| Size | Price | Stock | Qty |
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| 2mg |
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| 5mg |
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Purity: ≥98%
CGP-42112(also known as CGP-42112A) is a novel, potent and selective Angiotensin-II subtype 2 receptor(AT2 R) agonist. Angiotensin II subtype 2 receptor (AT(2)-R) is highly expressed in adrenal medullary chromaffin cells. What is still unknown, though, are AT(2)-R's physiological functions in chromaffin cells. From the baseline, cGMP production was markedly inhibited by CGP42112 (>==1 nM). Both TH-synthesis and TH-enzyme activity control the activity of tyrosine hydroxylase (TH), a rate-limiting enzyme in the biosynthesis of catecholamines. From the baseline value, TH-enzyme activity was markedly inhibited by CGP42112 (>==1 nM). PD123319 (an AT(2)-R antagonist) eliminated the inhibitory effects of CGP42112 on TH-enzyme activity and cGMP production, whereas CV-11974 (an AT(1)-R antagonist) had no effect.
| ln Vitro |
CGP-42112 (≥1 nM) significantly reduces the basal value of cGMP production. From the basal value, CGP-42112 (≥1 nM) significantly inhibits TH-enzyme activity. PD123319 (an AT(2)-R antagonist) completely eliminates the inhibitory effects of CGP-42112 on TH-enzyme activity and cGMP production, whereas CV-11974 (an AT(1)-R antagonist) has no effect[1]. [1255I] CGP-42112 selectively binds to the subtype of angiotensin II receptor known as AT2. [1255I] Compared to the adrenal, the brain is where CGP-42112 binds more strongly. Although it does not change its binding in the adrenal gland, beta-Mercaptoethanol increased the binding of [1255I]CGP-42112 in the brain[2]. High affinity binding is observed for [1255I]CGP-42112 (Kd = 0.07-0.3 nM, depending on the region studied). [1255I]CGP-42112 binding is selective for AT2 receptors, as shown by the non-selective peptides Ang II and angiotensin III (Ang III) as well as competition from the AT2 ligands PD 123177, unlabeled CGP-42112, and losartan, the AT1 ligand[4].
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| ln Vivo |
The upper limit of CBF autoregulation was shifted toward higher blood pressures by intravenous infusions of PD 123319 (0.36 and 1 mg kg-1 min-1) and CGP-42112 (0.1 and 1 mg kg-1 min-1) without changing baseline CBF[3].
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| References |
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| Molecular Formula |
C52H69N13O11
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| Molecular Weight |
1052.19
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| Exact Mass |
1051.52
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| Elemental Analysis |
C, 59.36; H, 6.61; N, 17.31; O, 16.73
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| CAS # |
127060-75-7
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| Related CAS # |
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| Appearance |
Solid powder
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| SMILES |
CC[C@H](C)[C@@H](C(=O)O)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC2=CN=CN2)NC(=O)[C@H](CCCCNC(=O)[C@H](CCCN=C(N)N)NC(=O)OCC3=CC=CC=C3)NC(=O)[C@H](CC4=CC=C(C=C4)O)NC(=O)C5=CN=CC=C5
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| InChi Key |
UXGNARZDONUMMK-LRMQDCNJSA-N
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| InChi Code |
InChI=1S/C52H69N13O11/c1-3-32(2)43(50(73)74)64-48(71)42-17-11-25-65(42)49(72)41(27-36-29-56-31-59-36)62-46(69)39(60-47(70)40(26-33-18-20-37(66)21-19-33)61-44(67)35-14-9-22-55-28-35)15-7-8-23-57-45(68)38(16-10-24-58-51(53)54)63-52(75)76-30-34-12-5-4-6-13-34/h4-6,9,12-14,18-22,28-29,31-32,38-43,66H,3,7-8,10-11,15-17,23-27,30H2,1-2H3,(H,56,59)(H,57,68)(H,60,70)(H,61,67)(H,62,69)(H,63,75)(H,64,71)(H,73,74)(H4,53,54,58)/t32-,38-,39-,40-,41-,42-,43-/m0/s1
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| Chemical Name |
(2S,3S)-2-[[(2S)-1-[(2S)-2-[[(2S)-6-[[(2S)-5-(diaminomethylideneamino)-2-(phenylmethoxycarbonylamino)pentanoyl]amino]-2-[[(2S)-3-(4-hydroxyphenyl)-2-(pyridine-3-carbonylamino)propanoyl]amino]hexanoyl]amino]-3-(1H-imidazol-5-yl)propanoyl]pyrrolidine-2-carbonyl]amino]-3-methylpentanoic acid
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| Synonyms |
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| HS Tariff Code |
2934.99.03.00
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (2.38 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 2.5 mg/mL (2.38 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: 2.5 mg/mL (2.38 mM) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 0.9504 mL | 4.7520 mL | 9.5040 mL | |
| 5 mM | 0.1901 mL | 0.9504 mL | 1.9008 mL | |
| 10 mM | 0.0950 mL | 0.4752 mL | 0.9504 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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