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PG 106

* Please kindly note that our products are not to be used for therapeutic purposes and cannot be sold to patients.

PG 106 is a selective human melanocortin receptor 3 (hMC3R) antagonist (IC50 = 210 nM), with no activity at hMC4 receptors and hMC5 receptors. PG 106 may be used to differentiate the substructural features responsible for selectivity at the hMC3R, hMC4R, and hMC5R.

Category
Peptide Inhibitors
Catalog number
BAT-010359
CAS number
944111-22-2
Molecular Formula
C51H69N13O9
Molecular Weight
1008.19
PG 106
IUPAC Name
(3S,6S,9R,16S,24S)-16-(2-acetamidohexanoylamino)-6-[3-(diaminomethylideneamino)propyl]-3-(1H-indol-3-ylmethyl)-9-(naphthalen-2-ylmethyl)-2,5,8,11,15,18-hexaoxo-1,4,7,10,14,19-hexazacyclotetracosane-24-carboxamide
Synonyms
PG106; PG-106; Ac-DL-Nle-Asp(1)-bAla-D-2Nal-Arg-Trp-Lys(1)-NH2; N-Acetyl-L-norleucyl-L-α-aspartyl-β-alanyl-3-(2-naphthalenyl)-D-alanyl-L-arginyl-L-tryptophyl-L-Lysinamide(2→7)-lactam; Ac-Nle-cyclo(-Asp-β-Ala-D-2-Nal-Arg-Trp-Lys)-NH2
Appearance
White Lyophilized Solid
Purity
>98%
Density
1.40±0.1 g/cm3 at 20°C, 760 mmHg
Sequence
XDXXRWK (Modifications: X-1 = Ac-Nle, X-3 = beta-Ala, X-4 = D-2-Nal, Lys-7 = C-terminal amide, Asp-2, Lys-7, Cyclized)
Storage
Store at -20°C
Solubility
Soluble in Ethanol, Water
InChI
InChI=1S/C51H69N13O9/c1-3-4-15-38(59-30(2)65)47(70)64-42-28-44(67)55-22-10-9-17-37(45(52)68)61-50(73)41(27-34-29-58-36-16-8-7-14-35(34)36)63-48(71)39(18-11-23-57-51(53)54)62-49(72)40(60-43(66)21-24-56-46(42)69)26-31-19-20-32-12-5-6-13-33(32)25-31/h5-8,12-14,16,19-20,25,29,37-42,58H,3-4,9-11,15,17-18,21-24,26-28H2,1-2H3,(H2,52,68)(H,55,67)(H,56,69)(H,59,65)(H,60,66)(H,61,73)(H,62,72)(H,63,71)(H,64,70)(H4,53,54,57)/t37-,38?,39-,40+,41-,42-/m0/s1
InChI Key
ZFZDDBJAFMOQSH-JHMPFZGISA-N
Canonical SMILES
CCCCC(C(=O)NC1CC(=O)NCCCCC(NC(=O)C(NC(=O)C(NC(=O)C(NC(=O)CCNC1=O)CC2=CC3=CC=CC=C3C=C2)CCCN=C(N)N)CC4=CNC5=CC=CC=C54)C(=O)N)NC(=O)C
1. REVIEWS
New Phytol . 1987 Aug;106(4):785-790. doi: 10.1111/j.1469-8137.1987.tb00179.x.
Books reviewed in this article: Techniques in Photomorphogenesis. Ed. by H. Smith and M. G. Holmes Reaction-Diffusion Equations and their Applications to Biology. By N. F. Britton Somaclonal Variations and Crop Improvement. Advances in Agricultural Biotechnology (Series). Ed. by J. Semal The Cytoskeleton: Cell Function and Organization (Journal of Cell Science, Supplement 5). Ed. by C. W. Lloyd, J. S. Hyams and R. M. Warn Membranes, Metabolism, and Dry Organisms. Ed. by A. Carl Leopold Water Fungi and Plants. Ed. by P. G. Ayres and L. Boddy The Rhizosphere. By E. A. Curl and B. Truelove Symbiosis. An Introduction to Biological Associations. By V. Ahmadjian and S. Paracer.
2. A systematic review of biomarkers in Takotsubo syndrome: A focus on better understanding the pathophysiology
Hassan Abbas,David Gamble,Amelia Rudd,Alice Mezincescu,Dana Dawson,Hilal Khan Int J Cardiol Heart Vasc . 2021 May 19;34:100795. doi: 10.1016/j.ijcha.2021.100795.
Background:The diagnosis of Takotsubo syndrome is made based on clinical presentation, ECG, biomarker, imaging and coronary angiography. There is a lack of diagnostic biomarkers that can discriminate patients with Takotsubo syndrome from those with acute myocardial infarction (AMI) and provide clinical monitoring and prognostic information in the long-term.Methods:A literature search of published Takotsubo syndrome biomarkers from PubMed was performed. All studies that included numerical biomarker data on Takotsubo syndrome was included. Exclusion criteria was any study without an AMI cohort for comparison in the acute phase biomarkers or due to the absence of numerical values. The results were tabulated in table form with results expressed as either mean ± SD or median (interquartile range).Results:The literature search produced 14 relevant studies that met search criteria.The results showed; high sensitivity Troponin I (3.21 ± 4.4 vs 34.4 ± 37 ng/ml), BNP [972 (578.5-1671.0) pg/L vs 358 (50.5-688.0) pg/L in NSTEMI and vs 381 (106.0-934.0) pg/L in STEMI] and BNP/Troponin I ratio [642 (331.8-1226.5) vs 184.5 (50.5-372.3) pg/ug in NSTEMI and 7.5 (2.0-29.6) pg/ug in STEMI] patients.Discussion:This study is limited by many studies being retrospective cohort studies. This data shows that acutely troponin is raised in Takotsubo syndrome but not enough to be discriminating from AMI. BNP level is significantly raised in Takotsubo syndrome compared to AMI.Conclusion:Current specificity of acute and chronic biomarkers for Takotsubo syndrome is lacking and further work is needed to address the gap in knowledge.
3. Associations of immunological features with COVID-19 severity: a systematic review and meta-analysis
Xiaodong Zhu,Shunfang Liu,Hua Qin,Junhui Hu,Chen Gong,Chunli Zhang,Jinjin Huang,Zhicheng Zhang,Liping Chen,Guo Ai BMC Infect Dis . 2021 Aug 3;21(1):738. doi: 10.1186/s12879-021-06457-1.
Background:COVID-19 has spread widely worldwide, causing millions of deaths. We aim to explore the association of immunological features with COVID-19 severity.Methods:We conducted a meta-analysis to estimate mean difference (MD) of immune cells and cytokines levels with COVID-19 severity in PubMed, Web of Science, Scopus, the Cochrane Library and the grey literature.Results:A total of 21 studies with 2033 COVID-19 patients were included. Compared with mild cases, severe cases showed significantly lower levels of immune cells including CD3+T cell (× 106, MD, - 413.87; 95%CI, - 611.39 to - 216.34), CD4+T cell (× 106, MD, - 203.56; 95%CI, - 277.94 to - 129.18), CD8+T cell (× 106, MD, - 128.88; 95%CI, - 163.97 to - 93.79), B cell (× 106/L; MD, - 23.87; 95%CI, - 43.97 to - 3.78) and NK cell (× 106/L; MD, - 57.12; 95%CI, - 81.18 to - 33.06), and significantly higher levels of cytokines including TNF-α (pg/ml; MD, 0.34; 95%CI, 0.09 to 0.59), IL-5 (pg/ml; MD, 14.2; 95%CI, 3.99 to 24.4), IL-6 (pg/ml; MD, 13.07; 95%CI, 9.80 to 16.35), and IL-10 (pg/ml; MD, 2.04; 95%CI, 1.32 to 2.75), and significantly higher levels of chemokines as MCP-1 (SMD, 3.41; 95%CI, 2.42 to 4.40), IP-10 (SMD, 2.82; 95%CI, 1.20 to 4.45) and eotaxin (SMD, 1.55; 95%CI, 0.05 to 3.05). However, no significant difference was found in other indicators such as Treg cell (× 106, MD, - 0.13; 95%CI, - 1.40 to 1.14), CD4+/CD8+ratio (MD, 0.26; 95%CI, - 0.02 to 0.55), IFN-γ (pg/ml; MD, 0.26; 95%CI, - 0.05 to 0.56), IL-2 (pg/ml; MD, 0.05; 95%CI, - 0.49 to 0.60), IL-4 (pg/ml; MD, - 0.03; 95%CI, - 0.68 to 0.62), GM-CSF (SMD, 0.44; 95%CI, - 0.46 to 1.35), and RANTES (SMD, 0.94; 95%CI, - 2.88 to 4.75).Conclusion:Our meta-analysis revealed significantly lower levels of immune cells (CD3+T, CD4+T, CD8+T, B and NK cells), higher levels of cytokines (TNF-α, IL-5, IL-6 and IL-10) and higher levels of chemokines (MCP-1, IP-10 and eotaxin) in severe cases in comparison to mild cases of COVID-19. Measurement of immunological features could help assess disease severity for effective triage of COVID-19 patients.
4. Association between serum soluble Toll-like receptor 2 and 4 and the risk of breast cancer
Ahmed Gowily,Ghada El-Kharashy,Tarek Okda,Maha Houssen Mol Clin Oncol . 2021 Feb;14(2):38. doi: 10.3892/mco.2020.2200.
Soluble Toll-like receptor (sTLR) 2 and 4 are endogenous negative regulators of TLR2 and TLR4 signaling. Therefore, the present study aimed to determine the serum levels of sTLR2 and 4, and to investigate the association between their levels and the clinicopathological parameters of patients with breast cancer. A total of 100 female patients with breast cancer (50 non-metastatic and 50 metastatic), as well as 50 healthy control volunteers were enrolled in the present study, and serum levels of sTLR2 and 4 were determined by ELISA. A significant increase in serum sTLR2 was detected in patients with non-metastatic (2,258.2±1,832.44 pg/ml) and metastatic (5,997.4±8,585.23 pg/ml) breast cancer, compared with the control group (1,106.8± 99.93 pg/ml; P=0.0001). A significant increase in serum sTLR4 was also detected in patients with both non-metastatic (1,945.2±1,709.53 pg/ml) and metastatic breast cancer (7,800.1±13,041.28 pg/ml), compared with the control group (1,106.8±108.32 pg/ml; P=0.0001). Furthermore, a positive correlation was observed between the levels of serum sTLR4 and 2 and clinicopathological parameters, such as progesterone receptor and estrogen receptor expression. In conclusion, sTLR2 and sTLR4 may be potential biomarkers of breast cancer susceptibility.
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