RM2
RM2 is a GRPr antagonist. RM2 selectively binds to GRPr, blocks agonist-induced receptor internalization, and inhibits agonist-triggered intracellular calcium mobilization. RM2 can be used in studies related to prostate cancer.
For research use only. We do not sell to patients.
- CAS No.: 1186600-65-6
- Formula: C78H118N20O19
- Molecular Weight:1639.89
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
RM2 binds the GRP receptor on human prostate carcinoma cryostat sections with high affinity, exhibiting an IC50 of 7.7nmol/L[1].
RM2 is a selective ligand for the GRP receptor on human tissue sections, with an IC50 of 9.3 nmol/L and no measurable affinity for NMBr or BB3r subtypes[1].
RM2 (1000 nmol/L; 30 min) acts as a GRP receptor antagonist in HEK-GRPr cells, failing to trigger receptor internalization at 1000 nmol/L but completely inhibiting Bombesin (HY-P0195)-induced receptor internalization at the same concentration[1].
RM2 (1-10 μmol/L; 60 s) acts as a GRP receptor antagonist in PC-3 cells, showing no intrinsic activity on intracellular Ca2+ mobilization at 1 or 10 μmol/L, but inhibiting Bombesin (HY-P0195)-induced Ca2+ mobilization at 10 μmol/L[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HEK293 cells stably expressing HA epitope-tagged human GRPr (HEK-GRPr cells)
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Concentration:1000 nmol/L
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Incubation Time:30 min
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Result:Failed to stimulate GRP receptor internalization.
Prevented bombesin-induced GRP receptor internalization when co-treated with 10 nmol/L Bombesin.
68Ga-RM2 (80 pmol; intravenous injection) exhibits high, GRPr-specific uptake in PC-3 prostate cancer xenografts, with tumour to kidney ratios reaching 6.1 at 80 minutes post-injection[1].
68Ga-RM2 (80 pmol; intravenous injection) achieves specific, GRPr-mediated uptake in androgen-dependent LNCaP prostate cancer xenografts, with tumour to blood ratios reaching 23.4 at 120 minutes post-injection[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 1186600-65-6
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Molecular Weight 1639.89
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Formula C78H118N20O19
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Sequence
DOTA-{2-(4-aminopiperidin-1-yl)acetic acid}-{DPhe}-Gln-Trp-Ala-Val-Gly-His-{Sta}-Leu-NH2
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Sequence Shortening
DOTA-{2-(4-aminopiperidin-1-yl)acetic acid}-{DPhe}-QWAVGH-{Sta}-L-NH2
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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)
RM2 Related Classifications
HY-P11769 Related Classifications
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