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GPCR

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Cat. No. Product Name Field of Application Chemical Structure
DC10583 RO 5028442 Featured
RO5028442 is a highly potent and selective Brain-Penetrant Vasopressin 1a (V1a) receptor antagonist with Kis of 1 nM (hV1a) and 39 nM (mV1a).
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DC11271 S38093 HCl Featured
S 38093 is a novel brain-penetrant antagonist/inverse agonist of H3 receptors.
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DC7274 S1RA Featured
S1RA(E-52862) is a potent and selective sigma-1 receptor(σ1R, Ki=17 nM), showed good selectivity against σ2R (Ki > 1000 nM).
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DC8436 Salmeterol Xinafoate Featured
Salmeterol Xinafoate is a long-acting β2-adrenergic receptor agonist with anti-inflammatory effects, used in the treatment of asthma symptoms and chronic obstructive pulmonary disease (COPD) symptoms.
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DC8610 Salmeterol Featured
Salmeterol Xinafoate is a long-acting β2-adrenergic receptor agonist with anti-inflammatory effects, used in the treatment of asthma symptoms and chronic obstructive pulmonary disease (COPD) symptoms.
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DC7913 SB225002 Featured
SB225002 is a potent, and selective CXCR2 antagonist with IC50 of 22 nM for inhibiting interleukin IL-8 binding to CXCR2, > 150-fold selectivity over the other 7-TMRs tested.
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DC8483 SB-399885 HCl Featured
Potent, brain penetrant, orally active 5-HT6 antagonist. Displays > 200-fold selectivity for 5-HT6 over other 5-HT receptors (pKi values are 9.11, 8.81 and 9.02 for human recombinant, native rat and native human 5-HT6 receptors respectively).
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DC41887 Cortagine Featured
Cortagine is a specific corticotropin-releasing factor receptor subtype 1 (CRF1) agonist with an IC50 of 2.6 nM for rCRF1. Cortagine is an anxiolytic and antidepressive drug in the mouse model.
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DC8624 Setipiprant(ACT129968) Featured
Setipiprant is an orally available, selective CRTH2 antagonist. CRTH2 is a G protein-coupled receptor for PGD2.
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DC12379 SKF 38393 Featured
SKF 38393 is a partial agonist of the dopamine D1-like receptors D1 and D5 (Kis = 1 and ~0.5 nM, respectively).
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DC7295 SphK-I2 Featured
SKI II is a highly selective and non ATP-competitive S1P receptor inhibitor with IC50 of 0.5 μM, while exhibits no inhibitory on other kinases including PI3K, PKCα and ERK2.
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DC11208 TAK-071 Featured
TAK-071 is a novel, potent and highly selective muscarinic acetylcholine receptor 1 (M1R) positive allosteric modulator. EC50 of TAK-071 M1R agonist activities is 520 nM.
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DC7932 TBPB Featured
TBPB is an allosteric M1 mAChR agonist(EC50=289 nM) that regulates amyloid processing and produces antipsychotic-like activity in rats.
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DC11461 TCS-OX2-29 Featured
TCS-OX2-29 is a potent and selective OX2 receptor antagonist with IC50 of 40 nM. Displays >250-fold selectivity for OX2 over OX1.
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DC8813 TD-4208 Featured
TD-4208 is a potent and selective inhaled muscarinic antagonist with functional lung selectivity and long duration of action in preclinical models of bronchoconstriction.
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DC9609 Terutroban Featured
Terutroban is a thromboxane/prostaglandin endoperoxide receptor antagonist.
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DC8054 Cariprazine (RGH-188) Featured
Cariprazine (RGH-188) is a novel putative antipsychotic drug that exerts partial agonism at dopamine D2/D3 receptors, with preferential binding to D3 receptors, and partial agonism at serotonin 5-HT1A receptors.
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DC8153 Umeclidinium bromide Featured
Umeclidinium bromide(GSK573719A) is a muscarinic receptor antagonist which is useful in treatment of chronic obstructive pulmonary disease (COPD).
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DC8613 Vortioxetine (Lu AA21004) Featured
Vortioxetine (Lu AA21004) is a multimodal serotonergic agent, inhibits 5-HT1A, 5-HT1B, 5-HT3A, 5-HT7 receptor and SERT with IC50 of 15 nM, 33 nM, 3.7 nM, 19 nM and 1.6 nM, respectively.
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DC8288 Vortioxetine hydrobromide Featured
Vortioxetine Hcl (Lu AA21004 Hcl) is a multimodal serotonergic agent, inhibits 5-HT1A, 5-HT1B, 5-HT3A, 5-HT7 receptor and SERT with IC50 of 15 nM, 33 nM, 3.7 nM, 19 nM and 1.6 nM, respectively.
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DC10717 VU6005649 Featured
VU6005649 is a dual mGlu7/8 positive allosteric modulator with EC50s of 649 nM and 2.6 μM for mGlu7 and mGlu8, respectively.
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DC10136 VUF10460 Featured
VUF10460 is a non-imidazole histamine H4 receptor agonist; binds to rat H4 receptor with a pKi of 7.46.
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DC8851 VUF11207 Featured
VUF11207 is a highly potent CXCR7 agonist. VUF11207 induces recruitment of β-arrestin2 to the CXCR7 followed by internalization of the receptor.
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DC9932 YL-0919 Featured
YL-0919 is a novel synthetic compound with combined high affinity and selectivity for serotonin transporter and 5-HT1A receptors.
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DC9435 Zibotentan(ZD4054) Featured
Zibotentan (ZD4054) is an orally administered, potent and specific ETA-receptor (endothelin A receptor) antagonist (IC50 = 21 nM).
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DC9637 Desmopressin (Acetate) Featured
Desmopressin(DDAVP) acetate is the synthetic analogue of the antidiuretic hormone arginine vasopressin.
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DC10423 Motixafortide(BKT140) Featured
Motixafortide (BKT140 4-fluorobenzoyl) is a novel CXCR4 antagonist with an IC50 vakue of ~1 nM.
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DC9552 Oxytocin (acetate) Featured
Oxytocin (α-Hypophamine) acetate is a mammalian neurohypophysial hormone; its actions are mediated by specific, high-affinity oxytocin receptors; ligand of oxytocin receptor.
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DC1076 Otenabant(CP945598.HCl) Featured
CP-945598 HCl is a potent and selective cannabinoid type 1 receptor antagonist with Ki of 0.7 nM.
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DC70940 ZY12201
ZY12201 is a potent, selective, orally bioavailable TGR5 agonist with hTGR5 EC50 of 57 pM and mTGR EC50 of 62 pM.ZY12201 displays a favorable pharmacokinetic properties and demonstrated in-vivo glucose lowering effects in animal models (ED50 of 7.9 mg/kg and ED90 of 29.2 mg/kg).
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