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GPCR

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Cat. No. Product Name Field of Application Chemical Structure
DC47583 W146 TFA W146 TFA is a selective antagonist of sphingosine-1-phosphate receptor 1 (S1PR1) with an EC50 value of 398 nM.
DC47622 Cyclizine Featured Cyclizine is a piperazine first-generation antagonist of histamine 1 receptor.
DC47628 GPR84 antagonist 1 GPR84 antagonist 1 is a high affinity and highly selective competitive antagonist of human GPR84.
DC47629 5-HT7R antagonist 1 free base 5-HT7R antagonist 1 (free base) is a G protein-biased antagonist against 5-HT7R (Ki = 6.5 nM).
DC47630 5-HT7R antagonist 1 5-HT7R antagonist 1 is a G protein-biased antagonist against 5-HT7R (Ki = 6.5 nM).
DC47635 GLP-1R modulator L7-028 Featured GLP-1R modulator L7-028 is an allosteric modulator enhancing GLP-1 binding to GLP-1R via a transmembrane site (EC50 11.01 ± 2.73 μM).
DC47636 GLP-1R modulator C5 GLP-1R modulator C5 is an allosteric modulator enhancing GLP-1 binding to GLP-1R via a transmembrane site (EC50 1.59 ± 0.53 μM).
DC47637 GLP-1R modulator C16 GLP-1R modulator C16 is an allosteric modulator enhancing GLP-1 binding to GLP-1R via a transmembrane site (EC50 8.43 ± 3.82 μM).
DC47682 Dopamine D3 receptor antagonist-2 Dopamine D3 receptor antagonist-2 is a dopamine D3 receptor-selective (Ki = 2.16 nM) or multitarget bitopic ligand potentially useful for central nervous system disorders.
DC47683 Mesdopetam hemitartrate Featured Mesdopetam (IRL790) hemitartrate is a dopamine D3 receptor antagonist (Ki=90 nM; IC50=9.8 μM for human recombinant D3 receptor) with psychomotor stabilizing properties. Mesdopetam hemitartrate is used for the research of motor and psychiatric complications in Parkinson disease.
DC47684 Dopamine D3 receptor antagonist-1 Dopamine D3 receptor antagonist-1 is a dopamine D3 receptor-selective or multitarget bitopic ligand (Ki = 1.58 nM) potentially useful for central nervous system disorders.
DC47764 Azepexole dihydrochloride Azepexole (B-HT 933) dihydrochloride is a potent and selective alpha 2-adrenoceptor agonist with pKis of 8.3, 7.6, and 7.5 for α2A-, α2B- and α2C-adrenoceptor subtypes, resepctively. Azepexole dihydrochloride causes concentration-dependent inhibition of peristaltic contractions (IC50= 78.72 nM).
DC47765 hA3AR agonist 1 hA3AR agonist 1 is a potent human A3 adenosine receptor (hA3AR) agonist with a Ki value of 2.40 nM.
DC47766 Adenosine receptor antagonist 1 Adenosine receptor antagonist 1 is a A2aR-selective antagonist with an IC50 of 0.29 nM and displays 14-fold more selective for A2aRthan A2bR.
DC47767 N6-Benzyl-5'-ethylcarboxamido adenosine N6-Benzyl-5'-ethylcarboxamido adenosine is a selective A3 adenosine receptor agonist.
DC47777 FPPQ FPPQ is a dual-acting 5-HT3 (Ki = 0.9 nM) and 5-HT6 (Ki = 3 nM) receptor antagonist with antipsychotic and procognitive properties.
DC47905 SB-206606 SB-206606, a stereoisomer of BRL 37344, is a potentially specific, beta 3-adrenergic receptor (β3-AR) ligand. The affinity of [3H]SB 206606 is 76 times higher for the β3-AR than for the beta 1/beta 2-adrenergic receptors.
DC47908 S-22153 S-22153 is a potent melatonin receptor antagonist with EC50 values of 19 nM, 4.6 nM for hMT1 and hMT2 melatonin receptor, respectively. S-22153 has Ki values of 8.6 nM (CHO cells) and 16.3 nM (HEK cells) for hMT1, and 6.0 nM (CHO cells) and 8.2 nM (HEK cells) for hMT2. S-22153 is a specific ligand of MT1 and MT2 melatonin receptors subtypes.
DC47909 S1P1 agonist 3 S1P1 agonist 3 is a selective G-protein-biased sphingosine-1 phosphate receptor-1 (S1P1 ) agonist for endothelial protection.
DC47911 Roxindole hydrochloride Roxindole hydrochloride (EMD 38362), an indot-alkyl-pipenidine, is a potent agonist at dopamine autoreceptors, with an affinity for the D2-like subtype in the low nanomolar range. Roxindole can be used for the research of positive and negative schizophrenic symptoms. Roxindole is a 5-HT1A agonist and 5-HT uptake inhibitor with high affinity for 5-HT1A (IC50=0.9 nM). Antipsychotic and antidepressant activities.
DC47955 LY266097 hydrochloride LY266097 hydrochloride is a selective 5-HT2B receptor antagonist with pKis of 7.7, 9.8, and 7.6 for 5-HT2A, 5-HT2B, 5-HT2C, respectively. 5-HT2B receptor blockade contributes to the research in depression.
DC47957 LSN3318839 Featured LSN3318839 is an orally efficacious positive allosteric modulator of the glucagon-like peptide-1 receptor (GLP-1R).
DC48026 Cerlapirdine Cerlapirdine (SAM-531, PF-05212365) is a selective and potent full antagonist of the 5-hydroxytryptamine 6 (5-HT6) receptor. Cerlapirdine has the potential for researching the Alzheimer's disease.
DC48031 CB2 receptor agonist 2 CB2 receptor agonist 2 is a potent and selective agonist for the CB2 (cannabinoid type 2) receptor with a Ki of 8.5 nM. CB2 receptor agonist 2 has high affinity and selectivity for CB2.
DC48037 Bopindolol fumarate Bopindolol ((±)-Bopindolol) fumarate is an orally active antagonist of β-adrenoceptors (ARs) with partial agonist activity. Bopindolol fumarate is non-selective for β1- and β2-ARs and has low affinity for β3-AR subtype. Bopindolol fumarate is a prodrug of pindolol and can be used for essential and renovascular hypertension research.
DC48039 BMS-753426 BMS-753426 is a potent and orally bioavailable antagonist of CCR2.
DC48046 AZD-5672 Featured AZD-5672 is an orally active, potent, and selective CCR5 antagonist (IC50=0.32 nM). AZD-5672 shows moderate activity against the hERG ion channel (binding IC50=7.3 μM). AZD5672 is a substrate of human P-gp, and inhibits P-gp-mediated digoxin transport (IC50=32 μM). AZD-5672 can be used for the research of rheumatoid arthritis.
DC48143 Usmarapride free base Usmarapride (SUVN-D4010) free base is a potent, selective, orally active and brain penetrant 5-HT4 receptor partial agonist (EC50=44 nM). Usmarapride (SUVN-D4010) free base can be used for the research of cognitive deficits associated with Alzheimer's disease.
DC48144 ST1936 ST1936 is a selective, nanomolar affinity 5-HT6 receptor agonist with Ki values of 13 nM, 168 nM and 245 nM for human 5-HT6, 5-HT7 and 5-HT2B receptors, respectively. ST1936 also shows moderate affinity (Ki of 300 nM) for human and rat α2 adrenergic receptor.
DC48145 Besipirdine Besipirdine is a non-receptor-dependent cholinomimetic agent with noradrenergic activity. Besipirdine inhibits voltage-dependent sodium and potassium channels.

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