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GPCR

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Cat. No. Product Name Field of Application Chemical Structure
DC78153 (1R,2S)-Dihydrobupropion
(1R,2S)-Dihydrobupropion is a norepinephrine-dopamine reuptake inhibitor. (1R,2S)-Dihydrobupropion is one of the active metabolites of Bupropion. (1R,2S)-Dihydrobupropion can be used for the researches of neurological disease and inflammation.
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DC78151 KRG-3332 hydrochloride
KRG-3332 (hydrochloride) is a selective α1A receptor antagonist. KRG-3332 (hydrochloride) can be used in Glaucoma.
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DC78144 Ifoxetine
Ifoxetine (CGP 15210G) is an inhibitor of 5-HT reuptake. Ifoxetine specifically and selectively blocks the 5-HT reuptake in the brain without affecting the 5-HT uptake processes in the periphery (blood platelets). Ifoxetine inhibits the uptake of radiolabelled 5-HT into rat brain synaptosomes in vitro or ex vivo. Ifoxetine has antidepressant properties.
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DC78143 OPC-4392
OPC-4392 is a orally active presynaptic dopamine autoreceptor agonist and postsynaptic D2 receptor antagonist. OPC 4392 reverses the Reserpine-induced dopamine accumulation, inhibits Apomorphine-induced stereotypic and climbing behaviors in mouse models. OPC-4392 can be used as antipsychotic agent.
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DC78135 Sigma-2 Receptor ligand 1
Sigma-2 Receptor ligand 1 (Compound 7i) is a highly selective Sigma-2 receptor ligand with a Ki value of 40 nM. Sigma-2 Receptor ligand 1 is promising for research of Alzheimer's disease.
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DC78134 S-14489
S-14489 is an orally active selective postsynaptic 5-HT1A receptor antagonist with a pKi of 9.2. S-14489 can act as a 5-HT1A autoreceptor agonist and inhibit striatal 5-hydroxytryptophan accumulation. S-14489 can be used for the research of neurological disease.
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DC78129 Phenethyl 4-ANPP
Phenethyl 4-ANPP is a MOR (μ-opioid receptor) agonist. Phenethyl 4-ANPP is an analytical reference standard that is structurally similar to known opioids.
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DC78108 JNJ-17166864
JNJ-17166864 is a highly selective CCR2 antagonist. JNJ-17166864 has low oral bioavailability. JNJ-17166864 can significantly reduce the area of alveolar bone loss in a mouse model of periodontitis induced by Porphyromonas gingivalis infection. JNJ-17166864 can be used in the research of inflammatory diseases such as allergic rhinitis and periodontitis.
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DC78089 A-75998
A-75998 is an antagonist of luteinizing hormone-releasing hormone (LHRH). A-75998 can be used in the research of diseases such as hormone-sensitive cancers and endometriosis.
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DC78085 KC-11458
KC-11458 is a motilin agonist. KC-11458 can accelerate gastric emptying.
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DC78080 Dazodeunetant
Dazodeunetant (Example 56) is a nitrogen-containing fused ring derivative. Dazodeunetant is an inhibitor of neurokinin (NK). Dazodeunetant has an IC50 0f 75.99 nM against NK3R in HEK293-NK3 (IP1). Dazodeunetant can be studied in research for menopausal hot flashes.
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DC78073 MKP10241
MKP10241 is an orally active GPR119 agonist. MKP10241 elevates cAMP levels in the GPR119 expressing cell line (EC50: 3.7 nM). MKP10241 reduces blood glucose levels and HbA1c in acute models and a chronic diabetic mouse model. MKP10241 also demonstrates excellent preclinical efficacy in acute as well as chronic rodent models of obesity, and MASH.
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DC78044 GSK1842799
GSK1842799 is an orally active selective S1P1 receptor agonist prodrug. GSK1842799 is promising for research of multiple sclerosis.
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DC78029 RS130-180
RS130-180 is a selective β-arrestin-biased agonist targeting the serotonin 2A receptor (5-HT2aR). RS130-180 is promising for research of neuropsychiatric disorders such as depression.
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DC78011 CH0076989
CH0076989 is a specific CCR3 agonist. CH0076989 activates eosinophils and transfectants expressing both wild-type CCR3 and a CCR1:CCR3 chimaeric receptor lacking the CCR3 amino-terminus. CH0076989 has a direct interaction with the transmembrane helices of CCR3, supported by the complete loss of its activity due to mutations of the residues Y41, Y113 and E287. CH0076989 can be used for the study of inflammation and allergic diseases (such as asthma).
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DC78004 Zilebesiran sodium
Zilebesiran sodium is a siRNA that reduce hepatic angiotensinogen levels through RNA interference. it is used for the study of mild to moderate Hypertension. Angiotensinogen is the predominant precursor of angiotensin peptides and a key regulator of syste
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DC77997 Vasotocin
Vasotocin is the precursor of vasopressin. Vasotocin has functions including innervating the limbic–midbrain changes rapidly over evolutionary time in mediating various affiliative and reproductive behaviours. Vasotocin is important in the modulation of stress-related cognitive processes. Vasotocin administration facilitates the learning of a complex (agonistic) song pattern in the wild sparrow.
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DC77912 Org 6582
Org 6582 is a competitive, selective, and long-acting 5-HT (Ki = 89 nM) uptake inhibitor. Org 6582’s inhibitory effect on 5-HT uptake can last for more than 48 hours. Org 6582 can be used for research on depressive disorders.
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DC47074 Sunobinop Featured
Sunobinop (S 117957) is a modulator of the opioid receptor-like orphan receptor (ORL1).
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DC71349 NF340 Featured
NF340 is a potent and selective P2Y11 receptor antagonist. NF340 inhibits the activity of P2Y11R by completely combining with ATP-binding amino acid residues. NF340 ameliorates inflammation in human fibroblast-like synoviocytes and can be used for rheumatoid arthritis research.
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DC73397 BPRCX807
BPRCX807 (BPRCX-807) is a highly selective and potent CXCR4 antagonist with binding IC50 of 40.4 nM and EC50 of 48.1 nM for cell-mobility activity in the chemotaxis assays, inhibits CXCL12-mediated cell signaling pathway.
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DC73396 BPRCX714
BPRCX714 (BPRCX 714) is a highly selective and potent CXCR4 antagonist with binding IC50 of 34.2 nM, effectively inhibits CXCL12-induced movement of CCRF-CEM cells with EC50 of 13.7 nM.
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DC70677 PAR2 antagonist C391 Featured
PAR2 antagonist C391 (C391) is a selective PAR2 antagonist, potently inhibits peptidomimetic-induced PAR2 Ca2+ signalling with IC50 of 1.3 uM.C391 blocks both PAR2 Ca2+ and MAPK signalling pathways activated by peptidomimetics and/or proteinase activation.C391 effectively attenuated compound 48/80-induced thermal hyperalgesia in vivo.C391 blocked A. alternata-induced, PAR2-dependent Ca2+ and MAPK signalling in 16HBE14o- cells, as well as β-arrestin recruitment in HEK 293 cells.C391 effectively attenuated A. alternata-induced inflammation, mucus production, mucus cell hyperplasia and airway hyperresponsiveness in acute allergen-challenged murine models.
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DC8773 JNJ-7777120 Featured
JNJ-7777120 is a selective H4R antagonist with Ki of 4 ±1 nM, exhibits >1000-fold selectivity over the other histamin receptors.
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DC5015 Rotigotine Hydrochloride Featured
Rotigotine is dopamine D2 and D3 receptor agonist. Ki values are 13 and 0.71 nM for D2 and D3 respectively. Rotigotine also has significant affinity for 5-HT1A and adrenergic α2B receptors. Rotigotine exhibits antiparkinsonian acitivity.
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DC28252 Seltorexant hydrochloride Featured
Seltorexant hydrochloride (JNJ-42847922 hydrochloride) is an orally active, high-affinity, and selective OX2R antagonist (pKi values of 8.0 and 8.1 for human and rat OX2R). Seltorexant hydrochloride crosses the blood-brain barrier and quickly occupies OX2R binding sites in the rat brain.
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DC40582 Montelukast Featured
Montelukast is a potent, selective and orally active antagonist of cysteinyl leukotriene receptor 1 (CysLT1). Montelukast can be used for the reseach of asthma and liver injury. Montelukast also has an antioxidant effect in intestinal ischemia-reperfusion injury, and could reduce cardiac damage.
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DCAPI1015 Zafirlukast(Accolate) Featured
Zafirlukast(Accolate)
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DC73393 alpha-NETA Featured
alpha-NETA (α-NETA) is a small molecule antagonist of chemerin receptor chemokine-like receptor 1 (CMKLR1), inhibits chemerin-stimulated β-arrestin2 association with CMKLR1 with IC50 of 4.9 uM.
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DC70577 LY3502970 (Orforglipron) Featured
LY-3502970 (Orforglipron) is a potent, selective, orally active non-peptide agonist of glucagon-like peptide-1 (GLP-1) receptor.LY3502970 is a partial agonist, biased toward G protein activation over β-arrestin recruitment at the GLP-1R.
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