AT1

Eprosartan Mesylate (SKF-108566J) is a competitive and reversible Angiotensin II Receptor Blocker.

TD-0212 is an orally active dual pharmacology antagonist of angiotensin II type 1 receptor (AT1) and inhibitor of neprilysin (NEP)(pKi of 8.9 for AT1 and a pIC50 of 9.2 for NEP).

TD-0212 TFA is an orally active dual pharmacology compound, functioning as an antagonist of the angiotensin II type 1 receptor (AT1) with a pKi of 8.9, and as an inhibitor of neprilysin (NEP) with a pIC50 of 9.2.

Buloxibutid (AT2 receptor agonist C21) is a novel and selective small molecule angiotensin II AT2 receptor agonist, exhibiting Ki values of 0.4 nM and 10 μM for AT2 and AT1 receptors, respectively.

BRD4 degrader AT1 is a highly selective Brd4 degrader based on PROTAC technology, with a Kd of 44 nM for Brd4BD2 in cells.

GAT107 is a novel and potent α7 nicotinic cholinergic receptor modifier agonist and modulator with anti-inflammatory activity that reverses injury perception in a mouse model of neuropathic pain.

LAT1-IN-1 (BCH) is a selective and competitive inhibitor of L-type amino acid transporter protein 1 (LAT1). LAT1-IN-1 has antitumor activity, inducing apoptosis in tumor cells and inhibiting cell proliferation.

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.

DGAT1-IN-1 is a potent inhibitor of diacylglycerol O-acyltransferase type 1 (DGAT1) with an IC50 of less than 10 nM.

MALAT1-IN-1 modulated Malat1 downstream genes in a dose-dependent manner without affecting the expression of nuclear enriched abundant transcript 1 (Neat1). MALAT1-IN-1 is an effective and specific Malat1 inhibitor.

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.

STAT1 3-IN-1 (Compound 6k) is an inhibitor of STAT1 3 phosphorylation. It prevents the phosphorylation and nuclear translocation of STAT1 3. Additionally, STAT1 3-IN-1 inhibits the inflammatory enzymes iNOS and COX-2. This compound exhibits anti-inflammatory properties by reducing pro-inflammatory cytokines, such as IL-1β, IL-6, and TNF-α, without significant cytotoxicity.

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.

AT1R antagonist 3 (Compound 1) is an antagonist of the angiotensin II type 1 receptor (AT1R) and an inhibitor of the L-type calcium channel CaV1.2 (IC50=0.57 μM). It exhibits vasodilatory effects in isolated rat aorta (10 μM, 88.7%) and shows antihypertensive activity in rat models.

AT13148 is an oral-active and ATP-competitive, multi-AGC kinase inhibitor for Akt1/2/3, p70S6K, PKA, and ROCKI/II.

DAT1 is an antimitotic and antiangiogenic that acts by binding to the colchicine binding site of tubulin.

JNJ-DGAT1-A is a DGAT1-selective inhibitor.

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].

DGAT1-IN-3 is a selective, potent, orally active DGAT-1 inhibitor that inhibits human DGAT-1 (IC50: 38 nM) and rat DGAT-1 (IC50: 120 nM).DGAT1-IN-3 can be used in studies of obesity, dyslipidemia and metabolic syndrome.

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].