CGP-42112
Based on 2 publication(s) in Google Scholar
CGP-42112 (CGP-42112A) is a potent Angiotensin-II subtype 2 receptor(AT2 R) agonist.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 99.84%
- CAS. Nr.: 127060-75-7
- Formel: C52H69N13O11
- Molecular Weight:1052.19
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Publications Citing Use of MedChemExpress (MCE) CGP-42112
MoreAlle Angiotensin Receptor Isoform-spezifische Produkte anzeigen
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Biologische Aktivität
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AT2 Receptor |
AT1 Receptor |
CGP-42112 (≥1 nM) significantly inhibits cGMP production from the basal value. CGP-42112 (≥1 nM) significantly inhibits TH-enzyme activity from the basal value. These inhibitory effects of CGP-42112 on TH-enzyme activity and-cGMP production are abolished by PD123319 (AT(2)-R antagonist) while CV-11974 (AT(1)-R antagonist) is ineffective[1]. [125I]CGP-42112 binds selectively to the AT2 angiotensin II receptor subtype. [125I]CGP-42112 binds with higher affinity in the brain than in the adrenal. beta-Mercaptoethanol enhanced [125I]CGP-42112 binding in the brain, but does not alter its binding in the adrenal[2]. [125I]CGP-42112 binds with high affinity (Kd = 0.07-0.3 nM, depending on the area studied). [125I]CGP-42112 binding is selective for AT2 receptors, as determined by lack of competition with the AT1 ligand losartan, and competition by the AT2 ligands PD 123177 and unlabeled CGP-42112 and the non-selective peptides Ang II and angiotensin III (Ang III)[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS. Nr. 127060-75-7
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Appearance Solid
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Molecular Weight 1052.19
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Formel C52H69N13O11
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Color White to off-white
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SMILES
CC[C@H](C)[C@@H](C(O)=O)NC([C@H]1N(C([C@H](CC2=CNC=N2)NC([C@H](CCCCNC([C@H](CCCNC(N)=N)NC(OCC3=CC=CC=C3)=O)=O)NC([C@H](CC4=CC=C(C=C4)O)NC(C5=CC=CN=C5)=O)=O)=O)=O)CCC1)=O
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Synonyms
CGP42112A
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (2)
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Journal Impact Factor
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Most Recent
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Cancer Cell
Reduction of Liver Metastasis Stiffness Improves Response to Bevacizumab in Metastatic Colorectal Cancer. [Abstract]2020 Jun 8;37(6):800-817.e7. PMID: 32516590 -
Sci Rep
AT1 and AT2 receptors modulate renal tubular cell necroptosis in angiotensin II-infused renal injury mice. [Abstract]2019 Dec 19;9(1):19450. PMID: 31857626
Lösungsmittel & Löslichkeit
DMSO : 100 mg/mL (95.04 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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 (2.38 mM); Clear solution; Need ultrasonic
This protocol yields a clear solution of 2.5 mg/mL.
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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (2.38 mM); Clear solution; Need ultrasonic
This protocol yields a clear solution of 2.5 mg/mL.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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.
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.
Reinheit & Dokumentation
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Data Sheet (282 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
Verweise
[1]. Takekoshi K, et al. Angiotensin-II subtype 2 receptor agonist (CGP-42112) inhibits catecholamine biosynthesis in cultured porcine adrenal medullary chromaffin cells. Biochem Biophys Res Commun. 2000 Jun 7;272(2):544-50. [Content Brief]
[2]. Speth RC. [125I]CGP 42112 binding reveals differences between rat brain and adrenal AT2 receptor binding sites. Regul Pept. 1993 Mar 19;44(2):189-97. [Content Brief]
[3]. Naveri L, et al. Angiotensin II AT2 receptor stimulation extends the upper limit of cerebral blood flow autoregulation: agonist effects of CGP 42112 and PD 123319. J Cereb Blood Flow Metab. 1994 Jan;14(1):38-44. [Content Brief]
[4]. Heemskerk FM, et al. Quantitative autoradiography of angiotensin II AT2 receptors with [125I]CGP 42112. Brain Res. 1995 Apr 17;677(1):29-38. [Content Brief]
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 0.9504 mL | 4.7520 mL | 9.5040 mL | 23.7600 mL |
| 5 mM | 0.1901 mL | 0.9504 mL | 1.9008 mL | 4.7520 mL | |
| 10 mM | 0.0950 mL | 0.4752 mL | 0.9504 mL | 2.3760 mL | |
| 15 mM | 0.0634 mL | 0.3168 mL | 0.6336 mL | 1.5840 mL | |
| 20 mM | 0.0475 mL | 0.2376 mL | 0.4752 mL | 1.1880 mL | |
| 25 mM | 0.0380 mL | 0.1901 mL | 0.3802 mL | 0.9504 mL | |
| 30 mM | 0.0317 mL | 0.1584 mL | 0.3168 mL | 0.7920 mL | |
| 40 mM | 0.0238 mL | 0.1188 mL | 0.2376 mL | 0.5940 mL | |
| 50 mM | 0.0190 mL | 0.0950 mL | 0.1901 mL | 0.4752 mL | |
| 60 mM | 0.0158 mL | 0.0792 mL | 0.1584 mL | 0.3960 mL | |
| 80 mM | 0.0119 mL | 0.0594 mL | 0.1188 mL | 0.2970 mL |
CGP-42112 Related Classifications
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