UT-B-IN-1
Names
[ CAS No. ]:
892742-76-6
[ Name ]:
UT-B-IN-1
Biological Activity
[Description]:
UT-B-IN-1 (UTBINH-14) is a reversible, competitive and selective urea transporter-B (UT-B) inhibitor with IC50 values of 10 and 25 nM for human and mouse UT-B, respectively. UT-B-IN-1 shows low toxicity and high selectivity for UT-B over UT-A isoforms. UT-B-IN-1 increases urine output and reduces urine osmolality of mice. UT-B-IN-1 can be used for diuretic mechanism research[1].
[Related Catalog]:
[Target]
IC50: 10 nM (human UT-B); 25 nM (mouse UT-B)[1]
[In Vitro]
UT-B-IN-1 (1-1000 nM) 抑制尿素预载红细胞的尿素外排，IC50 值为 26.7 nM[1]。 UT-B-IN-1 抑制 AQP1-null 红细胞的水运输[1]。 UT-B-IN-1 (0-10 μM；24 h) 对 MDCK 细胞无细胞毒性[1]。 Cell Cytotoxicity Assay[1] Cell Line: Madin-Darby canine kidney (MDCK) cell line Concentration: 0-10 μM Incubation Time: 24 hours Result: Exhibited no cytotoxic effect to MDCK cells.
[In Vivo]
UT-B-IN-1 (300 μg；腹腔注射，1 次) 在自由取水和进食的小鼠中，增加排尿量并降低尿液渗透性[1]。 Animal Model: Male mice (wild-type or UT-B knockout)[1] Dosage: 300 μg Administration: Intraperitoneal injection, 300 μg, once Result: Reduced urine osmolality and urea concentration in wild-type mice with V2-receptor agonist dDAVP injection. Increased urine volume and reduced urine osmolality and urea concentration in mice with free access to food and water but without dDAVP.
[References]
Chemical & Physical Properties
[ Molecular Formula ]:
C20H17N5O2S3
[ Molecular Weight ]:
455.58