TACR1-IN-1
TACR1-IN-1 is a TACR1 inhibitor. TACR1-IN-1 attenuates Substance P-driven ERK phosphorylation and downstream malignant programs. TACR1-IN-1 reduces PGP9.5-positive tumor innervation in orthotopic PDAC models. TACR1-IN-1 increases antigen presentation and immune chemokine-related transcript expression under Substance P treatment conditions. TACR1-IN-1 reverses Substance P-associated reduction in Gemcitabine (HY-17026) sensitivity. TACR1-IN-1 can be used for research on pancreatic ductal adenocarcinoma.
For research use only. We do not sell to patients.
- CAS No.: 901730-21-0
- Formula: C23H24FN3O3
- Molecular Weight:409.45
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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
IC50 & Target
[1]|
NK1R |
In Vitro
TACR1-IN-1 (72 h) shows a stronger selective inhibitory effect on the viability of MIA PaCa-2 cells with high TACR1 expression than on PANC-1 cells with low TACR1 expression[1].
TACR1-IN-1 (0-72 h) preferentially inhibits Substance P (HY-P0201)-driven growth in MIA PaCa-2 cells with high TACR1 expression[1].
TACR1-IN-1 (0-48 h) inhibits Substance P-induced migration of MIA PaCa-2 cells[1].
TACR1-IN-1 (48 h) attenuates Substance P-driven ERK activation in MIA PaCa-2 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MIA PaCa-2; PANC-1
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Concentration:1 μM (SP); increasing concentrations (C547)
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Incubation Time:72 h
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Result:Showed the strongest inhibitory activity in MIA PaCa-2 cells among the tested compounds.
Showed limited effects in TACR1-low PANC-1 cells even at higher concentrations.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6J (male, 6-8 weeks)[1]
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Dosage:10 mg/kg
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Administration:i.p.; three times per week; starting on day 5 after tumor implantation
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Result:Reduced orthotopic pancreatic tumor growth and decreased tumor weight at end point.
Did not show an obvious reduction in body weight compared to vehicle-treated controls.
Did not reveal overt morphological abnormalities in major organs.
Reduced PGP9.5-positive nerve fiber density in tumor tissues compared with vehicle treatment.
Upregulated Cd3, Cd8a, Gzmb, Prf1, and other immune-activated genes in KPPC tumors.
Chemical Information
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CAS No. 901730-21-0
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Molecular Weight 409.45
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Formula C23H24FN3O3
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SMILES
FC1=CC=C(N2CCN(C(COC3=CC(N(CC)C4=CC=CC=C43)=O)=O)CC2)C=C1
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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)
TACR1-IN-1 Related Classifications
HY-189358 Related Classifications
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