Chemicals & Small Molecules

[Leu31,Pro34]-Neuropeptide Y(human,rat) (Legacy Tebubio ref. 282TP1985). High affinity neuropeptide Y Y1 receptor agonist (Ki = 0.39 nM). Also shows affinity for Y4 and Y5 receptors.

[Arg14,Lys15]Nociceptin (Legacy Tebubio ref. 282TP1986). Highly potent and selective NOP receptor agonist (EC50 = 1 nM). Displays > 875-fold selectivity over opioid receptors (IC50 values are 0.32, 280, > 10000 and 1500 for NOP, μ, δ and κ receptors respectively). Longer lasting and 30-fold more potent than nociceptin in vivo; pronociceptive and inhibits locomotor activity.

[Nphe1]Nociceptin(1-13)NH2 (Legacy Tebubio ref. 282TP1987). 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.

[Phe1Ψ(CH2-NH)Gly2]Nociceptin(1-13)NH2 (Legacy Tebubio ref. 282TP1988). 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).

NEP(1-40) (Legacy Tebubio ref. 282TP1989). Peptide fragment corresponding to residues 1 - 40 of Nogo-66, the domain of the myelin protein Nogo that inhibits axonal outgrowth. Acts as a competitive antagonist at the Nogo-66 receptor (NgR); blocks Nogo-66- and CNS myelin-induced inhibition of axonal growth, but does not reduce myelin-associated glycoprotein (MAG) inhibition of neurite outgrowth in vitro. Promotes regeneration of hemisected spinal axons and locomotor recovery following spinal injury in vivo.

Norleual (Legacy Tebubio ref. 282TP1990). Angiotensin IV analog. Highly potent HGF/c-MET inhibitor (IC50 = 3 pM). Inhibits HGF-induced MDCK cell proliferation and invasion in vitro. Also AT4 receptor antagonist; disrupts LTP stabilization. Antiangiogenic.

M 1145 acetate (Legacy Tebubio ref. 282TP1991L). M1145 acetate, a chimeric peptide, is a selective galanin receptor type 2 (GAL2) agonist, with a Ki of 6.55 nM. M1145 acetate shows more than 90-fold higher affinity for GAL2 over GAL1 (Ki=587 nM) and a 76-fold higher affinity over GalR3 (Ki=497 nM). M1145 acetate has an additive effect on the signal transduction of galanin[1].

M40 (Legacy Tebubio ref. 282TP1992). Potent, non-selective galanin receptor antagonist (Ki values are 1.82 and 5.1 nM at GAL1 and GAL2 respectively) that inhibits galanin (1-29) binding in rat brain in vitro (IC50 = 3 - 15 nM). Attenuates the antidepressant effects of fluoxetine and blocks galanin-induced food intake in vivo. Also exhibits weak partial agonist activity at peripheral GAL2 receptors at doses > 100 nM.

M40 acetate(143896-17-7 free base) (Legacy Tebubio ref. 282TP1992L). M40 acetate is a potent, non-selective galanin receptor antagonist (Ki values are 1.82 and 5.1 nM at GAL1 and GAL2 respectively) that inhibits galanin (1-29) binding in rat brain in vitro (IC50 = 3 - 15 nM). Attenuates the antidepressant effects of fluoxetine and blocks galanin-induced food intake in vivo. Also exhibits weak partial agonist activity at peripheral GAL2 receptors at doses > 100 nM.