Home > Inhibitors & Agonists > GPCR > Opioid Receptor
Cat. No. Product name CAS No.
DC7050 ADL5859 HCl

ADL5859 agonizes δ-opioid receptor with a 1000-fold selectivity than µ- or κ-opioid receptor with Ki of 32 nM and 37 nM, respectively.ADL5859 displays weak inhibitory activity at the hERG channel with an IC50 of 78 μM. The EC50 of ADL5859 against δ opioid receptor is 20 nM. At the screening dose of 3 mg/kg p.o., ADL5859 produces 100% reversal of hyperalgesia in the inflamed paw. The oral ED50 of ADL5859 in the FCA mechanical hyperalgesia assay is 1.4 mg/kg. The antihyperalgesia produced by ADL5859 (3 mg/kg, p.o.) is reversed by pretreatment with the δ opioid antagonist naltrindole (0.3 mg/kg s.c.), thus demonstrating a δ receptor mediated effect.In the rat Forced swim assay, ADL5859 (3 mg/kg p.o.) produces robust antidepressant-like activity, as evidenced by a significant decrease in the time spent immobile and a significant increase in the time spent swimming. The bioavailability of ADL5859 (3 mg/kg p.o.) in rats and dogs is 33% and 66%, respectively.ADL5859 efficiently reduces inflammatory and neuropathic pain mainly by recruiting δ-opioid receptors expressed by peripheral Nav1.8-expressing neurons.For the detailed information of ADL5859 HCl, the solubility of ADL5859 HCl in water, the solubility of ADL5859 HCl in DMSO, the solubility of ADL5859 HCl in PBS buffer, the animal experiment (test) of ADL5859 HCl, the cell expriment (test) of ADL5859 HCl, the in vivo, in vitro and clinical trial test of ADL5859 HCl, the EC50, IC50,and Affinity of ADL5859 HCl, Please contact DC Chemicals..

850173-95-4
DC8584 AlviMopan

Alvimopan(LY 246736; ADL 8-2698) is a peripherally acting mu-opioid receptor (PAM-OR, IC50= 1.7 nM) antagonist for accelerating gastrointestinal recovery after surgery.

156053-89-3
DC8606 Alvimopan monohydrate

Alvimopan(LY 246736; ADL 8-2698) is a peripherally acting mu-opioid receptor (PAM-OR, IC50= 1.7 nM) antagonist for accelerating gastrointestinal recovery after surgery.

1383577-62-5
DC8605 Alvimopan dihydrate

Alvimopan(LY 246736; ADL 8-2698) is a peripherally acting mu-opioid receptor (PAM-OR, IC50= 1.7 nM) antagonist for accelerating gastrointestinal recovery after surgery.

170098-38-1
DC8298 BAN ORL 24

BAN ORL 24 is a potent, selective, competitive ORL1 non-peptide agonist. Displays 1000-fold selectivity over classical opioid receptors.

1401463-54-4
DC7097 Cebranopadol(GRT-6005)

branopadol(GRT-6005) is a novel first in class compounds with potent agonist activity on ORL-1 (opioid receptor like -1) and the well established mu opioid receptor.

863513-91-1
DC10945 BU09059

BU09059 is a potent, selective, short-acting kappa-opioid receptor antagonist with Ki of 1.72 nM, displays 15- and 616-fold selectivity over μ- and δ-receptors respectively.

1541206-05-6
DC9765 CERC-501(LY-2456302,Aticaprant)

CERC-501(LY-2456302) is a potent, selective antagonist of the kappa opioid receptor (KOR) (Ki = 0.81 nM vs. 24.0 nM and 155 nM for the μ-opioid receptor (MOR) and δ-opioid receptor (DOR), respectively.

1174130-61-0
DC8626 Eluxadoline

Eluxadoline is an orally active mixed μ opioid receptor (μOR) agonist δ opioid receptor (δOR) antagonist.

864821-90-9
DC9524 JDTic (dihydrochloride)

JDTic 2Hcl is a highly selective antagonist for the κ-opioid receptor; without affecting the μ- or δ-opioid receptors.

785835-79-2
DC9526 Meptazinol (hydrochloride)

Meptazinol Hcl(WY-22811 Hcl) is a unique centrally active opioid analgesic.

59263-76-2
DC9527 Methylnaltrexone (Bromide)

Methylnaltrexone Bromide is a pheriphally-acting μ-opioid antagonist that acts on the gastrointestinal tract to decrease opioid-induced constipation.

73232-52-7
DC11171 NFEPP

NFEPP is a novel potent, selective pH-dependent μ-opioid receptor (MOR) agonist with a low pKa, shows significantly lower affinity compared with fentanyl at pH 7.4.

1422952-82-6
DC10290 PZM21

PZM21 is a potent and selective μ opioid receptor agonist with an EC50 of 1.8 nM.

1997387-43-5
DC7439 JTC-801

JTC-801 is a selective opioid receptor-like1 (ORL1) receptor antagonist with IC50 of 94 nM, weakly inhibits receptors δ, κ, and μ.

244218-51-7
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