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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 Thalidomide was introduced as a sedative drug,immunomodulatory agent and also is investigated for treating symptoms of many cancers.Thalidomide inhibits an E3 ubiquitin ligase， which is a CRBN-DDB1-Cul4A complex. Description Thalidomide is initially promoted as a sedative, inhibits cereblon (CRBN), a part of the cullin-4 E3 ubiquitin ligase complex CUL4-RBX1-DDB1, with a Kd of ∼250 nM, and has immunomodulatory, anti-inflammatory and anti-angiogenic cancer properties. In Vitro Tha... -
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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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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... -
factory Outlets for Doxycycline Hyclate 50 Mg Acne - Ticagrelor – CPF
Background Ticagrelor is a novel antagonist of the P2Y12 receptor [1]. Ticagrelor has been reported to inhibit the prothrombotic effects of ADP on the platelet by against the P2Y12 receptor. Ticagrelor has shown the complete inhibition of platelet aggregation ex vivo. In addition Ticagrelor has suggested a dose-dependent inhibition of platelet aggregation in human being. Apart from these, Ticagrelor has also demonstrated an orally, actively, reversibly binding antagonist. Unlike other inhibit... -
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Description Bictegravir is a novel, potent inhibitor of HIV-1 integrase with an IC50 of 7.5 nM. In Vitro Bictegravir (BIC) inhibits the strand transfer activity with an IC50 of 7.5± 0.3 nM. Relative to its inhibition of strand transfer activity, Bictegravir is a much weaker inhibitor of 3′-processing activity of HIV-1 IN, with an IC50 of 241±51 nM. Bictegravir enhances the accumulation of 2-LTR circles ~5-fold relative to the mock-treated control and reduces the amount of authentic integrati... -
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Background Ticagrelor is a novel antagonist of the P2Y12 receptor [1]. Ticagrelor has been reported to inhibit the prothrombotic effects of ADP on the platelet by against the P2Y12 receptor. Ticagrelor has shown the complete inhibition of platelet aggregation ex vivo. In addition Ticagrelor has suggested a dose-dependent inhibition of platelet aggregation in human being. Apart from these, Ticagrelor has also demonstrated an orally, actively, reversibly binding antagonist. Unlike other inhibit... -
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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...
