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Acarbose is an acyl-CoA isolated from Pseudomonas species. A92. In the presence of oxidized low-density lipoprotein in macrophages J744, the synthesis of cholesterol enzymes is inhibited, with an IC50 of 45 μmol/L, and the IC50 for inhibiting ACAT in ratliver microsomes is 120 μmol/L. Inhibition of ACAT is non-competitive Sexual. Group: Pharmaceutical. CAS No. 144398-20-9. Pack Sizes: 1mg; 1g; 10g. Product ID: BBF-00539. Molecular formula: Custom synthesis is available. Send your inquiries for more information.
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Alectinib
Alectinib, marketed as Alecensa, is an oral drug that blocks the activity of anaplastic lymphoma kinase (ALK) and is used to treat non-small-cell lung cancer (NSCLC). Alectinib has a low potential for interactions. While it is metabolised by the liverenzyme CYP3A4, and blockers of this enzyme accordingly increase its concentrations in the body, they also decrease concentrations of the active metabolite M4, resulting in only a small overall effect. Conversely, CYP3A4 inducers decrease alectinib concentrations and increase M4 concentrations. Interactions via other CYP enzymes and transporter proteins cannot be excluded but are unlikely to be of clinical significance. Group: Pharmaceutical. CAS No. 1256580-46-7. Pack Sizes: 200 mg. Product ID: B0084-454466. Molecular formula: Custom synthesis is available. Send your inquiries for more information.
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Calcifediol monohydrate
Calcifediol monohydrate is a prehormone that is produced in the liver by hydroxylation of vitamin D3 (cholecalciferol) by the enzyme cholecalciferol 25-hydroxylase. It can be converted into 24-hydroxycalcidiol in the kidneys via 24-hydroxylation. Uses: Bone density conservation agents. Group: Pharmaceutical. CAS No. 63283-36-3. Pack Sizes: 100 mg. Product ID: B2694-073954. Molecular formula: Custom synthesis is available. Send your inquiries for more information.
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Estrone
Estrone is one of the three naturally occurring estrogens, the others being estradiol and estriol. Estrone is synthesized from androstenedione by the aromatase enzyme system in the ovaries and placenta, and is also synthesized from estradiol by 17-hydroxy steroid dehydrogenase in the liver. Serum concentrations of estrone in premenopausal women fluctuate according to the menstral cycle and becomes the most predominant estrogen in postmenopausal women. The binding affinities of estrone to the estrogen receptors α and β are approximately 60% and 37% relative to estradiol. Group: Pharmaceutical. CAS No. 53-16-7. Pack Sizes: 50 g. Product ID: NP6101. Molecular formula: Custom synthesis is available. Send your inquiries for more information.
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Sauchinone
Sauchinone, coming from the herbs of Saururus chinensis(Lour.) Baill, is a useful adjunctive treatment for bacterial infection. Sauchinone inhibited oxidative stress, as assessed by stainings of 4-hydroxynonenal and nitrotyrosine: these events may have a role in its inhibitory effects on HSCs activation. Sauchinone attenuated CCl4-induced liver fibrosis and TGF-β1-induced HSCs activation, which might be, at least in part, mediated by suppressing autophagy and oxidative stress in HSCs. Sauchinone protects skin keratinocytes through inhibition of extracellular signal-regulated kinase, c-Jun N-terminal kinase, and p38 MAPK signaling via upregulation of oxidative defense enzymes. Uses: Anti-inflammatory/antibacterial. Group: Pharmaceutical. CAS No. 177931-17-8. Pack Sizes: 10 mg. Product ID: B2703-464575. Molecular formula: Custom synthesis is available. Send your inquiries for more information.
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Simeprevir
Simeprevir plays an important role in HCV replication. Data from phase I and II clinical trials of TMC-435350 (TMC 435350; TMC 435; TMC-435350) to date have shown that this agent is well tolerated as a once-daily oral therapy and provides potent antiviral activity in HCV genotype 1-infected subjects, with restoration of liverenzymes and no evidence of viral breakthrough. Group: Pharmaceutical. CAS No. 923604-59-5. Pack Sizes: 100 mg. Product ID: B2693-433027. Molecular formula: Custom synthesis is available. Send your inquiries for more information.
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Telaprevir-[d4]
Labelled Telaprevir. VX-950 is a potent, selective, peptidomimetic inhibitor of the hepatitis C virus (HCV) NS3-4A serine protease, and it demonstrated excellent antiviral activity both in genotype 1b HCV replicon cells (50% inhibitory concentration [IC50] = 354 nM) and in human fetal hepatocytes infected with genotype 1a HCV-positive patient sera (IC50 = 280 nM). VX-950 forms a covalent but reversible complex with the genotype 1a HCV NS3-4A protease in a slow-on, slow-off process with a steady-state inhibition constant (K(I)*) of 7 nM. Dissociation of the covalent enzyme-inhibitor complex of VX-950 and genotype 1a HCV protease has a half-life of almost an hour. A >4-log10 reduction in the HCV RNA levels was observed after a 2-week incubation of replicon cells with VX-950, with no rebound of viral RNA observed after withdrawal of the inhibitor. In several animal species, VX-950 exhibits a favorable pharmacokinetic profile with high exposure in the liver. In a recently developed HCV protease mouse model, VX-950 showed excellent inhibition of HCV NS3-4A protease activity in the liver. Group: Pharmaceutical. Pack Sizes: 50 mg. Product ID: BLP-006018. Molecular formula: Custom synthesis is available. Send your inquiries for more information.
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Tretazicar
Tretazicar (CB1954) is a dinitrobenzamide prodrug that is converted in the presence of the enzyme NQO2 and co-substrate caricotamide (EP-0152R) (EP) into a potent cytotoxic bifunctional alkylating agent. CB1954 has been proposed for use in enzyme-prodrug gene therapy systems with the Escherichia coli enzyme nitroreductase (Ntr). Ntr converts CB1954 to 2- and 4-hydroxylamino derivatives, whereupon the non-enzymatic reaction of the 4-hydroxylamino derivative with cellular thio- esters generates a potent cytotoxic bifunctional alkylating agent capable of cross-linking DNA. Ntr delivery has been achieved in vitro using retroviral and adenoviral vectors and confirmed by immunocytochemical demonstration of Ntr expression. The Ntr-expressing cells have been shown to be sensitized to CB1954 by up to 2000-fold. The Ntr-CB1954 system shows effective bystander killing in mixed populations of Ntr-expressing and non-expressing cells treated with CB1954. The efficacy of this enzyme-prodrug approach in model systems compared with other VDEPT approaches demonstrates the feasibility and future promise of this gene therapy strategy. Uses: Antineoplastic agents. Group: Pharmaceutical. CAS No. 21919-05-1. Pack Sizes: 1 g. Product ID: B2693-366889. Molecular formula: Custom synthesis is available. Send your inquiries for more information.
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TUG-770
TUG-770 displayed excellent physicochemical and in vitro ADME properties, with good aqueous solubility, good chemical stability, low lipophilicity, and decreased plasma protein binding (PPB). TUG-770 furthermore showed excellent stability toward human liver microsomes (HLM), no inhibition of selected CYP-enzymes implicated in drug-drug interactions, no P-glycoprotein (P-gp) inhibition, and good permeability in the Caco-2 cell assay. Examination of TUG-770 in an acute intraperitoneal glucose tolerance test (IPGTT) in normal mice revealed a good dose dependent response with maximal reduction in glucose level reached at 50 mg/kg. The effect of TUG-770 was fully sustained after 29 days of daily oral treatment. Additional evaluation of TUG-770 in rats confirmed a significant glucose lowering effect for the high doses already after 10 min and for all doses after 30 min. Group: Pharmaceutical. CAS No. 1402601-82-4. Pack Sizes: 25 mg. Product ID: B0084-463218. Molecular formula: Custom synthesis is available. Send your inquiries for more information.
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