similar to non-diabetic control wounds.
Chemical Information
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CAS No. 2965316-77-0
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Masse moléculaire 405.52
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Formule C22H23N5OS
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SMILES
N=1N=C(C=2C=CC=CC2OCC)N3N=C(C=4C=CC(=CC4)N5CCCC5)CSC13
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
UCUF-965 Related Classifications
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