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MPEP is a selective antagonist for the metabotropic glutamate receptor subtype 5 (mGluR5) with IC50 of 36 nM. MPEP is a significantly more potent antagonist derived by structural derivatization around SIB-1757 and SIB-1893. MPEP has no agonist or antagonist activities at the human mGlu1b receptor expressed in CHO-K1 cells at concentrations up to 30 ¦ÌM. When tested at group II and III receptors, MPEP does not show agonist or antagonist activity at 100 ¦ÌM on human mGlu2, -3, -4a, -7b, and -8a receptors nor at 10 ¦ÌM on the human mGlu6 receptor.

June 21, 2017

prudect name : MPEP is a selective antagonist for the metabotropic glutamate receptor subtype 5 (mGluR5) with IC50 of 36 nM. MPEP is a significantly more potent antagonist derived by…

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MEK162 (ARRY-162) is an oral, highly selective MEK inhibitor. In preclinical studies, MEK162 showed significant antitumor activities in cell lines and animal models. MEK162 is now being investigated in Phase I trials in advanced solid tumors. Recent research confirms that the MEK pathway acts as a central axis in the proliferation of different tumors including melanoma, non-small cell lung, head/neck and pancreatic cancers. And MEK inhibition, either alone or in combination with other agents, is an important therapeutic strategy in treating cancer. ARRY-162 is a novel, orally active, potent, selective, non-ATP-competitive inhibitor of MEK 1 / 2 that has the potential to treat a range of malignant diseases.

prudect name : MEK162 (ARRY-162) is an oral, highly selective MEK inhibitor. In preclinical studies, MEK162 showed significant antitumor activities in cell lines and animal models. MEK162 is now being…

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Maxacalcitol (22-Oxacalcitriol) is non-calcemic vitamin D3 analog and ligand of VDR-like receptors.

prudect name : Maxacalcitol (22-Oxacalcitriol) is non-calcemic vitamin D3 analog and ligand of VDR-like receptors.Maxacalcitol Synonyms: CAS NO: 103909-75-7Molecular Formula: C26H42O4Molecular Weight: 418.61Purity: 98% minSolubility: In DMSOStorage: -20 oC web…

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MG132 is a potent cell-permeable proteasome and calpain inhibitor with IC50 of 0.1 and 1.2 ¦ÌM for the inhibition of proteasome and calpain, respectively. The Ki of MG132 is 4 nM. MG132 inhibits TNF-¦Á-induced NF-¦ÊB activation and I¦ÊB¦Á degradation with an IC50 of 3 µM and prevents ¦Â-secretase cleavage. MG132 induces neurite outgrowth in PC12 cells and has anticancer properties in vitro. MG132 reduces the degradation of ubiquitin-conjugated proteins in mammalian cells and permeable strains of yeast by the 26S complex without affecting its ATPase or isopeptidase activities. MG132 activates c-Jun N-terminal kinase (JNK1), which initiates apoptosis.

prudect name : MG132 is a potent cell-permeable proteasome and calpain inhibitor with IC50 of 0.1 and 1.2 ¦ÌM for the inhibition of proteasome and calpain, respectively. The Ki of…

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L-663,536;1-[(4-CHLOROPHENYL)METHYL]-3-[(1,1-DIMETHYLETHYL)THIO]-ALPHA,ALPHA-DIMETHYL-5-(1-METHYLETHYL)-1H-INDOLE-2-PROPANOIC ACID;MK-886;3-[tert-Butylthio-1-(4-chlorobenzyl)-5-isopropyl-1H-indol-2-yl]-2,2-dimethylpropionic Acid, Sodium Salt;1-[(4-Chlorophenyl)methyl]-3-[(1,1-dimethylethyl)thio]-alpha,alpha-dimethyl-5-(1-methylethyl)-1H-indole-2-propanoic acid;3-[1-(4-Chlorobenzyl)-3-(tert-butylthio)-5-isopropyl-1H-indol-2-yl]-2,2-dimethylpropanoic acid;3-[1-(4-Chlorobenzyl)-3-(tert-butylthio)-5-isopropyl-1H-indol-2-yl]-2,2-dimethylpropionic acid;3-[3-tert-Butylthio-1-(4-chlorobenzyl)-5-isopropyl-1H-indol-2-yl]-2,2-dimethylpropionic acid

prudect name : L-663,536;1-[(4-CHLOROPHENYL)METHYL]-3-[(1,1-DIMETHYLETHYL)THIO]-ALPHA,ALPHA-DIMETHYL-5-(1-METHYLETHYL)-1H-INDOLE-2-PROPANOIC ACID;MK-886;3-[tert-Butylthio-1-(4-chlorobenzyl)-5-isopropyl-1H-indol-2-yl]-2,2-dimethylpropionic Acid, Sodium Salt;1-[(4-Chlorophenyl)methyl]-3-[(1,1-dimethylethyl)thio]-alpha,alpha-dimethyl-5-(1-methylethyl)-1H-indole-2-propanoic acid;3-[1-(4-Chlorobenzyl)-3-(tert-butylthio)-5-isopropyl-1H-indol-2-yl]-2,2-dimethylpropanoic acid;3-[1-(4-Chlorobenzyl)-3-(tert-butylthio)-5-isopropyl-1H-indol-2-yl]-2,2-dimethylpropionic acid;3-[3-tert-Butylthio-1-(4-chlorobenzyl)-5-isopropyl-1H-indol-2-yl]-2,2-dimethylpropionic acidMK-886 Synonyms: L-663,536CAS NO: 118414-82-7Molecular Formula: C27H33ClNO2S.NaMolecular Weight: 494.07Purity: 98% minSolubility: In DMSOStorage: −20°C web site: www.medchemexpress.com References PubMed…

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MK-0752 is a potent gamma secretase (¦Ã-secretase) inhibitor in clinical development with an IC50 of 5 nM for A¦Â40 in human SH-SY5Y cells.Defining the metabolic fate of amyloid precursor protein (APP) in the central nerve system (CNS) is critically important for the development of ¦Ã-secretase inhibitors to treat Alzheimer¡¯s disease (AD), as a substrate build-up of APP fragments could potentially lead to an overshoot in neurotoxic amyloid peptides. The lack of A¦Â rebound in the CNS could be attributed to the shunting of APP (possibly beta C-terminal fragments, e.g. C99) to ¦Ã-secretase independent degradation. MK-0752 reduced A¦Â40 in a dose-dependent manner. Dose-dependent reductions in plasma, brain and CSF A¦Â40 were observed in guinea-pigs following single oral doses of 10¨C30 mg/kg (brain IC50 = 0.44 ¦ÌM). Concentration required for 50 percent reduction of brain A¦Â40 was 318 nM and 0.15 ¦ÌM in APP-YAC and Tg2576 mice, respectively.

prudect name : MK-0752 is a potent gamma secretase (¦Ã-secretase) inhibitor in clinical development with an IC50 of 5 nM for A¦Â40 in human SH-SY5Y cells.Defining the metabolic fate of…

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HEK293 cells stably expressing the human CGRP receptor are preincubated with various concentrations of MK 3207 in the presence or absence of 50% human serum for 30 minutes at 37 °C. Isobutyl-methylxanthine (300 ¦ÌM) is added to the cells, and then they are incubated for 30 minutes at 37 °C followed by stimulation with 0.3 nM ¦Á-CGRP for 5 minutes at 37 °C. After agonist stimulation cells are washed with PBS and the intracellular cAMP concentration is measured using the cAMP SPA Biotrak direct screening assay. Dose-response curve is plotted, and IC50 value is determined.

prudect name : HEK293 cells stably expressing the human CGRP receptor are preincubated with various concentrations of MK 3207 in the presence or absence of 50% human serum for 30…

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Description: IC50 Value: 0.34uM(for K562 cell)[1] M344 is a potent HDAC inhibitor, which can also induced expression of the pro-apoptotic genes, Puma and Bax, together with the morphological features of apoptosis, in MCF-7 cells. in vitro: In contrast to the significant induction of p21(waf1/cip1) mRNA expression following treatment with M344 (10¦ÌM) for 1 or 3 days, there was a significant decrease in p53 mRNA expression, although p53 protein levels were unchanged. Similar treatment with M344 also induced expression of the pro-apoptotic genes, Puma and Bax, together with the morphological features of apoptosis, in MCF-7 cells [2]. With the addition of M344, the platinum-sensitive breast and ovarian cancer cell lines that displayed relatively high BRCA1 protein levels demonstrated significant potentiation of cisplatin cytotoxicity in association with a reduction of BRCA1 protein[3]. M344 up-regulates SMN2 protein expression in fibroblast cells derived from SMA patients up to 7-fold after 64 h of treatment [5]. in vivo: M344 was a highly effective inhibitors of histone deacetylases as potential therapeutic tools for high-risk embryonal tumors of the nervous system of childhood[4].

prudect name : Description: IC50 Value: 0.34uM(for K562 cell)[1] M344 is a potent HDAC inhibitor, which can also induced expression of the pro-apoptotic genes, Puma and Bax, together with the…

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Matrine can reduce aminotransferase, liver disease to reduce symptoms and prevent cell replication system of hepatitis B virus.

prudect name : Matrine can reduce aminotransferase, liver disease to reduce symptoms and prevent cell replication system of hepatitis B virus.Matrine Synonyms: SophocarpidineCAS NO: 519-02-8Molecular Formula: C15H24N2OMolecular Weight: 248.37Purity: ≥98%Solubility:…

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Micafungin is a semisynthetic lipopeptide substances by fungi Coleophomaempetri derived fermentation product development. Micafungin can specifically inhibit fungal cell wall component ¦Â (1,3)-D-glucan synthesis, destruction of fungal cell structure, to dissolve.

prudect name : Micafungin is a semisynthetic lipopeptide substances by fungi Coleophomaempetri derived fermentation product development. Micafungin can specifically inhibit fungal cell wall component ¦Â (1,3)-D-glucan synthesis, destruction of fungal…

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