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GPCR

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Cat. No. Product Name Field of Application Chemical Structure
DC78758 U 93385
U93385 is a 5-HT₁A receptor agonist. U93385 exhibits no significant α₂ adrenergic, D₂ dopamine, or other receptor activities. U93385 has a heart rate regulating effect, stimulating the vagus nerve to induce bradycardia. U93385 can be used to study the 5-HT₁A receptor-mediated vagal nerve tolerance mechanism.
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DC78754 Dicytidine 5′-triphosphate
Dicytidine 5′-triphosphate (Cp3C) is a cytosine-containing dinucleoside polyphosphate. Dicytidine 5′-triphosphate inhibits the intracellular accumulation of trans-resveratrol and trans-piceid. Dicytidine 5′-triphosphate induces the expression of CCR2 and upregulates the expression of PAL1 and 4CL1.
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DC78747 MDL 105212A
MDL 105212A is a potent and orally active nonpeptide neurokinin receptor (NK-1/NK-2) tachykinin receptor antagonist. MDL 105212A can be used for the researches of inflammation, immunology and neurological disease, such as asthma.
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DC78746 TD-6301
TD-6301 is a bladder-selective M2/4 muscarinic receptor antagonist. TD-6301 binds to and blocks M2/4 muscarinic receptors with high selectivity, especially human M2 receptors with strong affinity (Ki = 0.36 nM). TD-6301 inhibits volume-induced bladder contractions (ID50 = 0.075 mg/kg). TD-6301 can be used in the research of overactive bladder.
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DC78745 BC264
BC264 is a highly potent and selective CCK-B agonist that crosses the blood-brain barrier. BC264 increases dopamine in the nucleus accumbens and facilitates motivation and attention in rats.
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DC78742 BP 554
BP 554 is a selective 5-HT1A receptor agonist and Piperazine derivative. BP 554 leads to hypothermia.
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DC78717 EMD 86006
EMD 86006 is a candidate for selective serotonin inhibitors. EMD 86006 has the potential for research on depressive disorders.
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DC78710 RAGE406R
RAGE406R is an orally active RAGE-DIAPH1 interaction antagonist. RAGE406R can bind to ctRAGE and prevent the formation of the RAGE-DIAPH1 complex and inhibit its interaction. RAGE406R can reduce the expression of CCL2, TNF, and IL-6 in THP1 cells. RAGE406R suppresses delayed-type hypersensitivity in T2D mice. RAGE406R can be used for the study of diabetes.
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DC78706 RS 2232
RS 2232 is an orally active, competitive 5-HT deamination inhibitor with a Ki of 0.054 μM. RS-2232 exhibits reversible and specific inhibition of type A monoamine oxidase. RS 2232 can be used in brain research.
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DC78685 BMS-181101 hydrochloride
BMS-181101 (hydrochloride) is an orally active antidepressant. BMS-181101 (hydrochloride) can interact with a variety of central presynaptic and postsynaptic 5-HT receptors. BMS-181101 (hydrochloride) can be used in the research of diseases such as depression.
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DC78681 Nebivolol O-β-D-glucuronide
Nebivolol O-β-D-glucuronide is a derivative of Nebivolol. Nebivolol is an orally active beta receptor blocker and has the high beta(1)-receptor affinity. Nebivolol has direct vasodilator properties and adrenergic blocking characteristics. Nebivolol can be used for the research of kinds of diseases such as hypertension, coronary artery disease, congestive heart failure and ischemic heart disease.
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DC78674 CHO-4′Me-5′Br-FUBOXPYRA
CHO-4’Me-5’Br-FUBOXPYRA (CH-FUBBMPDORA) is an oxopyridine carboxamide that shares a similar structure to known synthetic cannabinoids. CHO-4’Me-5’Br-FUBOXPYRA demonstrates limited activation potential at both cannabinoid receptors CB1 and CB2.
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DC78662 R 1485 dihydrochloride
R 1485 is a 5-HT6 receptor antagonist.
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DC78654 MARY1
MARY1 is a selective 5-HT2BR antagonist with an IC50 of 380 nM and a Ki of 764 nM (human 5-HT2BR). MARY1 induces renal mitochondrial biogenesis (MB) and enhances renal mitochondrial function by increasing mitochondrial respiratory capacity, mitochondrial protein levels, and mitochondrial number in renal proximal tubular cells (RPTCs). MARY1 induces MB through 5-HT2BR and dual PI3K/AKT and RAS/MEK/ERK cell signaling pathways in RPTCs. MARY1 can be used to study renal diseases associated with metabolic and mitochondrial dysfunction.
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DC78640 BRL-52656
BRL-52656 is a blood-brain barrier (BBB)-penetrable KOR receptor agonist that exhibits a biphasic effect. At low doses, BRL-52656 decreases blood pressure, whereas high doses have the opposite effect in spontaneously hypertensive rats. Additionally, BRL-52656 induces water diuresis by inhibiting the secretion of vasopressin (AVP).
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DC78639 CJ-17493
CJ-17493 is a neurokinin-1 (NK1) receptor antagonist, with a Ki of 0.2 nM. CJ-17493 shows moderate affinity for the verapamil-binding site of L-type Ca2+ channels (IC50 = 164 nM) and site 2 of sodium channels (IC50 = 48 nM). CJ-17493 can be used for the study of neurological diseases.
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DC78619 DL-017
DL-017 is a Quinazoline derivative. DL-017 shows inhibitory constants of approximately 0.90 nM for α1-adrenergic receptors and 404 nM for Na+ channels. DL-017 exerts antihypertensive effect.
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DC78610 BMS-210285
BMS-210285 is a highly selective agonist for the β3 receptor. BMS-210285 can be studied for obesity and type 2 diabetes research.
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DC78606 CB2R ligand-1
CB2R ligand-1 (Compound L14) is a selective Cannabinoid type 2 receptor (CB2R) ligand with a with Ki of 0.16  nM for CB2R over CB1R. CB2R ligand-1 as be used as a tracer for positron emission tomography (PET) imaging of neurodegenerative diseases, inflammation and cancer.
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DC78599 UVI3502
UVI3502 is a cannabinoid receptor 1 (CB1) antagonist with an IC50 value of 4641 nM for CB1 and approximately 16200 nM for CB2. UVI3502 blocks Gi/o protein coupling induced by the agonist CP55,940. UVI3502 is promising for research of endocannabinoid system-related diseases in the central nervous system (such as cognitive impairment and neurodegenerative diseases).
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DC78596 ST171
ST171 is a bitopic 5-HT1AR agonist with an Ki of 0.41  nM. ST171 selectively activates Gi/o signaling pathway and inhibits 5-HT1AR-mediated cAMP accumulation without Gs activation and marginal β-arrestin recruitment. T171 reduces hypersensitivity in chronic neuropathic and inflammatory pain mice model. ST171 can be used for pain research.
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DC78595 IP-66
IP-66 is a potent postsynaptic alpha-receptor antagonist. IP-66 can be used for the research of cardiovascular disease, such as hypertension.
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DC78576 5-HT2AR ligand 1
5-HT2AR ligand 1 (Compound 2 cis) is a 5-HT2AR ligand with nanomolar affinity for 5-HT2AR (Ki: 32 nM). 5-HT2AR ligand 1 is capable of inducing β-arrestin 2 recruitment. 5-HT2AR ligand 1 can be used in the research of neurological diseases.
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DC78568 β-Blocker B-24/76
β-Blocker B-24/76 is a beta adrenoceptor blocker. β-Blocker B-24/76 exhibits beta 1-adrenoceptor blocking and beta 2-adrenoceptor stimulating properties. β-Blocker B-24/76 can suppress the increased ornithine decarboxylase activity in hypertrophied hearts. β-Blocker B-24/76 can be used for the research of cardiovascular disease.
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DC78560 Dopamine D3 receptor ligand-6
Dopamine D3 receptor ligand-6 (Compound 196476) is a selective dopamine D3 receptor (D3) antagonist. Dopamine D3 receptor ligand-6 is promising for research of substance use disorders (such as opioid and psychostimulant addiction).
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DC78557 L-759656
L-759656 is a selective cannabinoid CB2 receptor agonist, with the Ki of 11.8 nM for the human CB2 receptor. L-759656 potently inhibits Forskolin-stimulated cyclic AMP production in Chinese Hamster Ovary (CHO) cells, with an EC50 of 3.1 nM. L-759656 can be used for the study of immune-related diseases and inflammatory diseases.
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DC78556 (±)-WB 4101
(±)-WB 4101 is a highly selective α1-adrenergic receptor antagonist. (±)-WB 4101 blocks norepinephrine-induced vascular smooth muscle contraction to exert antihypertensive and benign prostatic hyperplasia (BPH)-relieving effects. (±)-WB 4101 is promising for research of hypertension and BPH.
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DC78554 F-14258
F-14258 is a 5-HT1B/1D receptor agonist. F-14258 can achieve receptor specific analgesia through local administration. F-14258 can be used for research on ear pain.
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DC78550 TGF-8027
TGF-8027 is a selective 5-HT2A agonist that can cross the blood-brain barrier. TGF-8027 exhibits EC50s of 3.3 nM, 160 nM and 7600 nM against 5-HT2A, 5-HT2C and 5-HT2B and exhibits EC50s against mouse 5-HT2A and mouse 5-HT2C of 14 and 210 nM. TGF-8027 can induce a head-shaking response in mice. TGF-8027 can be used to study diseases that target the 5-HT2A receptor (such as depression).
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DC78543 Y-36912
Y-36912 is an orally active, highly selective and affinity 5-HT4 receptor agonist (Ki = 1.5 nM). Y-36912 can accelerate gastric emptying and increase bowel frequency and stool weight. Y-36912 can be used for research on gastrointestinal conditions.
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