tc-c 14g

CB1 receptor inverse agonist

Compound 1059182-21-6 features a cyclic structure characterized by a nitrogen atom occupying an apex (corner) within the heterocycle. Its molecular scaffold integrates aromatic properties due to the presence of a conjugated system, while the inclusion of hydroxyl (-OH) groups confers reactive potential for subsequent modification. Additionally, a halogenated component, specifically a bromine atom, is attached to the aromatic ring, enhancing its propensity for undergoing further synthetic transformations.

14-Hydroxy sprengerinin C is a natural product from Ophiopogon japonicus.

α2D-adrenoceptor agonist

adenosine A2A receptors antagonist

c-Fms-IN-14 (Example 76) is a potent inhibitor of the c-Fms kinase with an IC50 of 4 nM, utilized in cancer and autoimmune disease research [1].

TC-SP 14, also known as compound 14, is a highly active and potent S1P1 agonist with oral bioavailability. It exhibits an EC50 value of 0.042 μM, indicating its strong binding affinity to the S1P1 receptor. Notably, its interaction with the S1P3 receptor is minimal, as evidenced by an EC50 value of 3.47 μM. TC-SP 14 demonstrates significant pharmacological effects, including a marked reduction in blood lymphocyte counts and the attenuation of delayed type hypersensitivity response to antigen challenge [1].

Compound 40, NH2-c[X-R-L-S-X]-K-G-P-(D-2Nal), a macrocyclic analogue of Ape13, acts as a potent APJ agonist with a Ki of 5.7 nM. It demonstrates favorable Gα12-biased signaling and possesses an enhanced in vivo half-life [1].

TC-G 1005 is a potent and selective GPBA agonist (EC50 :0.72 nM; hTGR5). Selective for TGR5 over FXR (farnesoid X receptor). Increases plasma GLP-1 levels and reduces blood glucose in mice. Orally available.

c-Met-IN-14, a N-sulfonylamidine-based derivative, is a selective c-Met kinase inhibitor with an IC50 value of 2.89 nM. It exhibits anticancer properties by inhibiting c-Met phosphorylation and arresting the cell cycle at the G2/M phase. Additionally, c-Met-IN-14 promotes dose-dependent apoptosis in A549 cells.

GSK-3β inhibitor

Compound 39 (NH2-c[X-R-L-S-X]-K-G-P-(D-1Nal)) is a potent agonist of the APJ receptor, possessing a K i value of 0.6 nM. It is capable of activating Gαi1, with an EC 50 of 0.8 nM, and of recruiting β-arrestin2, with an EC 50 of 31 nM. Furthermore, this compound demonstrates extended effects on cardiac function [1].

TC-G-1008 (GPR39-C3) is a GPR39 (zinc receptor) agonist (EC50 values are 0.4 and 0.8 nM for rat and human receptors respectively).