WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H697737
CAS#: 127060-75-7
Description: Cgp 42112A is a hexapeptide analog of angiotensin II; activation of Receptor, Angiotensin, Type 2 results in vasodilation.
Hodoodo Cat#: H697737
Name: Cgp 42112A
CAS#: 127060-75-7
Chemical Formula: C52H69N13O11
Exact Mass: 1,051.52
Molecular Weight: 1,052.200
Elemental Analysis: C, 59.36; H, 6.61; N, 17.31; O, 16.73
Synonym: Cgp 42112A; Cgp-42112A; Cgp42112A; Cgp 42112B; Cgp-42112B; Cgp42112B; CGP-42112; CGP 42112; CGP42112;
IUPAC/Chemical Name: N6-(((benzyloxy)carbonyl)-L-arginyl)-N2-(nicotinoyl-L-tyrosyl)-L-lysyl-L-histidyl-L-prolyl-L-isoleucine
InChi Key: UXGNARZDONUMMK-LRMQDCNJSA-N
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
SMILES Code: 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(O)C=C4)NC(C5=CC=CN=C5)=O)=O)=O)=O)CCC1)=O
Appearance: Solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO
Shelf Life: >3 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.03.00
More Info:
| Biological target: | |
| In vitro activity: | |
| In vivo activity: |
The following data is based on the product molecular weight 1,052.20 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
| Formulation protocol: | |
| In vitro protocol: | |
| In vivo protocol: |
1: Braszko JJ, Kułakowska A, Karwowska-Polecka W. CGP 42112A antagonism of the angiotensin II and angiotensin II(3-7) facilitation of recall in rats. Pharmacol Res. 1998 Dec;38(6):461-8. PubMed PMID: 9990655.
2: Braszko JJ, Kułakowska A, Winnicka MM, Karwowska-Polecka W. CGP 42112A abolishes facilitation of recognition caused by angiotensin II and angiotensin II(3-7) in rats. Acta Neurobiol Exp (Wars). 1997;57(3):227-34. PubMed PMID: 9407709.
3: Hines J, Heerding JN, Fluharty SJ, Yee DK. Identification of angiotensin II type 2 (AT2) receptor domains mediating high-affinity CGP 42112A binding and receptor activation. J Pharmacol Exp Ther. 2001 Aug;298(2):665-73. PubMed PMID: 11454929.
4: Whitebread SE, Taylor V, Bottari SP, Kamber B, de Gasparo M. Radioiodinated CGP 42112A: a novel high affinity and highly selective ligand for the characterization of angiotensin AT2 receptors. Biochem Biophys Res Commun. 1991 Dec 31;181(3):1365-71. PubMed PMID: 1764088.
5: Ewert S, Laesser M, Johansson B, Holm M, Aneman A, Fandriks L. The angiotensin II receptor type 2 agonist CGP 42112A stimulates NO production in the porcine jejunal mucosa. BMC Pharmacol. 2003 Mar 4;3:2. Epub 2003 Mar 4. PubMed PMID: 12689346; PubMed Central PMCID: PMC153509.
6: Heemskerk FM, Zorad S, Seltzer A, Saavedra JM. Characterization of brain angiotensin II AT2 receptor subtype using [125I] CGP 42112A. Neuroreport. 1993 Jan;4(1):103-5. PubMed PMID: 8453029.
7: Pechlivanova DM, Markova PP, Popov D, Stoynev AG. The role of the angiotensin AT2 receptor on the diurnal variations of nociception and motor coordination in rats. Peptides. 2013 Jan;39:152-6. doi: 10.1016/j.peptides.2012.11.011. Epub 2012 Nov 28. PubMed PMID: 23201312.
8: Sabuhi R, Asghar M, Hussain T. Inhibition of NAD(P)H oxidase potentiates AT2 receptor agonist-induced natriuresis in Sprague-Dawley rats. Am J Physiol Renal Physiol. 2010 Oct;299(4):F815-20. doi: 10.1152/ajprenal.00310.2010. Epub 2010 Jul 28. PubMed PMID: 20668101; PubMed Central PMCID: PMC2957256.
9: Gao S, Park BM, Cha SA, Park WH, Park BH, Kim SH. Angiotensin AT2 receptor agonist stimulates high stretch induced- ANP secretion via PI3K/NO/sGC/PKG/pathway. Peptides. 2013 Sep;47:36-44. doi: 10.1016/j.peptides.2013.06.008. Epub 2013 Jun 18. PubMed PMID: 23791669.
10: Jaiswal N, Tallant EA, Jaiswal RK, Diz DI, Ferrario CM. Differential regulation of prostaglandin synthesis by angiotensin peptides in porcine aortic smooth muscle cells: subtypes of angiotensin receptors involved. J Pharmacol Exp Ther. 1993 May;265(2):664-73. PubMed PMID: 8496814.
11: Taguchi K, Matsumoto T, Kamata K, Kobayashi T. Angiotensin II type 2 receptor-dependent increase in nitric oxide synthase activity in the endothelium of db/db mice is mediated via a MEK pathway. Pharmacol Res. 2012 Jul;66(1):41-50. doi: 10.1016/j.phrs.2012.02.010. Epub 2012 Mar 22. PubMed PMID: 22465219.
12: Sabuhi R, Ali Q, Asghar M, Al-Zamily NR, Hussain T. Role of the angiotensin II AT2 receptor in inflammation and oxidative stress: opposing effects in lean and obese Zucker rats. Am J Physiol Renal Physiol. 2011 Mar;300(3):F700-6. doi: 10.1152/ajprenal.00616.2010. Epub 2011 Jan 5. PubMed PMID: 21209001; PubMed Central PMCID: PMC3064141.
13: Luo H, Wang X, Chen C, Wang J, Zou X, Li C, Xu Z, Yang X, Shi W, Zeng C. Oxidative stress causes imbalance of renal renin angiotensin system (RAS) components and hypertension in obese Zucker rats. J Am Heart Assoc. 2015 Feb 16;4(2). pii: e001559. doi: 10.1161/JAHA.114.001559. PubMed PMID: 25687731; PubMed Central PMCID: PMC4345876.
14: Egidy G, Friedman J, Viswanathan M, Wahl LM, Saavedra JM. CGP-42112 partially activates human monocytes and reduces their stimulation by lipopolysaccharides. Am J Physiol. 1997 Sep;273(3 Pt 1):C826-33. PubMed PMID: 9316402.
15: López RM, Castillo MC, López JS, Guevara G, López P, Castillo EF. Activation of upregulated angiotensin II type 2 receptors decreases carotid pulse pressure in rats with suprarenal abdominal aortic coarctation. Clin Exp Hypertens. 2015;37(4):271-9. doi: 10.3109/10641963.2014.954714. Epub 2014 Oct 1. PubMed PMID: 25271908.
16: Lu J, Wu L, Jiang T, Wang Y, Zhao H, Gao Q, Pan Y, Tian Y, Zhang Y. Angiotensin AT2 receptor stimulation inhibits activation of NADPH oxidase and ameliorates oxidative stress in rotenone model of Parkinson's disease in CATH.a cells. Neurotoxicol Teratol. 2015 Jan-Feb;47:16-24. doi: 10.1016/j.ntt.2014.11.004. Epub 2014 Nov 14. PubMed PMID: 25446015.
17: Gong WK, Lü J, Wang F, Wang B, Wang MY, Huang HP. Effects of angiotensin type 2 receptor on secretion of the locus coeruleus in stress-induced hypertension rats. Brain Res Bull. 2015 Feb;111:62-8. doi: 10.1016/j.brainresbull.2014.12.011. Epub 2015 Jan 3. PubMed PMID: 25562714.
18: Pechlivanova DM, Stoynev AG. Effect of chronic treatment with angiotensin receptor ligands on water-salt balance in Wistar and spontaneously hypertensive rats. Folia Med (Plovdiv). 2013 Jul-Dec;55(3-4):63-9. PubMed PMID: 24712284.
19: Heemskerk FM, Saavedra JM. Quantitative autoradiography of angiotensin II AT2 receptors with [125I]CGP 42112. Brain Res. 1995 Apr 17;677(1):29-38. PubMed PMID: 7606467.
20: 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. PubMed PMID: 8469773.
