CLR/RAMP3-receptor antagonist-1
CLR/RAMP3-receptor antagonist-1 is a selective antagonist of the CLR/RAMP3 receptor (CLR/RAMP3, AM2 receptor), with pIC50 values of 5.86, 9.21 and 9.07 against AM1 (CLR/RAMP2), AM2 (CLR/RAMP3) and CGRP (CLR/RAMP1) receptors, respectively. CLR/RAMP3-receptor antagonist-1 reduces the levels of pancreatic cancer progression markers, induces apoptosis in vitro, and prolongs survival in mouse models of pancreatic cancer. CLR/RAMP3-receptor antagonist-1 can be used in pancreatic cancer-related research.
For research use only. We do not sell to patients.
- CAS No.: 2252341-45-8
- Formula: C31H35N5O3
- Molecular Weight:525.64
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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
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
CLR/RAMP3-receptor antagonist-1 (Compound 8) (10-11 to 10-5 M; 30 min pre-incubation, 15 min agonist incubation) potently inhibits AM-induced cAMP production in human pancreatic cancer CFPAC-1 cells with a pIC50 of 8.96[1].
CLR/RAMP3-receptor antagonist-1 (Compound 8) (3 μM; 9 days daily treatment) reduces the viability of human pancreatic cancer CFPAC-1 cells by up to 31%[1].
CLR/RAMP3-receptor antagonist-1 (Compound 8) (100 nM-3 μM; 24 h) increases apoptosis in serum-starved human pancreatic cancer CFPAC-1 cells by up to 104% after 24 hours of treatment[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:human pancreatic cancer CFPAC-1 cells
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Concentration:3 μM
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Incubation Time:9 days (daily treatment)
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Result:Decreased CFPAC-1 cell viability by up to 31% compared to vehicle-treated controls.
| Species | Dose | Route | CLplasma | Vss | T1/2 (Elimination) |
|---|---|---|---|---|---|
| Rat[1] | 2.0 mg/kg | i.v. | 65.6 mL/min/kg | 16.8 L/kg | 5.2 h |
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 (female, 6-7 weeks old, 15-20g, subcutaneous xenograft model)[1]
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Dosage:20 mg/kg
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Administration:i.p.; daily; until humane endpoint (about 30 days)
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Result:Reduced tumor growth by 44% after three weeks compared to vehicle-treated controls.
Extended median survival to humane endpoint to 29.5 days compared to 21 days in vehicle-treated controls.
Maintained 50% survival rate at 28 days while all vehicle-treated mice were euthanized.
Showed no significant differences in body weight gain or adverse effects compared to controls.
Chemical Information
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CAS No. 2252341-45-8
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Molecular Weight 525.64
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Formula C31H35N5O3
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SMILES
O=C1[C@]2(CC3=CC(NC(CN(C(C(C)(C)C)=O)CC4=C(C=CC=C4)CNC)=O)=CC=C3C2)C5=CC=CN=C5N1
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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)
CLR/RAMP3-receptor antagonist-1 Related Classifications
HY-183142 Related Classifications
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