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Motesanib (AMG-706) is an orally bioavailable diphosphate salt of a multiple receptor tyrosine kinase inhibitor with potential antineoplastic activity[1]. This reagent selectively targets and inhibits VEGFR1/2/3(IC50: 2 nM /3 nM /6 nM), PDGFR (84nM), kit (8nM), and Ret (59nM)receptors, thereby inhibiting angiogenesis and cellular proliferation. Oral administration of AMG 706 potently inhibited VEGF-induced angiogenesis in the rat corneal model and induced regression of established A431 xenografts

June 21, 2017

prudect name : Motesanib (AMG-706) is an orally bioavailable diphosphate salt of a multiple receptor tyrosine kinase inhibitor with potential antineoplastic activity[1]. This reagent selectively targets and inhibits VEGFR1/2/3(IC50: 2…

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Prostacyclin (PGI2) is a potent vasorelaxant and inhibitor of platelet aggregation. It mediates its actions by binding to a specific G protein-coupled receptor, the IP receptor, on the surface of endothelial cells, arterial smooth muscle, and platelets.The IP receptor also participates in signal transduction of the pain response, cardioprotection, and inflammation.MRE-269 is the active form of the prodrug NS-304. It is a potent and selective agonist for the human IP receptor with a Ki value of 20 nM. In contrast to PGI2, which has a half-life of 30 seconds to a few minutes in vivo, plasma concentrations of MRE-269 remain near peak levels for more than eight hours in rats and dogs.Unlike the PGI2 analogues, beraprost and iloprost, MRE-269 lacks high affinity for the EP3 receptor.As a result, MRE-269 induces vasodilation equally in large and small pulmonary arteries, whereas vasodilation of small arteries by beraprost and iloprost is reduced via EP3-mediated vasoconstriction.Aristoff, P.A., Johnson, P.D., and Harrison, A.W. Synthesis of 9-substituted carbacyclin analogues. J Org Chem 48 5341-5348 (1983). Murata, T., Ushikubi, F., Matsuoka, T., et al. Altered pain perception and inflammatory response in mice lacking prostacyclin receptor. Nature 388 678-682 (1997). Cheng, Y., Austin, S.C., Rocca, B., et al. Role of prostacyclin in the cardiovascular response to thromboxane A2. Science 296 539-541 (2002). Cui, Y., Kataoka, Y., Satoh, T., et al. Protective effect of prostaglandin I2 analogs on ischemic delayed neuronal damage in gerbils. Biochem Biophys Res Commun 265 301-304 (1999). McLaughlin, V.V., Genthner, D.E., Panella, M.M., et al. Reduction in pulmonary vascular resistance with long-term epoprostenol (prostacyclin) therapy in primary pulmonary hypertension. N Engl J Med 338 273-277 (1998). Kuwano, K., Hashino, A., Asaki, T., et al. 2-{4-[(5,6-diphenylpyrazin-2-yl)(isopropyl)amino]butoxy}-N-(methylsulfonyl)acetamide (NS-304), an orally available and long-acting prostacyclin receptor agonist prodrug. J Pharmacol Exp Ther 322(3) 1181-1188 (2007).Kuwano, K., Hashino, A., Noda, K., et al. A long-acting and highly selective prostacyclin receptor agonist prodrug, 2-{4-[5,6-diphenylpyrazin-2-yl)(isopropyl)amino]butoxy}-N-(methylsulfonyl)acetamide (NS-304), ameliorates rat pulmonary hypertension with unique relaxant responses of its active form, {4-[5,6-diphenylpyrazin-2-yl)(isopropyl)amino]butoxy}acetic acid (MRE-269), on rat pulmonary artery. J Pharmacol Exp Ther 326(3) 691-699 (2008).

prudect name : Prostacyclin (PGI2) is a potent vasorelaxant and inhibitor of platelet aggregation. It mediates its actions by binding to a specific G protein-coupled receptor, the IP receptor, on…

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Monomethyl auristatin E (MMAE; Vedotin) is a hot topic in Antibody-drug conjugates (ADCs) studies. It is an antimitotic agent which inhibits cell division by blocking the polymerisation of tubulin.

prudect name : Monomethyl auristatin E (MMAE; Vedotin) is a hot topic in Antibody-drug conjugates (ADCs) studies. It is an antimitotic agent which inhibits cell division by blocking the polymerisation…

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prudect name : MRS 2578Synonyms: MRS 2578CAS NO: 711019-86-2Molecular Formula: C20H20N6S4Molecular Weight: 472.67Purity: 98% minSolubility:

prudect name : MRS 2578 Synonyms: MRS 2578CAS NO: 711019-86-2Molecular Formula: C20H20N6S4Molecular Weight: 472.67Purity: 98% minSolubility: In DMSOStorage: −20°C web site: www.medchemexpress.com References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/18528753

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Mirtazapine is antidepressants. Acting on central presynaptic a2 receptor antagonist, can enhance the adrenergic nerve conduction.

prudect name : Mirtazapine is antidepressants. Acting on central presynaptic a2 receptor antagonist, can enhance the adrenergic nerve conduction.Mirtazapine Synonyms: CAS NO: 61337-67-5Molecular Formula: C17H19N3Molecular Weight: 265.35Purity: ≥99%Solubility: Storage: airtight…

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prudect name : MK-0524Synonyms: LaropiprantCAS NO: 571170-77-9Molecular Formula: C21H19ClFNO4SMolecular Weight: 435.901Purity: 98% minSolubility: In DMSOStorage:

prudect name : MK-0524 Synonyms: LaropiprantCAS NO: 571170-77-9Molecular Formula: C21H19ClFNO4SMolecular Weight: 435.901Purity: 98% minSolubility: In DMSOStorage: −20°C web site: www.medchemexpress.com References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/18528685

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Meleagrin is a new FabI inhibitor from Penicillium chryosogenum. Bacterial enoyl-acyl carrier protein reductase (FabI) is a promising novel antibacterial target.

prudect name : Meleagrin is a new FabI inhibitor from Penicillium chryosogenum. Bacterial enoyl-acyl carrier protein reductase (FabI) is a promising novel antibacterial target.Meleagrin Synonyms: CAS NO: 71751-77-4Molecular Formula: C23H23N5O4Molecular…

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prudect name : MK-8245Synonyms: CAS NO: 1030612-87-3 Molecular Formula: C16H15BrFN7O3SMolecular Weight: 484.309Purity: 98% minSolubility: Storage:

prudect name : MK-8245 Synonyms: CAS NO: 1030612-87-3 Molecular Formula: C16H15BrFN7O3SMolecular Weight: 484.309Purity: 98% minSolubility: Storage: −20°C web site: www.medchemexpress.com References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/18528670

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2-[6-(Morpholin-4-yl)pyrimidin-4-yl]-4-(1H-1,2,3-triazol-1-yl)-1,2-dihydro-3H-pyrazol-3-one;

prudect name : 2-[6-(Morpholin-4-yl)pyrimidin-4-yl]-4-(1H-1,2,3-triazol-1-yl)-1,2-dihydro-3H-pyrazol-3-one;Molidustat;BAY85-3934 Synonyms: CAS NO: 1154028-82-6Molecular Formula: C13H14N8O2Molecular Weight: 314.30Purity: 98% minSolubility: In DMSOStorage: −20°C 2 years web site: www.medchemexpress.com References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/18528544

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MLN8237 (0.5 ¦ÌM) treatment causes the inhibition of colony formation of FLO-1, OE19, and OE33 esophageal adenocarinoma cell lines, and induces a significant increase in the percentage of polyploid cells, and subsequently an increase in the percentage of cells in the sub-G1 phase, which can be further enhanced in combination with cisplatin (2.5 ¦ÌM), involving the higher induction of TAp73¦Â, PUMA, NOXA, cleaved caspase-3, and cleaved PARP as compared with a single-agent treatment.

prudect name : MLN8237 (0.5 ¦ÌM) treatment causes the inhibition of colony formation of FLO-1, OE19, and OE33 esophageal adenocarinoma cell lines, and induces a significant increase in the percentage…

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