2. GPCR/G Protein Neuronal Signaling
  3. CGRP Receptor
  4. 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.

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CLR/RAMP3-receptor antagonist-1

CLR/RAMP3-receptor antagonist-1 Chemical Structure

CAS No. : 2252341-45-8

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CLR/RAMP3-receptor antagonist-1 Related Antibodies

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Description

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[1].

In Vitro

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.

CLR/RAMP3-receptor antagonist-1 Related Antibodies

Cell Viability Assay[1]

Cell Line: human pancreatic cancer CFPAC-1 cells
Concentration: 3 μM
Incubation Time: 9 days (daily treatment)
Result: Decreased CFPAC-1 cell viability by up to 31% compared to vehicle-treated controls.
Parmacokinetics
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
In Vivo

CLR/RAMP3-receptor antagonist-1 (Compound 8) (20 mg/kg; i.p.; daily administration; for 30 consecutive days) significantly inhibits the growth of subcutaneous pancreatic xenografts in BALB/c nude mice after three weeks[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: BALB/c nude (female, 6-7 weeks old, 15-20g, subcutaneous xenograft model)[1]
Dosage: 20 mg/kg
Administration: i.p.; daily; until humane endpoint (about 30 days)
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.
Molecular Weight

525.64

Formula

C31H35N5O3
CAS No.
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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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CLR/RAMP3-receptor antagonist-1 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

CLR/RAMP3-receptor antagonist-12252341-45-8CGRP ReceptorCalcitonin gene-related peptide receptoradrenomedullin-1 receptorCFPAC-1 cellsCYP2D6BALB/c nude miceAM2 receptor178-2 BMA cellsCYP3A4CGRP receptorpancreatic cancerCLR/RAMP3 receptorInhibitorinhibitorinhibit

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