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Oxidized ATP (oATP) trisodium salt is a broad-spectrum P2 receptor inhibitor. Oxidized ATP trisodium salt irreversibly antagonizes P2X7R activation. Oxidized ATP trisodium salt inhibits c-reactive protein (CRP)-induced NLRP3 inflammasome activation. Oxidized ATP trisodium salt can be used for research of atherosclerosis .
Mulberrin is a strong inhibitor of organic anion-transporting polypeptide 2B1 (OATP2B1)-mediated estrone-3-sulfate (E3S) uptake with an IC50 value being 1.8 ±1.5 μM.
TME-HYM (PH Probe) is a novel fluorescent probe based on acidic tumor microenvironment (TME) activation and organic anion transporting polypeptide (OATPs, overexpressed on cancer cells), and can be selective uptaken. TME-HYM (PH Probe) can selectively lit up cancer cells and tumor tissues, offering dual tumor selectivity for precise visualization of tumor mass .
IR-251 is a mitochondrion-targeting NIR fluorescent probe. IR-251 targets mitochondria via OATPs and causes mitochondrial damage in tumor cells. IR-251 IR-251 induced ROS overproduction by inhibiting PPARγ, and then inhibiting the β-catenin signaling pathway and downstream protein molecules related to the cell cycle and metastasis. IR-251 inhibits tumor proliferation and metastasis .
Euphol acetate is a triterpene that can be isolated from Euphorbia broteri. Euphol acetate is an inhibitor of hepatic transport proteins organic anion-transporting polypeptide 1/3 (OATP1B1/3) .
Simvastatin acid (Tenivastatin) ammonium is a potent HMG-CoA reductase (HMGCR) inhibitor. Simvastatin acid ammonium reduces Indoxyl sulfate-mediated reactive oxygen species (ROS) production in human cardiomyocytes. Simvastatin acid ammonium can also modulates OATP3A1 expression in cardiomyocytes and HEK293 cells transfected with the OATP3A1 gene .
Simvastatin hydroxy acid (Tenivastatin) sodium is a potent HMG-CoA reductase (HMGCR) inhibitor. Simvastatin hydroxy acid sodium reduces Indoxyl sulfate-mediated reactive oxygen species (ROS) production in human cardiomyocytes. Simvastatin hydroxy acid sodium can also modulates OATP3A1 expression in cardiomyocytes and HEK293 cells transfected with the OATP3A1 gene .
Simvastatin acid (Tenivastatin) calcium hydrate is a potent HMG-CoA reductase (HMGCR) inhibitor. Simvastatin acid calcium hydrate reduces Indoxyl sulfate-mediated reactive oxygen species (ROS) production in human cardiomyocytes. Simvastatin acid calcium hydrate can also modulates OATP3A1 expression in cardiomyocytes and HEK293 cells transfected with the OATP3A1 gene .
Simvastatin acid (Tenivastatin), a hydrolysate of Simvastatin (HY-17502), is a HMG-CoA reductase (HMGCR) inhibitor. Simvastatin acid reduces Indoxyl sulfate-mediated reactive oxygen species (ROS) production in human cardiomyocytes. Simvastatin acid can also modulates OATP3A1 expression in cardiomyocytes and HEK293 cells transfected with the OATP3A1 gene .
Daclatasvir dihydrochloride (BMS-790052 dihydrochloride) is a potent and orally active HCV NS5A protein inhibitor with EC50s range of 9-146 pM for multiple HCV replicon genotypes. Daclatasvir dihydrochloride is also an organic anion transporting polypeptide 1B (OATP1B) and OATP1B3 inhibitor with IC50s of 1.5 µM and 3.27 µM, respectively .
Daclatasvir (BMS-790052) is a potent and orally active HCV NS5A protein inhibitor with EC50s range of 9-146 pM for multiple HCV replicon genotypes. Daclatasvir is also a organic anion transporting polypeptide 1B (OATP1B) and OATP1B3 inhibitor with IC50s of 1.5 µM and 3.27 µM, respectively .
Simvastatin acid-d6 (ammonium)mis the deuterium labeled Simvastatin acid ammonium. Simvastatin ammonium is an active metabolite of simvastatin lactone mediated by CYP3A4/5 in the intestinal wall and liver (pKa=5.5). Simvastatin ammonium reduces indoxyl sulfate-mediated reactive oxygen species and modulates OATP3A1 expression in cardiomyocytes and HEK293 cells transfected with the OATP3A1 gene[1].
6-Hydroxyindole is a biochemical reagent. 6-hydroxyindole is an endogenous long-lasting OATP1B1 inhibitor, and is elevated plasma of the renal failure patients .
6α-Hydroxy paclitaxel is a primary metabolite of Paclitaxel. 6α-Hydroxy paclitaxel retains a time-dependent effect on organic anion–transporting polypeptides 1B1/SLCO1B1(OATP1B1) with similar inhibition potency to Paclitaxel, whereas it no longer showed time-dependent inhibition of OATP1B3. 6α-Hydroxy paclitaxel can be used for the research of cancer .
Daclatasvir-d6 is deuterium labeled Daclatasvir. Daclatasvir (BMS-790052) is a potent and orally active HCV NS5A protein inhibitor with EC50s range of 9-146 pM for multiple HCV replicon genotypes. Daclatasvir is also a organic anion transporting polypeptide 1B (OATP1B) and OATP1B3 inhibitor with IC50s of 1.5 µM and 3.27 µM, respectively[1][2][3].
Daclatasvir-d16 is deuterium labeled Daclatasvir. Daclatasvir (BMS-790052) is a potent and orally active HCV NS5A protein inhibitor with EC50s range of 9-146 pM for multiple HCV replicon genotypes. Daclatasvir is also a organic anion transporting polypeptide 1B (OATP1B) and OATP1B3 inhibitor with IC50s of 1.5 µM and 3.27 µM, respectively[1][2][3].
Estradiol 17-(β-D-Glucuronide), a metabolite of estrogen, is well known to cause intrahepatic cholestasis in humans. Estradiol 17-(β-D-Glucuronide) is a high-affinity substrate for oatp organic anion transporter .
Abi-DZ-1 is a potential multifunctional theranostic agent via the HIF1α/OATPs Pathway. Abi-DZ-1 can be used in the research of tumor-targeted imaging and precision therapy .
6α-Hydroxy Paclitaxel-d5 is the deuterium labeled 6α-Hydroxy paclitaxel. 6α-Hydroxy paclitaxel is a primary metabolite of Paclitaxel. 6α-Hydroxy paclitaxel retains a time-dependent effect on organic anion–transporting polypeptides 1B1/SLCO1B1 (OATP1B1) with similar inhibition potency to Paclitaxel, whereas it no longer showed time-dependent inhibition of OATP1B3. 6α-Hydroxy paclitaxel can be used for the research of cancer[1].
Nadolol (SQ-11725) is a non-selective and orally active β-adrenergic receptors blocker and is a substrate of organic anion transporting polypeptide 1A2 (OATP1A2). Nadolol has the the potential for high blood pressure, angina pectoris and vascular headaches research .
HMG-CoA Reductase-IN-1 is a HMG-CoA reductase inhibitor. HMG-CoA Reductase-IN-1has high HMGR inhibitory activity and OATP1B1 affinity with pIC50 and pKm values of 8.54 and 1.98, respectively. HMG-CoA Reductase-IN-1 can be used for the research of hypercholesterolemia .
Pradigastat (LCQ-908) is a potent, selective and orally active diacylglycerol acyltransferase 1 (DGAT1) inhibitor. Pradigastat has anti-obesity and anti-diabetic effects .
CP-100356 hydrochloride is an orally active dual MDR1 (P-gp)/BCRP inhibitor, with an IC50s of 0.5 and 1.5 µM for inhibiting MDR1-mediated Calcein-AM transport and BCRP-mediated Prazosin transport, respectively. CP-100356 hydrochloride is also a weak inhibitor of OATP1B1 (IC50=∼66 µM). CP-100356 hydrochloride is devoid of inhibition against MRP2 and major human P450 enzymes (IC50>15 µM) .
6-Hydroxyindole is a biochemical reagent. 6-hydroxyindole is an endogenous long-lasting OATP1B1 inhibitor, and is elevated plasma of the renal failure patients .
Mulberrin is a strong inhibitor of organic anion-transporting polypeptide 2B1 (OATP2B1)-mediated estrone-3-sulfate (E3S) uptake with an IC50 value being 1.8 ±1.5 μM.
Simvastatin acid (Tenivastatin) ammonium is a potent HMG-CoA reductase (HMGCR) inhibitor. Simvastatin acid ammonium reduces Indoxyl sulfate-mediated reactive oxygen species (ROS) production in human cardiomyocytes. Simvastatin acid ammonium can also modulates OATP3A1 expression in cardiomyocytes and HEK293 cells transfected with the OATP3A1 gene .
6-Hydroxyindole is a biochemical reagent. 6-hydroxyindole is an endogenous long-lasting OATP1B1 inhibitor, and is elevated plasma of the renal failure patients .
Euphol acetate is a triterpene that can be isolated from Euphorbia broteri. Euphol acetate is an inhibitor of hepatic transport proteins organic anion-transporting polypeptide 1/3 (OATP1B1/3) .
Estradiol 17-(β-D-Glucuronide), a metabolite of estrogen, is well known to cause intrahepatic cholestasis in humans. Estradiol 17-(β-D-Glucuronide) is a high-affinity substrate for oatp organic anion transporter .
SLC21A3 is a Na(+)-independent transporter that greatly facilitates cellular uptake of a variety of organic anions, including bile salts necessary for intestinal absorption. SLC21A3 is responsible for transporting substances such as DHEAS, estrone 3-sulfate, and atROL in human retinal pigment epithelial cells to maintain the integrity of the visual cycle. SLC21A3 Protein, Human (Sf9, His, MBP, FLAG) is the recombinant human-derived SLC21A3 protein, expressed by Sf9 insect cells , with N-MBP, C-Flag, N-8*His labeled tag. The total length of SLC21A3 Protein, Human (Sf9, His, MBP, FLAG) is 669 a.a., .
6α-Hydroxy Paclitaxel-d5 is the deuterium labeled 6α-Hydroxy paclitaxel. 6α-Hydroxy paclitaxel is a primary metabolite of Paclitaxel. 6α-Hydroxy paclitaxel retains a time-dependent effect on organic anion–transporting polypeptides 1B1/SLCO1B1 (OATP1B1) with similar inhibition potency to Paclitaxel, whereas it no longer showed time-dependent inhibition of OATP1B3. 6α-Hydroxy paclitaxel can be used for the research of cancer[1].
Simvastatin acid-d6 (ammonium)mis the deuterium labeled Simvastatin acid ammonium. Simvastatin ammonium is an active metabolite of simvastatin lactone mediated by CYP3A4/5 in the intestinal wall and liver (pKa=5.5). Simvastatin ammonium reduces indoxyl sulfate-mediated reactive oxygen species and modulates OATP3A1 expression in cardiomyocytes and HEK293 cells transfected with the OATP3A1 gene[1].
Daclatasvir-d6 is deuterium labeled Daclatasvir. Daclatasvir (BMS-790052) is a potent and orally active HCV NS5A protein inhibitor with EC50s range of 9-146 pM for multiple HCV replicon genotypes. Daclatasvir is also a organic anion transporting polypeptide 1B (OATP1B) and OATP1B3 inhibitor with IC50s of 1.5 µM and 3.27 µM, respectively[1][2][3].
Daclatasvir-d16 is deuterium labeled Daclatasvir. Daclatasvir (BMS-790052) is a potent and orally active HCV NS5A protein inhibitor with EC50s range of 9-146 pM for multiple HCV replicon genotypes. Daclatasvir is also a organic anion transporting polypeptide 1B (OATP1B) and OATP1B3 inhibitor with IC50s of 1.5 µM and 3.27 µM, respectively[1][2][3].
