selectivity

G-418 disulfate (Geneticin sulfate) is an aminoglycoside antibiotic, an inhibitor of protein synthesis with eukaryotic selectivity. G-418 disulfate blocks peptide synthesis by inhibiting peptide chain elongation.

[Ala17]-MCH acetate is a selective ligand for MCHR1 with a Ki of 0.16 nM and Kd of 0.37 nM(Eu3+ chelate-labeled). [Ala17]-MCH acetate shows selectivity over MCHR2 with Ki of 34 nM.

MLCK inhibitor peptide 18 acetate is a selective competitive inhibitor of myosin light chain kinase (IC50 = 50 nM). Displays 4000-fold selectivity over CaM kinase II and does not inhibit PKA. Cell permeable.

UFP-101 acetate is a selective and competitive antagonist of the NOP receptor (pKi = 10.24) with >3000-fold selectivity over δ, μ, and κ opioid receptors.

[Des-Arg9]-Bradykinin is an agonist of Bradykinin (B1) receptor that displays selectivity for B1 over B2 receptors.

NoxA1ds acetate is a potent and selective NADPH oxidase 1 (NOX1) inhibitor (IC50 : 20 nM). Exhibits selectivity for NOX1 over NOX2, NOX4, NOX5 and xanthine oxidase. Inhibits NOX1-derived O2- production in HT-29 human colon cancer cells. Attenuates VEGF-induced human pulmonary artery endothelial cell migration under hypoxic conditions in vitro.

CTAP(TFA) (103429-32-9 free base) is a potent, highly selective, and brain-penetrant antagonist of the μ-opioid receptor with IC50 of 3.5 nM. It displays over 1200-fold selectivity over δ opioid (IC50=4500 nM) and somatostatin receptors. CTAP(TFA） (103429-32-9 free base) can be used for the study of L-DOPA-induced dyskinesia (LID)

AY 77 (Unk-Cha-Chg-NH2) is a potent and selective PAR2 agonist. AY 77 showed selectivity for Ca2+ and ERK1/2 signaling (ec50 value of Ca2+ release was 40 nM and ec50 value of ERK1/2 phosphorylation was 2 μM). AY 77 can promote migration of human breast cancer cells in vitro.

Bombinakinin M acetate is a potent bradykinin receptor agonist with high selectivity for mammalian arterial smooth muscle bradykinin receptors and is approximately 50 times more potent than bradykinin.

[(pF)Phe4]Nociceptin(1-13)NH2 acetate is a selective agonist of NOP receptor with a pKi of 10.68 and a pEC50 of 9.31. [(pF)Phe4]Nociceptin(1-13)NH2 acetate displays high selectivity over δ, κ, and μ opioid receptors (>3000 fold).

Cilengitide (EMD 121974) is a potent integrin inhibitor for the αvβ3/5 receptor (IC50: 4.1/79 nM, in cell-free assays); ~10-fold selectivity against gpIIbIIIa.

AP 811 acetate is a selective antagonist of the atrial natriuretic peptide clearance receptor (ANP-CR, NPR3), demonstrating high affinity with a K_i value of 0.48 nM and exhibiting over 20,000-fold selectivity for NPR3 compared to NPR1. It effectively inhibits ANP-induced pump stimulation [1] [2].

AP 811, a selective antagonist of the atrial natriuretic peptide clearance receptor (APN-CR, NPR3) with a K i value of 0.48 nM, exhibits remarkable selectivity for NPR3 over NPR1 by more than 20,000-fold. Moreover, AP 811 effectively eliminates ANP-induced pump stimulation.

AC 187 TFA, a potent and orally active amylin receptor antagonist, exhibits an IC50 of 0.48 nM and a Ki of 0.275 nM. It demonstrates greater selectivity for the amylin receptor over calcitonin and CGRP receptors and has been shown to possess neuroprotective effects [1] [2].

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 noc

Selective NaV1.7 channel blocker. Shifts activation gating positively and decreases current magnitude. Displays 100-fold selectivity over other sodium channel subtypes.

Evybactin, a DNA gyrase inhibitor, selectively targets Mycobacterium tuberculosis, demonstrating a minimum inhibitory concentration (MIC) value of 0.25 µg/mL. It stands out as the initial antimicrobial agent to utilize this distinct mechanism of selectivity [1].

Potent somatostatin receptor 1 (sst1) agonist; displays selectivity for sst1 (IC50 values are 30.9 nM, 345 nM, > 1 μM, > 10 μM and > 10μM for human sst1, sst3, sst4, sst2 and sst5 respectively). Attenuates somatostatin release in the rat nucleus accumbens

Selective antagonist of α3β4 nicotinic acetylcholine receptors. Displays > 100-fold selectivity over other receptor subunit combinations including α2β2, α2β4, α3β2, α4β2, α4β4 and α1β1γδ.

Potent, selective and competitive silent antagonist for the NOP opioid receptor. Binds to NOP with high affinity (pKi = 10.24) and displays > 3000-fold selectivity over δ, μ and κ opioid receptors. Antinociceptive and opposes the action of nociceptin in v

UFP-101 TFA is a potent, selective, and competitive N/OFQ peptide (NOP) receptor antagonist, boasting a pK i value of 10.24 and demonstrating over 3000-fold selectivity against δ, μ, and κ opioid receptors. It exhibits antidepressant-like effects [1] [2].

Deltorphin acetate is a substance obtained from the skin secretions of a frog, Phyllomedusa bicolor and shows high selectivity and affinity for δ-opioid receptor.

WL47 is a high-affinity ligand for caveolin-1 (CAV1) with a dissociation constant (Kd) of 23 nM, demonstrating potent disruption of CAV1 oligomers. This compound exhibits selectivity for CAV1, with minimal interaction towards BSA, casein, and HEWL. Notably, WL47's molecular structure is 80% smaller than its T20 parent sequence, rendering it a useful tool for investigating caveolin-1 function [1].

Endogenous melanocortin MC3 receptor agonist (pKi = 7.46) that displays ~ 40-fold selectivity over MC4. Increases the release of extracellular dopamine, which induces grooming and vertical activity (rearing) in rats. Exhibits hypertensive, tachycardic and

Potent and selective NADPH oxidase 1 (NOX1) inhibitor (IC50 = 20 nM). Exhibits selectivity for NOX1 over NOX2, NOX4, NOX5 and xanthine oxidase. Inhibits NOX1-derived O2- production in HT-29 human colon cancer cells. Attenuates VEGF-induced human pulmonary

Potent and selective μ opioid receptor antagonist (IC50 = 3.5 nM). Displays > 1200-fold selectivity over δ opioid and somatostatin receptors. Brain penetrant and active in vivo.

[Ala11,D-Leu15]-Orexin B acetate is a selective agonist of orexin-2 receptor (OX2) with an EC50 of 0.13 nM, showing 400-fold selectivity over OX1 (52 nM).

Potent neuropeptide Y (NPY) Y5 receptor agonist (pEC50 values are 7.82, 6.28, 6.44 and > 6 at rat Y5, Y4, Y1 and Y2 receptors respectively) that displays > 26-fold, > 1000-fold and > 1000-fold selectivity over Y1, Y2 and Y4 receptors respectively. Induces

α-Conotoxin MII is a highly potent and selective competitive antagonist for α3β2 subunit-containing nicotinic receptors (IC50 = 0.5 - 3.5 nM at α3β2 expressed in Xenopus oocytes). Also potently blocks β3-containing neuronal nicotinic receptors. Displays >

Selective competitive inhibitor of myosin light chain kinase (IC50 = 50 nM). Displays 4000-fold selectivity over CaM kinase II and does not inhibit PKA. Cell permeable.

GpTx-1 exhibits potent selectivity as a NaV1.7 antagonist, demonstrating an inhibition concentration (IC50) of 10 nM [1].

Blocker of Kir1.1 channels; displays >250-fold selectivity for Kir1.1 (Kd values are 1.1, 274 and 361 nM for Kir1.1, Kir3.1/3.2 and Kir3.1/3.4 respectively). Derivative of tertiapin-Q.

γ1-MSH TFA, a melanocortin MC3 receptor agonist, demonstrates a binding affinity (K i) of 34 nM for the rat MC3 receptor. Notably, it exhibits approximately 40-fold greater selectivity for the MC3 receptor compared to the MC4 receptor, with a K i of 1318 nM for MC4 [1].

[Arg14,Lys15]Nociceptin TFA is a potent and selective agonist for the NOP receptor (ORL1; OP4), exhibiting an EC50 of 1 nM. It demonstrates significant selectivity against opioid receptors, with IC50 values of 0.32 nM for NOP, and 280, >10000, and 1500 nM for μ, δ, and κ receptors, respectively [1].

Potent melanin-concentrating hormone (MCH) receptor agonist (EC50 values are 17 and 54 nM at MCH1 and MCH2 receptors respectively). Displays some selectivity towards MCH1 over MCH2 (Ki values are 0.16 and 34 nM respectively).

'(D-Arg8)-Inotocin is a potent, selective, and competitive antagonist of the vasopressin receptor (V 1a R), exhibiting a binding affinity (K i) of 1.3 nM. It demonstrates over 3000-fold selectivity for the human V1aR compared to the OTR, V1bR, and V2R subtypes [1].'

UFP101 is a synthetic peptide that functions as an antagonist of the nociceptin receptor, demonstrating high affinity with a Ki of 0.06 nM in CHO cells expressing the human receptor. It exhibits selectivity for the nociceptin receptor over the κ-opioid receptor, with a Ki of 204 nM in CHO cells expressing the rat receptor. The compound effectively inhibits GTPγS release from the nociceptin receptor in CHO cell membranes, with an EC50 of 1.86 nM. When administered intracerebroventricularly at a dose of 10 nmol/animal, UFP101 prolongs the latency to tail withdrawal in the tail-flick test in mice, indicating its potential as an analgesic. Additionally, at doses of 0.003, 0.03, and 0.3 mg/kg, UFP101 enhances survival in a sepsis mouse model induced by cecal ligation and puncture, suggesting potential therapeutic applications in sepsis management.

CTAP TFA, a potent and highly selective μ opioid receptor antagonist that effectively crosses the blood-brain barrier, exhibits a significant inhibition concentration (IC50) of 3.5 nM. It demonstrates extraordinary selectivity, being over 1200-fold more specific to μ opioid receptors than to δ opioid (IC50 = 4500 nM) and somatostatin receptors. This compound is primarily leveraged for researching L-DOPA-induced dyskinesia (LID) and opiate overdose or addiction [1] [2].

[Ala11,D-Leu15]-Orexin B(human) TFA is a potent, selective agonist for the orexin-2 receptor (OX2), demonstrating 400-fold higher selectivity for OX2 (EC 50 =0.13 nM) compared to the orexin-1 receptor (OX1) with an EC 50 of 52 nM.

Dermorphin Analog is an analog of Dermorphin. Dermorphin is a natural heptapeptide μ-opioid receptor agonist found in amphibian skin. The dermorphin-derived peptide [Dmt1] dermorphin analog labels m-opioid receptors with high affinity and selectivity in r

FR 113680 is a tripeptide substance P antagonist with NK1 receptor selectivity.

High affinity, selective KCa2.2 (SK2) channel blocker (Kd = 3.8 nM). Exhibits >200-fold selectivity for KCa2.2 over KCa2.1, KCa2.3, KCa3.1, IK, Kv and Kir2.1. Increases theta-burst responses and increases LTP in rat hippocampal slices in vitro. Convulsive

MitTx-alpha, a component of the complex MitTx, acts as a powerful and enduring agonist specifically targeting acid-sensing ion channels (ASICs), with a pronounced selectivity for ASIC1 under neutral pH conditions. At lower pH levels (pH<6.5), MitTx significantly amplifies (over 100-fold) the activation of ASIC2a channels induced by protons [1].

MitTx, a complex consisting of MitTx-α and MitTx-β, serves as an ASIC1 channel activator, demonstrating EC50 values of 9.4 nM and 23 nM for the ASIC1a and ASIC1b isoforms, respectively. It exhibits high selectivity for ASIC1 isoforms at neutral pH, while under acidic conditions, it substantially potentiates proton-evoked activation of the ASIC2a channel [1].

Ala-parafluoroPhe-Arg-Cha-Cit-Tyr-NH2 is a biologically active peptide functioning as a selective agonist for Protease Activated Receptor 1 (PAR-1), a subtype of G-protein coupled receptors involved in mediating thrombin's cellular effects. Exhibiting high specificity for PAR-1 over PAR-2, its selectivity was assessed via cell-based calcium signaling assays in HEK293 cells. As an agonist, it is instrumental for in vivo investigations of PAR-1 activation. PAR-1 also collaborates with PAR-4, influencing thrombin-induced hepatocellular carcinoma within 'coagulation type' tumor environments where thrombin generation occurs.

SMAP-18, an 18-amino acid residue peptide amide, is a biologically active truncated variant of Sheep myeloid antimicrobial peptide-29 (SMAP-29). It retains potent antimicrobial activity against Pseudomonas strains, other Gram-negative bacteria, and multidrug-resistant pathogens. Notably, SMAP-18 exhibits increased cell selectivity relative to the parent peptide SMAP-29 due to its reduced hemolytic activity while maintaining its antimicrobial efficacy.

K 41498 is a selective peptide antagonist targeting both corticotropin-releasing factor receptor 2α (CRF2α) and CRF2β, demonstrating high affinity with Kis of 0.66 and 0.62 nM, respectively, in HEK293 cells expressing these human receptors. Its selectivity is evident as it exhibits a significantly reduced affinity for CRF1 receptor (Ki = 425 nM in HEK293 cells expressing the human CRF1 receptor). Additionally, K 41498, when administered intravenously at 1.84 µg/animal, effectively mitigates urocortin-induced hypotension in rats. Furthermore, its intrathecal delivery ranging from 0.075 to 0.5 µmol/animal significantly lowers the mechanical paw withdrawal threshold in a rat model, indicating its potential utility in managing nociception triggered by complete Freund's adjuvant.

UDP-β-S, serving as a specific agonist for the purinergic P2Y6 receptor, effectively promotes inositol phosphate accumulation in 1321N1 cells containing P2Y6 receptors, with an EC50 value of 28 nM. This selectivity is evident when compared to its effects on cells expressing P2Y1, P2Y2, or P2Y4 receptors, where a concentration of 10 µM is used. Additionally, at a concentration of 1 µM, UDP-β-S stimulates DNA synthesis in isolated rat aorta smooth muscle cells.

Helianorphin-19 is a high affinity, potent and selective κ-opioid receptor (KOR) agonist (Ki = 25 nM; EC50= 45 nM). Helianorphin-19 exhibits approximately 200-fold selectivity for KOR over μ and δ-opioid receptors.In vivoHelianorphin-19 shows potent peripheral analgesic efficacy in a mouse model of visceral pain without affecting motor coordination/sedation.

Lei-Dab7 TFA, a selective and high-affinity blocker of the K Ca 2.2 (SK2) channel with a dissociation constant (K d) of 3.8 nM, demonstrates over 200-fold selectivity for K Ca 2.2 compared to K Ca 2.1, K Ca 2.3, K Ca 3.1, K v, and Kir2.1. Furthermore, Lei-Dab7 TFA enhances theta-burst responses and long-term potentiation (LTP) in rat hippocampal slices in vitro.