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BMS-248360 is a potent, orally active dual antagonist of both angiotensin II receptor (AT1) and endothelin A (ETA) receptor, with Kis of 10 nM and 1.9 nM for hAT1 and hETA receptors, respectively. BMS-248360 demonstrates hypertensive effects[1].

URAT1 inhibitor 1 (1g) is a potent inhibitor of uric acid transporter 1 (URAT1) with an IC50 of 32 nM, and has potential therapeutic applications for treating hyperuricemia associated with gout.

Compound 27b, also known as hURAT1 inhibitor 1, is an isomarine-derived, orally active inhibitor that targets both hURAT1 and GLUT9 with IC50 values of 0.16 μM and 4.47 μM, respectively. This compound exhibits significant anti-hyperuricemia effects and has demonstrated potent uric acid-lowering activity in a hyperuricemia mouse model at a dose of 10 mg/kg. Importantly, Compound 27b displays no notable in vitro cytotoxicity or in vivo hepatotoxicity, and possesses favorable pharmacokinetic (PK) characteristics.

URAT1 inhibitor11 (Compound 7) is a potent URAT1 inhibitor, exhibiting an IC50 of 0.18 μM. It effectively reduces uric acid levels in zebrafish with hyperuricemia induced by Potassium oxonate and Xanthinesodium salt.

hURAT1 inhibitor 2 (Compound 5) is an inhibitor of hURAT1 (uric acid transporter 1, SLC22A12) with an IC50 of 18 nM. It also exhibits some inhibitory activity against OATP1B1, with an IC50 of 0.73 μM. hURAT1 inhibitor 2 can be used in research related to hyperuricemia, gout, and other diseases associated with abnormal uric acid metabolism.

URAT1 inhibitor13 (compound 22k) is a potent inhibitor of URAT1, useful for research related to gout.

URAT1 inhibitor10 (Compound 23a) is a URAT1 inhibitor with an IC50 of 0.052 μM. It exhibits oral efficacy and low cytotoxicity. The compound demonstrates high selectivity for OAT1, with an IC50 of 9.17 μM.

URAT1/GLUT9-IN-1 (compound 29) effectively inhibits urate transporter 1 (URAT1) with an IC50 value of 2.01 μM and glucose transporter 9 (GLUT9) with an IC50 of 18.21 μM. This compound exhibits favorable pharmacokinetic properties and oral bioavailability, making it useful for research in gout and hyperuricemia.

URAT1 inhibitor 3 is a potent, orally active, selective inhibitor of URAT1 (IC50 = 0.8 nM) demonstrating urate-lowering efficacy, suitable for research in gout and hyperuricemia [1].

URAT1 inhibitor 2 is an orally active inhibitor of URAT1 and CYP isozyme with IC50 values of 1.36 μM, 16.97 μM, and 5.22 μM for URAT1-mediated 14C-UA uptake, CYP1A2, and CYP2C9, respectively [URAT1 inhibitor 2 is a promising drug candidate for the study of hyperuricemia and gout].

URAT1 Inhibitor 4, derived from Lesinurad, is a potent, orally active inhibitor of URAT1 with an IC50 value of 7.56 μM, demonstrating greater in vivo urate-lowering efficacy than Lesinurad [1].

URAT1 inhibitor 7 is a novel and potent inhibitor of the human uric acid transporter protein URAT1 (IC50:12 nM).URAT1 inhibitor 7 inhibits CYP2C9 with an IC50 of 4.2 μM.URAT1 inhibitor 7 can be used to study hyperuricemia and gout.

URAT1 Inhibitor 8 (example 247) serves as a highly potent inhibitor of URAT1, demonstrating an IC50 value of 0.001 μM. It is applicable in the study of gout [1].

URAT1 inhibitor 6 (Compound 1h), with an IC50 of 35 nM for hURAT1, demonstrates 200-fold and 8-fold greater potency compared to Lesinurad and Benzbromarone, respectively. This compound is utilized in the study of inflammation [1].

Compound BDEO (URAT1&XO inhibitor 2) serves as a dual-action inhibitor targeting both xanthine oxidase (XO) and URAT1, demonstrating an IC50 value of 3.3 μM for XO inhibition. It effectively impedes uric acid uptake in HEK293 cells with URAT1 expression, evidenced by a Ki of 0.145 μM. In hyperuricemic mice models, the compound has been shown to reduce serum urate levels and uric acid excretion, indicating potential utility for hyperuricemia research [1].

Compound II15, known as XOR/URAT1-IN-1, serves as a dual inhibitor targeting xanthine oxidoreductase (XOR) and uric acid transporter 1 (URAT1), exhibiting IC50 values of 6 nM and 12.9 μM, respectively. This compound effectively reduces uric acid levels in a mouse model of acute hyperuricemia induced by potassium oxonate and hypoxanthine.

XMD15-44, a RET kinase inhibitor, demonstrates potent growth-inhibitory effects on RAT1 cells transformed by RET/C634R and RET/M918T, with IC50 values of 11.5 nM and 8.3 nM, respectively. It effectively inhibits RET kinase activity and signaling in human thyroid cancer cell lines harboring oncogenic RET alleles, thereby reducing cell proliferation.

PF-06843195 is a potent and selective PI3Kα inhibitor that binds to the active site of PI3Kα and prevents it from catalyzing the conversion of PIP2 to PIP3, thereby inhibiting the activation of AKT, with anti-tumor activity in vitro and in vivo.