Zoniporide hydrochloride hydrate is a potent and selective sodium-hydrogen exchanger type 1 (NHE-1) inhibitor. Zoniporide hydrochloride hydrate inhibits human NHE-1 with IC50 of 14 nM.
Bombesin receptor antagonist that inhibits bombesin binding to rat brain with an IC50 value of 2 μM. Inhibits amylase release in vitro (IC50 = 4 μM) and attenuates bombesin-mediated suppression of food intake in vivo.
Selective and competitive nociceptin receptor antagonist, devoid of any agonist activity. Binds selectively to recombinant nociceptin receptors (pKi = 8.4), and competitively antagonizes the actions of nociceptin in vitro and in vivo.
Potent agonist of the nociceptin (ORL1) receptor, demonstrated both in vitro and in vivo. Selective, competitive antagonism at the nociceptin receptor has also been reported (pA2 = 7.02 and 6.75 in the guinea pig ileum and mouse vas deferens respectively)
D18 is an immune modulator that acts as a dual agonist for TLR7/8 (with EC50 values of 24 nM for hTLR7 and 10 nM for hTLR8, respectively). It enhances the expression of PD-L1 through epigenetic regulation, thereby increasing the sensitivity of tumors to PD-1/PD-L1 blockade. Additionally, D18 functions as a cytotoxin for ADC synthesis, specifically for the ADC HE-S2 [1].
AMD 3465 also potently inhibits the replication of X4 HIV strains (IC50: 1-10 nM). However, it has no effect on CCR5-using (R5) viruses. AMD 3465 (GENZ-644494) is a potent antagonist of CXCR4, inhibits binding of 12G5 mAb and CXCL12AF647 to CXCR4, with IC