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MCOPPB trihydrochloride is a trihydrochloride form of MCOPPB that is a new nonpeptide nociceptin/orphanin FQ peptide (NOP)-receptor agonist with a pKi of 10.07 ¡À 0.01 for the human NOP receptor. MCOPPB exhibits anxiolytic effects with no effect on memory or locomotion. MCOPPB was regarded as one of the most potent, non-peptide NOP full agonists in vitro. MCOPPB has a high affinity for the human NOP receptor. MCOPPB has a high selectivity for the NOP receptor over other members of the opioid receptor family: 12-, 270- and >1000-fold more selective for the NOP receptor than for the micro-, kappa-, and delta-receptor, respectively. In an ex vivo binding study, MCOPPB (10 mg/kg, p.o.) inhibited signaling through the NOP receptor in the mouse brain, suggesting that MCOPPB penetrated into the brain after MCOPPB was orally administered. In the mouse Vogel conflict test, MCOPPB (10 mg/kg, p.o.) and diazepam (3 mg/kg, p.o.) elicited anxiolytic-like effects, although MCOPPB produced a bell-shaped response curve. MCOPPB at an oral dose of 10 mg/kg did not affect locomotor activity or memory, nor did MCOPPB contribute to ethanol-induced hypnosis.

June 21, 2017

prudect name : MCOPPB trihydrochloride is a trihydrochloride form of MCOPPB that is a new nonpeptide nociceptin/orphanin FQ peptide (NOP)-receptor agonist with a pKi of 10.07 ¡À 0.01 for the…

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Telmisartan£¨CAS NO£º144701-48-4£©intermediates

prudect name : Telmisartan£¨CAS NO£º144701-48-4£©intermediatesMethyl 4’-Bromomethylbiphenyl-2-Carboxylate Synonyms: CAS NO: 114772-38-2Molecular Formula: C15H13BrO2Molecular Weight: 305.17Purity: ≥98%Solubility: Storage: −20°C 2 years web site: www.medchemexpress.com References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/18528313

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MK-8245, a phenoxy piperidine isoxazole derivative, has been identified as a potent and liver-specific SCD inhibitor. It contains a tetrazole acetic acid moiety, which is the key molecule for OATPs recognition and liver-targeting. MK-8245 displays similar potencies against human, rat and mouse SCD1 with IC50 values of 1 nM for human SCD1 and 3 nM for both rat SCD1 and mouse SCD1. MK-8245 exhibits a significant SCD inhibition in the rat hepatocyte assay which contains functional, active OATPs with an IC50 of 68 nM, while being only weakly active in the HepG2 cell assay which is devoid of active OATPs with an IC50 of ~1 ¦ÌM. MK-8245 displays highly selective activity for the ¦¤-5 and ¦¤-6 desaturases (i.e., >100000 ¦ÌM vs rat and human ¦¤5D and ¦¤6D as assessed in the HepG assay.

prudect name : MK-8245, a phenoxy piperidine isoxazole derivative, has been identified as a potent and liver-specific SCD inhibitor. It contains a tetrazole acetic acid moiety, which is the key…

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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

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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MK-1775 is a potent and selective Wee1 kinase inhibitor with an IC50 of 5.2 nM. It abolishes cyclin-dependent kinase 1 (CDC2) activity by phosphorylation of the Tyr15 residue. It abrogates a DNA damage checkpoint (G2-phase), leading to apoptosis in combination with several DNA-damaging agents selectively in p53-deficient tumor cell lines. It is under clinical trial for advanced solid tumors.

prudect name : MK-1775 is a potent and selective Wee1 kinase inhibitor with an IC50 of 5.2 nM. It abolishes cyclin-dependent kinase 1 (CDC2) activity by phosphorylation of the Tyr15…

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MLN4924 is a potent and selective small molecule NEDD8-activating enzyme (NAE) inhibitor (IC50 = 4.7 nM).

prudect name : MLN4924 is a potent and selective small molecule NEDD8-activating enzyme (NAE) inhibitor (IC50 = 4.7 nM).MLN 4924 Synonyms: CAS NO: 905579-51-3;1160295-21-5(HCl salt)Molecular Formula: C21H25N5O4SMolecular Weight: 443.52Purity: 98%…

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Telmisartan CAS NO£º144701-48-4 intermediates

prudect name : Telmisartan CAS NO£º144701-48-4 intermediatesMethyl-4-(Butyrylamino)-3-Methyl-5-Nitrobenzoate Synonyms: CAS NO: 152628-01-8Molecular Formula: C13H16N2O5Molecular Weight: 280.28Purity: ≥98%Solubility: Storage: −20°C 2 years web site: www.medchemexpress.com References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/1852726

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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.

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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