Activators & Inhibitors

CB1R Allosteric modulator 1 (compound 11) is a potent allosteric modulator of CB1R. CB1R Allosteric modulator 1 negatively affects the functional activity of orthosteric ligands (NAM) at CB1Rs.

Adenosine receptor inhibitor 2 (compound 14b) is a potent inhibitor of AR (adenosine receptor). Adenosine receptor inhibitor 2 exhibits dual affinity toward A 1 /A 2A ARs with higher affinity for the A 1 - than the A 2A AR. Adenosine receptor inhibitor 2 exhibits Ki values of 52.2 nM for the A 1 AR and 167 nM for the A 2A AR.

Sheng Gelieting (CGT-8012) is a inhibitor of dipeptidy peptidase-IV enzyme (DP-IV) with an IC 50 value of 87 nM. Sheng Gelieting can be used for researching to the dipeptidy peptidase-IV enzyme, such as the diabetes, particularly the II-type diabete.

Pelecopan (BCX9930) is a potent, selective, orally active inhibitor of complement factor D (IC50= 14.3 nM). Pelecopan can prevent both intravascular and extravascular hemolysis in PNH.

TrxR-IN-2 is a potential thioredoxin reductase (TrxR) inhibitor. TrxR-IN-2 has research value in the chemotherapy of drug-resistant hepatocellular carcinoma.

SKI-I is a potent and selective inhibitor of human sphingosine kinase (SK). SKI-I shows an IC 50 of 1.2 μM for ST-hSK. SKI-I is also a hERK2 inhibitor( IC 50 =11 μM). SKI-I induces apoptosis in tumor cell lines.

Penamecillin (Wy 20788) is an orally active antibacterial agent.

GSK852 is a potent, second bromodomain (BD2)-selective, bromo and extra-terminal domain (BET) inhibitor with pIC50 of 7.9.

μ opioid receptor agonist 2 （Compound H-3）is a MOR receptor agonist. μ opioid receptor agonist 2 can be used for the research of pain and pain related diseases.