MIP-1095 I-123, as a radiotracer, is under investigation in clinical trial NCT00712829 (Evaluating the Safety, Pharmacokinetics, Tissue Distribution, Metabolism and Dosimetry of Two Prostate Cancer Imaging Agents).
STING agonist 12b is an agonist of stimulator of interferon genes (STING).1It binds to STING (Kd= 26.4 μM) and induces interferon reporter gene expression in cells expressing human or mouse STING (EC50s = 7.45 and 10.23 μM, respectively). STING agonist 12b (40 μM) induces expression of TNF-a, IL-6, IP-10, and IL-1b in THP-1 cells. 1.Hou, S., Lan, X.-j., Li, W., et al.Design, synthesis and biological evaluation of acridone analogues as novel STING receptor agonistsBioorg. Chem.95103556(2020)
AMG 487 is an effective and selective antagonist of chemokine receptor 3. AMG 487 inhibited CXCR3-mediated cell migration induced by three CXCR3 chemokines, IP-10, ITAC and MIG (IC50: 8, 15 and 36 nM, respectively).
Hydrochloride salt of dTAGV-1. Suitable for use in vivo. Following ip administration of 10 mg kg in mice: T = 4.43 h; Cmax = 2123 ng mL-1; AUCinf = 18517 hr*ng mL-1 and CL = 9.05 mL min-1 kg-1 Negative control dTAGV-1-NEG also available. Important: It is recommended that DMSO stock solutions of this compound are made and used on the same day and are not subjected to freeze thaw.
YM 298198 Hydrochloride is a non-competitive antagonist with high affinity and selectivity for mGlu1 receptors (Ki = 19 nM). YM 298198 Hydrochloride is inactive at other mGlu receptor subtypes (mGlu2-7), ionotropic receptors and glutamate transporters (IC50 > 10 μM). It inhibits glutamate-induced IP production more potently than CPCCOEt (IC50 values are 16 nM and 6.3 μM respectively).