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Background Enalapril Maleate Description Enalapril (maleate) (MK-421 (maleate)), the active metabolite of enalapril, is an angiotensin-converting enzyme (ACE) inhibitor. In Vivo Enalapril (MK-421) is a prodrug that belongs to the angiotensin-converting enzyme (ACE) inhibitor class of medications. It is rapidly metabolized in the liver to enalaprilat following oral administration. Enalapril (MK-421) is a potent, competitive inhibitor of ACE, the enzyme responsible for the conversion of angio... -
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Foreign Names Velpatasvirum (Latin) Velpatasvir (German) Velpatasvir (French) Velpatasvir (Spanish) Generic Names Velpatasvir (OS: USAN) GS-5816 (IS) UNII-KCU0C7RS7Z (IS) Multi-ingredient medications containing velpatasvir:sofosbuvir/velpatasvir systemic Brand names: Epclusa Drug class(es): antiviral combinations Sofosbuvir/velpatasvir systemic is used in the treatment of:Hepatitis C sofosbuvir/velpatasvir/voxilaprevir systemic Brand names: Vosevi Drug class(es): antiviral combinations Sofosb... -
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Background Ezetimibe is a potent and novel inhibitor of cholesterol absorption [1]. Cholesterol is a lipid molecule and is required to build and maintain membranes structural integrity and fluidity. Also, it serves as a precursor of vitamin D, bile acids and steroid hormones. In differentiated Caco-2 cells incubated with a carotenoid (1 μM), ezetimibe (10 mg/L) inhibited carotenoid transport with 50% inhibition for ɑ-carotene and β-carotene. Also, it inhibited the transport of β-cryptoxanthin... -
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Background Agomelatine is an agonist of melatonin receptors and an antagonist of the serotonin 5-HT2C receptor with Ki values of 0.062nM and 0.268nM and IC50 value of 0.27μM, respectively for MT1, MT2 and 5-HT2C [1]. Agomelatine is a unique antidepressant and is developed for treatment of major depressive disorder (MDD). Agomelatine is selective against 5-HT2C. It shows low affinities to cloned human 5-HT2A and 5-HT1A. For melatonin receptors, agomelatine shows similar affinities to cloned hu... -
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Background Ezetimibe is a potent and novel inhibitor of cholesterol absorption [1]. Cholesterol is a lipid molecule and is required to build and maintain membranes structural integrity and fluidity. Also, it serves as a precursor of vitamin D, bile acids and steroid hormones. In differentiated Caco-2 cells incubated with a carotenoid (1 μM), ezetimibe (10 mg/L) inhibited carotenoid transport with 50% inhibition for ɑ-carotene and β-carotene. Also, it inhibited the transport of β-cryptoxanthin... -
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多西环素一水物 Doxycycline Monohydrate 17086-28-1 USP/EP Generic Name: doxycycline (DOX i SYE kleen) Brand Names: Acticlate, Adoxa CK, Adoxa Pak, Adoxa TT, Alodox, Avidoxy, Doryx, Mondoxyne NL, Monodox, Morgidox, Oracea, Oraxyl, Periostat Targadox, Vibramycin calcium, Vibramycin Hyclate, Vibramycin monohydrate, Vibra-Tabs Dosage Form: capsule Doxycycline is a tetracycline antibiotic that fights bacteria in the body and an antibiotic and broad-spectrum metalloproteinase (MMP) inhibi... -
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Background Tofacitinib citrate, also known as CP-690550 citrate, is a potent inhibitor of janus kinase 3 (JAK3), a hematopoetic cell-restricted tyrosine kinase involved in signal transduction regulating lymphocyte survival, proliferation, differentiation, and apoptosis. The inhibition is JAK3 specific with a selectivity 1000-fold more than other non-JAK family kinases. Besides inhibiting JAKS (IC50 = 1 nM), tofacitinib citrate also inhibits janus kinase 2 (JAK2) and janus kinase 1 (JAK1) wit... -
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Background Ezetimibe is a potent and novel inhibitor of cholesterol absorption [1]. Cholesterol is a lipid molecule and is required to build and maintain membranes structural integrity and fluidity. Also, it serves as a precursor of vitamin D, bile acids and steroid hormones. In differentiated Caco-2 cells incubated with a carotenoid (1 μM), ezetimibe (10 mg/L) inhibited carotenoid transport with 50% inhibition for ɑ-carotene and β-carotene. Also, it inhibited the transport of β-cryptoxanthin... -
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Background IC50: low nanomolar range for inhibition of all TRK family members LOXO-101 is a tropomyosin receptor kinases (TRK) inhibitor. The TRK family of neurotrophin receptors and their neurotrophin ligands regulate neuron growth, differentiation and survival. In vitro: In previous study, LOXO-101 was evaluated for off-target kinase enzyme inhibition against a panel of non-TRK kinases at a concentration of 1,000 nM and ATP concentrations around the Km. Results showed that LOXO-101 had grea... -
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Background Tofacitinib citrate, also known as CP-690550 citrate, is a potent inhibitor of janus kinase 3 (JAK3), a hematopoetic cell-restricted tyrosine kinase involved in signal transduction regulating lymphocyte survival, proliferation, differentiation, and apoptosis. The inhibition is JAK3 specific with a selectivity 1000-fold more than other non-JAK family kinases. Besides inhibiting JAKS (IC50 = 1 nM), tofacitinib citrate also inhibits janus kinase 2 (JAK2) and janus kinase 1 (JAK1) wit... -
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Background Canagliflozin is a novel, potent, and highly selective sodium glucose co-transporter (SGLT) 2 inhibitor [1]. It has been proved that Canagliflozin can increase urine glucose excretion by reducing the renal glucose threshold and by decreasing the filtered glucose re-absorption [2]. Canagliflozin has been shown to inhibit the Na+-mediated 14C-AMG intakes in CHO-hSGLT2, CHO-rat SGLT2 and CHO-mouse SGLT2 with IC50 values of 4.4, 3.7 and 2.0 nM, respectively [1]. Canagliflozin has been ... -
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Description Dabigatran etexilate mesylate (BIBR 1048MS) is an orally active prodrug of Dabigatran. Dabigatran etexilate mesylate has anticoagulant effects and is used for the prophylaxis of venousthromboembolism and stroke due to atrial fibrillation. Background Description: IC50 Value: 4.5nM (Ki); 10nM(Thrombin-induced platelet aggregation) [1] Dabigatran is a reversible and selective, direct thrombin inhibitor (DTI) undergoing advanced clinical development as its orally active prodrug,dabiga...
