WKYMVm |
| رقم الكتالوجGC16498 |
WKYMVm هو محفز قوي لمستقبل الببتيد النموذجي (FPR1) وFPRL1/2، ويعمل أيضًا على تنشيط تحلل فوسفوإينوزيتيد في خلايا HL-60 غير المتمايزة.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 187986-17-0
Sample solution is provided at 25 µL, 10mM.
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WKYMVm is a potent N-formyl peptide receptor (FPR1) and FPRL1/2 agonist, and also activate phosphoinositide hydrolysis in undifferentiated HL-60 cells.[1]
In vitro efficacy test indicated that treatment with 0.01, 0.1, 1 and 10 µmol/L WKYMVm for 24 hours or 48 hours obviouly suppressed RANKL‐induced mature osteoclasts.[3] In vitro, treatment with 10 μM WKYMVm to stimulate FPR2 can induce p47phox phosphorylation in IMR90 fibroblasts and in human lung cancer cells, which is considered the key event for NADPH oxidase-dependent superoxide generation. Moreover, 10 μM WKYMVm to stimulate also induced NADPH oxidase-dependent superoxide generation with maximal production occurring at 2 min.[6]
In vivo experiment it shown that treatment with 2.5- and 5 mg/kg/d daily over four days intraperitoneally in ALI mice decreased the levels of proinflammatory cytokines TNF-α, IL-6, and IL-1β, while it increased the MPO and NO release by differentiated HL-60 neutrophil-like cells.[2].
Intramuscular injection of 10−5 mol/l WKYMVm improves blood perfusion and provides protection from tissue damage in the ischemic hind limb.[4] In vivo, treatment with 8 mg/kg WKYMVm subcutaneously (at 0, 12, 24, 36, 48 and 60 h) effectively attenuated the DSS-induced increase in the bleeding score and the stool score and protects dextran sodium sulfate (DSS)-induced experimental ulcerative colitis.[5] In addition, administration of 4 mg/kg WKYMVm, to septic mice strongly increased neutrophil number through augmented emergency granulopoiesis[7].
References:
[1]. Christophe T, et al. The synthetic peptide Trp-Lys-Tyr-Met-Val-Met-NH2 specifically activates neutrophils through FPRL1/lipoxin A4 receptors and is an agonist for the orphan monocyte-expressed chemoattractant receptor FPRL2. J Biol Chem. 2001 Jun 15;276(24):21585-93.
[2]. Lee H, et al. WKYMVm ameliorates acute lung injury via neutrophil antimicrobial peptide derived STAT1/IRF1 pathway. Biochem Biophys Res Commun. 2020 Dec 10;533(3):313-318.
[3]. Hu J, et al. The protective effect of WKYMVm peptide on inflammatory osteolysis through regulating NF-κB and CD9/gp130/STAT3 signalling pathway. J Cell Mol Med. 2020 Jan;24(2):1893-1905.
[4]. Heo SC, et al. WKYMVm-induced activation of formyl peptide receptor 2 stimulates ischemic neovasculogenesis by promoting homing of endothelial colony-forming cells. Stem Cells. 2014 Mar;32(3):779-90.
[5]. Kim SD, et al. The immune-stimulating peptide WKYMVm has therapeutic effects against ulcerative colitis. Exp Mol Med. 2013 Sep 13;45(9):e40.
[6]. Cattaneo F, et al. WKYMVm-induced cross-talk between FPR2 and HGF receptor in human prostate epithelial cell line PNT1A. FEBS Lett. 2013 May 21;587(10):1536-42.
[7]. Kim HS, et al. Activation of formyl peptide receptor 2 by WKYMVm enhances emergency granulopoiesis through phospholipase C activity. BMB Rep. 2018 Aug;51(8):418-423.
| Cell experiment [1]: | |
Cell lines | human pulmonary microvascular endothelial cells |
Preparation Method | In the hydrogen peroxide (H2O2)-induced oxidative stress in lung cell assay, cells were exposed to 100 µM H2O2 with WKYMVm treatment. After incubation with WKYMVm for 24 hours in 96-well plates, the cell counting kit (CCK)-8 assay was carried out to determine the relative cell proliferation rate (%), according to the manufacturer’s instructions. |
Reaction Conditions | 100 µM, 24 h |
Applications | In human pulmonary microvascular endothelial cells (HULEC-5a) and primary murine pulmonary endothelial and epithelial cells, 1 and 100 µM WKYMVm treatments significantly increased proliferation in both the control and H2O2-exposed groups. |
| Animal experiment [2]: | |
Animal models | male C57/BL6J mice |
Preparation Method | A total of 20 male C57/BL6 mice, eight‐week‐old, were split randomly into four equal groups: sham, LPS, low‐dose WKYMVm (4 mg/kg bodyweight) and high‐dose WKYMVm (8 mg/kg bodyweight). The sham and LPS group were injected with PBS and LPS (5 mg/kg bodyweight), respectively. Predetermined WKYMVm doses were mixed with LPS and injected into the mice in combination. Injections were performed subcutaneously against the skull altogether 7 times with 48 hours intervals between applications. |
Dosage form | 4 mg/kg and 8 mg/kg;s.c. |
Applications | WKYMVm protected against LPS‐induced bone loss in vivo. |
References: | |
| Cas No. | 187986-17-0 | SDF | |
| Chemical Name | (S)-6-amino-2-((S)-2-amino-3-(1H-indol-3-yl)propanamido)-N-((5R,8S,11S,14S)-5-carbamoyl-15-(4-hydroxyphenyl)-8-isopropyl-11-(2-(methylthio)ethyl)-7,10,13-trioxo-2-thia-6,9,12-triazapentadecan-14-yl)hexanamide | ||
| Canonical SMILES | O=C([C@H](CCCCN)NC([C@H](CC1=CNC2=CC=CC=C12)N)=O)N[C@H](C(N[C@H](C(N[C@H](C(N[C@@H](C(N)=O)CCSC)=O)C(C)C)=O)CCSC)=O)CC(C=C3)=CC=C3O | ||
| Formula | C41H61N9O7S2 | M.Wt | 856.11 |
| الذوبان | Soluble to 2 mg/ml in Water | Storage | -20°C, protect from light |
| 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 | 1.1681 mL | 5.8404 mL | 11.6807 mL |
| 5 mM | 0.2336 mL | 1.1681 mL | 2.3361 mL |
| 10 mM | 0.1168 mL | 0.584 mL | 1.1681 mL |
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Quality Control & SDS
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- Purity: >99.50%
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Average Rating: 5 (Based on Reviews and 33 reference(s) in Google Scholar.)
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