Talogreptide vizaxetan
Based on 1 Customer Validation
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.
- Purity: 98.12%
- CAS No.: 1186600-65-6
- Formula: C78H118N20O19
- Molecular Weight:1639.89
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Storage:
Sealed storage, away from moisture.
Powder -80°C, 2 years , -20°C, 1 year* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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
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Solvent & Solubility
- 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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Appearance Solid
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Molecular Weight 1639.89
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Formula C78H118N20O19
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Color White to off-white
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Synonyms
RM2
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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
Sealed storage, away from moisture
Powder -80°C 2 years -20°C 1 year * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
DMSO : 100 mg/mL (60.98 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (1.52 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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Data Sheet (274 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 0.6098 mL | 3.0490 mL | 6.0980 mL | 15.2449 mL |
| 5 mM | 0.1220 mL | 0.6098 mL | 1.2196 mL | 3.0490 mL | |
| 10 mM | 0.0610 mL | 0.3049 mL | 0.6098 mL | 1.5245 mL | |
| 15 mM | 0.0407 mL | 0.2033 mL | 0.4065 mL | 1.0163 mL | |
| 20 mM | 0.0305 mL | 0.1524 mL | 0.3049 mL | 0.7622 mL | |
| 25 mM | 0.0244 mL | 0.1220 mL | 0.2439 mL | 0.6098 mL | |
| 30 mM | 0.0203 mL | 0.1016 mL | 0.2033 mL | 0.5082 mL | |
| 40 mM | 0.0152 mL | 0.0762 mL | 0.1524 mL | 0.3811 mL | |
| 50 mM | 0.0122 mL | 0.0610 mL | 0.1220 mL | 0.3049 mL | |
| 60 mM | 0.0102 mL | 0.0508 mL | 0.1016 mL | 0.2541 mL |
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