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GPCR

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Cat. No. Product Name Field of Application Chemical Structure
DC40872 DuP 734
DuP 734 is a sigma receptor antagonist. DuP 734 is a selective and potent sigma and 5-HT2 receptor ligand with weak affinity for D2 receptors. DuP 734 may have antipsychotic activity without the liability of motor side effects typical of neuroleptics.
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DC40871 Panamesine
Panamesine (EMD 57445) is a sigma receptor ligand, which has a high affinity (IC50 6 nM) and selectivity for sigma binding sites. Panamesine is a potential atypical neuroleptic agent.
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DC40856 PM226
PM226 is a selective cannabinoid CB2R agonist (Ki (CB2R)=13 nM; EC50 (CB2R)=39 nM; Ki (CB1R) >40 μM;) with neuroprotective properties in vitro and vivo.
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DC40855 PSB 0777 ammonium
PSB 0777 ammonium is a potent and selective adenosine A2A receptor full agonist with Ki values of 44.4 nM, 360 nM for rat and human A2A receptors, respectively. PSB 0777 ammonium has Ki values of ≥10000 nM, 541 nM for rat and human A1 receptors, respectively. PSB 0777 ammonium shows poor brain penetrant and perorally non-absorbable effect. PSB 0777 ammonium has the potential for inflammatory bowel disease (IBS) research research.
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DC40852 TAN-452
TAN-452 is an orally active, selective peripherally acting δ-opioid receptor (DOR) antagonist with a Ki of 0.47?nM and a Kb of 0.21?nM. TAN-452 is an antagonist for μ-opioid receptor (MOR; Ki=36.56?nM and Kb=9.43?nM) and κ-opioid receptor (KOR; Ki=5.31?nM and Kb=7.18?nM). TAN-452, a derivative of Naltrindole, demonstrates low brain penetrability and attenuates morphine-induced side effects without affecting pain control.
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DC40780 AZD2423
AZD2423 is a potent, selective, orally bioavailable, and non-competitive CCR2 chemokine receptor negative allosteric modulator. AZD2423 has an IC50 of 1.2 nM for CCR2 Ca2+ flux .
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DC40767 (S)-Verapamil D7 hydrochloride
(S)-Verapamil D7 hydrochloride ((S)-(-)-Verapamil D7 hydrochloride) is a deuterium labeled (S)-Verapamil hydrochloride. (S)-Verapamil hydrochloride (S(-)-Verapamil hydrochloride) inhibits leukotriene C4 (LTC4) and calcein transport by MRP1. (S)-Verapamil hydrochloride leads to the death of potentially resistant tumor cells.
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DC40761 Rupatadine D4 fumarate
Rupatadine D4 fumarate (UR-12592 D4 fumarate) is a deuterium labeled Rupatadine fumarate. Rupatadine Fumarate (UR-12592 Fumarate) is a potent dual PAF/H1 antagonist with Ki of 0.55/0.1 μM(rabbit platelet membranes/guinea pig cerebellum membranes).
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DC40729 Olmesartan impurity
Olmesartan impurity is an Olmesartan impurity. Olmesartan (RNH-6270) is an angiotensin II receptor (AT1R) antagonist has the potential for high blood pressure study.
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DC40627 mGluR2 antagonist 1
mGluR2 antagonist 1 is a highly potent, orally bioavailable and selective class of mGluR2 negative allosteric modulator (IC50 of 9 nM) with excellent brain permeability.
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DC40610 O-2050
O-2050 is a high affinity cannabinoid CB1?receptor silent antagonist. O-2050 also acts as a partial agonist in inhibiting forksolin-induced cyclic AMP stimulation (EC50=40.4 nM). O-2050 antagonizes effects of?CP-55940 in vitro.
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DC40588 Mabuterol-D9
Mabuterol-D9 is a deuterium labeled Mabuterol. Mabuterol is an agonist of the β2-adrenergic receptor.
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DC40572 Terazosin dimer impurity dihydrochloride
Terazosin dimer impurity dihydrochloride, a dimer of Terazosin, is an impurity of Terazosin. Terazosin is a quinazoline derivative and a competitive and orally active α1-adrenoceptor antagonist.
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DC40561 LY3020371
LY3020371 is a potent and selective antagonist of glutamate (mGlu) 2/3 receptor, with Kis of 5.26 and 2.50 nM for hmGluR2 and hmGluR3, respectively. LY3020371 can be used for the research of depression.
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DC40554 Olmesartan methyl ester
Olmesartan methyl ester is an intermediate in the synthesis of Olmesartan medoxomil. Olmesartan medoxomil is a potent and selective angiotensin AT1 receptor antagonist with IC50 of 66.2 μM.
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DC40553 Dehydro Olmesartan
Dehydro Olmesartan is a derivative of Olmesartan. Olmesartan is an angiotensin II receptor (AT1R) antagonist and has the potential for high blood pressure study.
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DC40552 Olmesartan lactone impurity
Olmesartan lactone impurity is a cyclic ester impurity of Olmesartan. Olmesartan is an angiotensin II receptor (AT1R) antagonist and has the potential for high blood pressure study.
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DC40540 Olmesartan medoxomil impurity C
Olmesartan medoxomil impurity C is an Olmesartan medoxomil impurity. Olmesartan medoxomil is a potent and selective angiotensin AT1 receptor inhibitor with IC50 of 66.2 μM.
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DC40532 Cetirizine Impurity C
Cetirizine Impurity C is an impurity of Cetirizine. Cetirizine, a second-generation antihistamine and the carboxylated metabolite of hydroxyzine, is a specific, orally active and long-acting histamine H1-receptor antagonist[1][2].
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DC40531 Ziprasidone amino acid
Ziprasidone amino acid (Ziprasidone Impurity C) is an impurity of Ziprasidone. Ziprasidone is a combined 5-HT (serotonin) and dopamine receptor antagonist. Ziprasidone exhibits potent effects of antipsychotic activity .
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DC40516 Brombuterol hydrochloride
Brombuterol hydrochloride (Bromobuterol hydrochloride) is a β-adrenergic receptor agonist.
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DC40492 Clorprenaline D7
Clorprenaline D7 is a deuterium labeled Clorprenaline. Clorprenaline is a β2-adrenergic receptor agonist that is implicated in bronchial expansion. Clorprenaline has the potential for asthma research.
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DC40491 Cimbuterol-D9
Cimbuterol-D9 is the deuterium labeled Cimbuterol. Cimbuterol is aβ-adrenergic agonist.
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DC40490 Brombuterol D9
Brombuterol D9 (Bromobuterol D9) is a deuterium labeled Brombuterol. Brombuterol is a β-adrenergic receptor agonist.
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DC40489 Brombuterol D9 hydrochloride
Brombuterol D9 hydrochloride (Bromobuterol D9 hydrochloride) is a deuterium labeled Brombuterol hydrochloride. Brombuterol hydrochloride is a β-adrenergic receptor agonist.
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DC40488 Phenylethanolamine A-D3
Phenylethanolamine A-D3 is a deuterium labeled Phenylethanolamine A. Phenylethanolamine A acts as a β-adrenergic agonist. Phenylethanolamine A is a byproduct during the Ractopamine synthesis process.
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DC40487 Phenylethanolamine A
Phenylethanolamine A acts as a β-adrenergic agonist. Phenylethanolamine A is a byproduct during the Ractopamine synthesis process.
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DC40403 Bisoprolol
Bisoprolol is a potent, selective and orally active β1-adrenergic receptor blocker. Bisoprolol has little activity on β2-receptor and has the potential for hypertension, coronary artery disease and stable ventricular dysfunction research.
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DC40396 KAG-308
KAG-308 is a potent selective and orally active agonist of EP4 receptor (a prostaglandin E2 receptor subtype), suppresses colitis and promotes histological mucosal healing, potently inhibits TNF-α production. KAG-308 shows a Ki and an EC50 of 2.57 nM and 17 nM for human EP4 receptor, respectively, more selective over EP1, EP2, EP3 and IP receptor.
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DC40381 Dibenamine hydrochloride
Dibenamine hydrochloride is a competitive and irreversible?adrenergic blocking agent and?is known to modify the pharmacological effects of epinephrine. Dibenamine hydrochloride cause a significant increase in the rate of destruction of I-epinephrine in the mouse.
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