UPG-111
UPG-111 is a peptide compound that acts as a negative allosteric modulator of the Urotensin II receptor (UTR). UPG-111 exhibits a dual inhibitory effect on the vasoconstriction induced by UTR agonists - it reduces both the maximum response intensity and the sensitivity of the agonist. UPG-111 does not induce calcium release or cause contraction of the endothelium-deprived rat aortic rings. UPG-111 can be used for the study of various diseases related to the angiotensinergic system.
For research use only. We do not sell to patients.
- CAS No.: 3090687-02-5
- Formula: C64H87N13O17S2
- Molecular Weight:1374.58
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
Chemical Information
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CAS No. 3090687-02-5
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Molecular Weight 1374.58
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Formula C64H87N13O17S2
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Sequence
{hSer}-{TPED}-{Pen}-Phe-{d-Trp}-{Orn}-Tyr-Cys-Val (Disulfide bridge: Pen-Cys)
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Sequence Shortening
{hSer}-{TPED}-{Pen}-F-{d-Trp}-{Orn}-YCV (Disulfide bridge: Pen-Cys)
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocols
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Calcium Spark Assay
Calcium sparks are localized, transient increases in intracellular calcium concentration ([Ca2+]i) that occur in cardiac myocytes and represent elementary events underlying excitation-contraction coupling. These events are generated by the coordinated opening of clusters of ryanodine receptors (RyRs) on the sarcoplasmic reticulum membrane, leading to a brief release of Ca2+ into the cytosol. The detection and analysis of calcium sparks provide insights into the mechanisms of calcium handling and signaling in cardiac cells. Imaging techniques using fluorescent calcium indicators such as Fluo-3 are employed to visualize these subcellular calcium transients with high spatial and temporal resolution. The protocol is based on established methodologies described in primary literature for both experimental measurement and automated analysis of calcium sparks.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
UPG-111 Related Classifications
HY-P11259 Related Classifications
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Keywords
- UPG-111
- 3090687-02-5
- UPG111
- UPG 111
- Urotensin Receptor
- Urotensin II receptor (UTR) modulators
- Negative allosteric modulator (NAM)
- Lateral allostery
- GPCR multimeric model
- Structure-activity relationship (SAR)
- N-terminal peptide engineering
- Noncompetitive antagonism
- Calcium mobilization
- Rat aorta contraction
- Inhibitor
- inhibitor
- inhibit