TRP-PK1
TRP-PK1 is a polypeptide. TRP-PK1 can be derived from the fourth transmembrane segment of TRPV4. TRP-PK1 can insert into the phospholipid bilayer. TRP-PK1 self-assembles to form K+-permeable channels, mediates K+ flux, hyperpolarizes the membrane potential of vascular smooth muscle, relaxes agonist-induced vasoconstriction, and lowers mean arterial pressure. TRP-PK1 enhances the tumor-targeting capability of cell membrane vesicles and displays Angiopep-2 (HY-P2341) on the surface of engineered vesicles. TRP-PK1 can be used for research on glioblastoma multiforme, head and neck cancer, and hypertension.
For research use only. We do not sell to patients.
- Formula: C132H199N29O29S2
- Molecular Weight:2720.30
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Description
IC50 & Target
[1]|
TRPV4 |
In Vitro
ANG-TRP-PK1@EAVs (25-200 μg; 24-48 h) exhibit no significant cytotoxicity in U87MG, U251, or L02 cells[1].
ANG-TRP-PK1@EAVs demonstrate specific targeting to U87MG glioma cells[1].
TRP-PK1 modification alone facilitates the uptake of RBCVs by HN4 cells[2].
TRP-PK1 (500 nM) self-assembles into cation-permeable ion channels with a conductance of 51.5 pS in giant liposome membranes, as measured by patch-clamp single-channel recording[3].
TRP-PK1 (5 μM) effectively mediates K+ flow into liposomes, as demonstrated by increased intravesicular PBFI fluorescence[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:U87MG, U251, L02
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Concentration:25, 50, 100, 200 μg (24 h); 50 μg (24 and 48 h)
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Incubation Time:24 h; 48 h
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Result:Showed no cytotoxicity in U87MG, U251, or L02 cells at concentrations of 25, 50, 100, and 200 μg for 24 h.
Showed no significant cell toxicity in U87MG, U251, and L02 cells at 50 μg for 48 h.
In Vivo
TRP-PK1 (1 mg/25 g; intravenous injection; single bolus injection; 10 min) significantly reduces mean arterial pressure in anesthetized mice[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c nude mice (female, approximately 7 weeks old, HN4 cell-derived xenograft model)[2]
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Dosage:2 mg/kg
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Administration:i.v.; once every three days
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Result:Showed tumor sizes comparable to the PBS control group.
Did not effectively reduce PCNA expression in tumor tissues compared to the control.
Showed no significant pathological changes in major organs including heart, liver, spleen, lungs, and kidneys.
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Animal Model:C57 mice (male, 4-6 weeks old, approximately 25 g)[3]
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Dosage:1 mg/25 g
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Administration:i.v.; single bolus injection; 10 min
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Result:Decreased mean arterial pressure (MAP) by approximately -4 mmHg compared to approximately -0.7 mmHg with DMSO control (n = 5).
Chemical Information
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Molecular Weight 2720.30
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Formula C132H199N29O29S2
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Sequence
Ala-Tyr-Leu-Ala-Val-Met-Val-Phe-Ala-Leu-Val-Leu-Gly-Trp-Met-Asn-Ala-Leu-Tyr-Phe-Thr-Arg-Gly-Leu
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Sequence Shortening
AYLAVMVFALVLGWMNALYFTRGL
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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.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)