CGP 42112 (Synonyms: CGP42112A) |
| Catalog No.GC15406 |
CGP 42112 (CGP 42112A) es un potente agonista del receptor de angiotensina-II subtipo 2 (AT2 R).
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 127060-75-7
Sample solution is provided at 25 µL, 10mM.
_1-3.$$$39978408@51.jpg');)
_1-9.$$$38538795@65.jpg');)
_1-9.$$$39112701@51.jpg');)
_1-7.$$$37316672@70.jpg');)
_366-372.$$$36198801@70.jpg');)
.$$$38565142@65.jpg');)
_1867-1883.$$$33248023@67.jpg');)
_eads6055.$$$39977546@45.jpg');)
_eadm9805.$$$40080571@45.jpg');)
_eadj3020.$$$39666821@45.jpg');)
_1-20.$$$39757301@28.jpg');)
_1-24.$$$38898113@28.jpg');)
_273-287.$$$36806353@46.jpg');)
_1-16.$$$37156877@44.jpg');)
_1-19.$$$37460805@44.jpg');)
_1291-1307.$$$34518654@46.jpg');)
CGP 42112 is an effective angiotensin II subtype 2 receptor (AT2R) agonist [1]. AT2R plays a crucial role in the development of the kidney and exerts anti-proliferative, anti-fibrotic and pro-apoptotic effects in vivo [2]. CGP 42112 can be used for studies on isolated rat hearts and vascular endothelial function [3].
In vitro, treatment of NR8383 cells with CGP 42112 (2nM) for 6-24 hours can weaken the effect of lipopolysaccharide (LPS) on the cells, significantly reduce the expression of M1 polarization markers (including iNOS and TNF-α), and inhibit the expression of p-p65, p50, p-ERK1/2 and p-IκBα [4]. CGP 42112 (0.1-100μM) treated the renal proximal tubule suspension (1mg/ml) at 37°C for 30 minutes can inhibit NKA activity in a dose-dependent manner and increase the accumulation of cGMP in the proximal tubules [5].
In vivo, CGP 42112 (5, 10 and 20μg/kg, once every 3 days, total three times) administered by intra-articular injection to rats can significantly reduce the arthritis index of a single left hind paw. CGP 42112 can improve the histological signs of arthritis rats [6]. CGP 42112 (1mg/kg; once; i.p.) administered to ATla-deficient mice has no effect on the plasma aldosterone and corticosterone levels of the mice [7].
References:
[1] Takekoshi K, Ishii K, Isobe K, et al. Angiotensin-II subtype 2 receptor agonist (CGP-42112) inhibits catecholamine biosynthesis in cultured porcine adrenal medullary chromaffin cells[J]. Biochemical and Biophysical Research Communications, 2000, 272(2): 544-550.
[2] Elbaz N, Bedecs K, Masson M, et al. Functional trans-inactivation of insulin receptor kinase by growth-inhibitory angiotensin II AT2 receptor[J]. Molecular Endocrinology, 2000, 14(6): 795-804.
[3] Raffai G, Durand M J, Lombard J H. Acute and chronic angiotensin-(1–7) restores vasodilation and reduces oxidative stress in mesenteric arteries of salt-fed rats[J]. American Journal of Physiology-Heart and Circulatory Physiology, 2011, 301(4): H1341-H1352.
[4] Zheng X, Xu Z, Xu L, et al. Angiotensin II Type 2 receptor inhibits M1 polarization and apoptosis of alveolar macrophage and protects against mechanical ventilation-induced lung injury[J]. Inflammation, 2025, 48(1): 165-180.
[5] Hakam A C, Hussain T. Angiotensin II AT2 receptors inhibit proximal tubular Na+-K+-ATPase activity via a NO/cGMP-dependent pathway[J]. American Journal of Physiology-Renal Physiology, 2006, 290(6): F1430-F1436.
[6] Wang D, Hu S, Zhu J, et al. Angiotensin II type 2 receptor correlates with therapeutic effects of losartan in rats with adjuvant‐induced arthritis[J]. Journal of cellular and molecular medicine, 2013, 17(12): 1577-1587.
[7] Naruse M, Tanabe A, Sugaya T, et al. Deferential roles of angiotensin receptor subtypes in adrenocortical function in mice[J]. Life sciences, 1998, 63(18): 1593-1598.
| Cell experiment [1]: | |
Cell lines | NR8383 cells |
Preparation Method | Rat alveolar macrophages (NR8383) were cultured in F12K medium supplemented with 10% fetal bovine serum (FBS) and 1% penicillin/streptomycin. Cells were seeded on 6-well plates at a density of 4 × 106 cells/ml for Western blot, PCR and flow cytometry experiments. After 24h incubation, the cells were stimulated with DMSO medium, LPS (100ng/mL) 、AT2R activator CGP 42112 (2nM) 、AT2R inhibitor PD123319 (70nM) and AT1R inhibitor valsartan (100μM, CGP 48933) for 6h or 24h. In addition, the cells were mounted onto slides for fluorescent immunohistochemistry. |
Reaction Conditions | 2nM; 6h, 24h |
Applications | The AT2R agonist CGP 42112 can weaken the effect of LPS, significantly reducing the expression of M1 polarization markers (including iNOS and TNF-α), and simultaneously inhibiting the expressions of p-p65, p50, p-ERK1/2 and p-IκBα. |
| Animal experiment [2]: | |
Animal models | Sprague-Dawley rats |
Preparation Method | Adjuvant-induced arthritis (AIA) rats were randomly assigned to the following treatments: losartan (5, 10 and 15mg/kg/day, orally, once daily), MTX (0.5mg/kg, intraperitoneally, per 3 days), and vehicle (NS). Sham-operated rats received the vehicle (NS). The treatment started on day 14 after immunization and continued until day 28. After 15 days of treatment, on day 28, all rats were anesthetized with the chloral hydrate and killed (n = 6 per group). The serum, paw and spleen were collected for further study. To study the effects of AT2R agonist on rats with AIA, CGP 42112 (5, 10 and 20μg/kg, once every 3 days, total three times) and triamcinolone acetonide (1mg/kg, once every 3 days, total three times) were administered by intra-articular injection into the left hind (non-injected) paws following the onset of the secondary arthritis (n = 7 per group). Normal and model rats received NS instead. |
Dosage form | 5, 10 and 20μg/kg, once every 3 days, total three times; intra-articular injection |
Applications | Intra-articular injection of AIA rats with CGP 42112 (10 and 20μg/kg) significantly decreased the arthritis index of single left hind (non-injected) paw on days 22 and 26. |
References: | |
| Cas No. | 127060-75-7 | SDF | |
| Sinónimos | CGP42112A | ||
| Formula | C52H69N13O11 | M.Wt | 1052.2 |
| Solubility | DMF: 30 mg/ml,DMSO: 30 mg/ml,Ethanol: 30 mg/ml,PBS (pH 7.2): 10 mg/ml | Storage | Desiccate at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 950.4 μL | 4.7519 mL | 9.5039 mL |
| 5 mM | 190.1 μL | 950.4 μL | 1.9008 mL |
| 10 mM | 95 μL | 475.2 μL | 950.4 μL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 5 reference(s) in Google Scholar.)
GLPBIO products are for RESEARCH USE ONLY. Please make sure your review or question is research based.
Required fields are marked with *