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GPCR

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Cat. No. Product Name Field of Application Chemical Structure
DC10391 EBI2 inhibitor GS682753A GSK682753A is a selective and highly potent inverse agonist of the epstein-barr virus-induced receptor 2 (EBI2) with an IC50 of 53.6 nM.
DC10233 Guanfacine Hydrochloride Guanfacine Hydrochloride is a selective α2A-adrenoceptor agonist with anti-hypertensive effect.
DC9819 Guanoclor Featured Guanoclor is a sympatholytic drug. It is known to bind to non-adrenergic sites in pig kidney membranes.
DC9458 GW-1100 GW 1100 is a selective antagonist of GPR40-mediated Ca2+ elevations in HEK293 cells stimulated by GW 9508 (an agonist of both GPR40 and GPR120, another GPCR activated by long chain fatty acids) or linoleic acid with a pIC50 value equal to 5.99.
DC8266 GW-627368X Featured GW 627368X is a selective prostanoid EP4 receptor competitive antagonist with additional affinity at TP receptors (pKi values are 7.0 and 6.8 in competition radioligand bioassays).
DC12266 H4 Receptor antagonist 1 H4 Receptor antagonist 1 is a potent and selective histamine H4 receptor inverse agonist, with an IC50 of 19 nM.
DC10935 HAMI3379 HAMI3379 (HAMI-3379) is a potent and selective antagonist of cysteinyl leukotriene 2 (CysLT(2)) receptor, inhibits LTD4- and LTC4-induced intracellular calcium mobilization withIC50 of 3.8 nM and 4.4 nM respectively.
DC12493 HT-2157(SNAP37889) Featured HT-2157 (SNAP 37889) is a selective, high-affinity, competitive antagonists of galanin-3 receptor (Gal3).
DC11328 Hydroxyzine Hydroxyzine is a histamine H1 receptor antagonist (Ki = 1.9 nM).
DC7020 Ibutamoren mesylate Featured Ibutamoren mesylate (MK-0677) is an orally active nonpeptide growth hormone (GH) secretagogue.
DC3115 ICI-118551 Featured ICI-118,551 is a selective beta-2 (β2) adrenergic receptor antagonist.ICI binds to the β2 subtype with at least 100 times greater affinity than β1 or β3, the two other known subtypes of the beta adrenoceptor.
DCAPI1055 Iloperidone (Fanapt) Iloperidone (Fanapt)
DC9389 INCB3344 INCB3344 is a novel, potent and selective small molecule antagonist of the mouse CCR2 receptor; inhibits the binding of CCL2 to mouse monocytes with nanomolar potency (IC50 = 10 nM).
DC7429 INCB 8761 Featured INCB8761(PF-4136309) is a potent, Selective, and orally bioavailable CCR2 antagonist.
DCAPI1701 Indacaterol Maleate Indacaterol is an ultra-long-acting β-adrenoceptor agonist with pKi of 7.36.
DC8914 Indacaterol Featured Indacaterol is a potent, orally administered ultra-long-acting β2 adrenergic receptor (ADRB2) agonist, widely recognized for its therapeutic potential in respiratory and cardiovascular conditions. By selectively activating ADRB2, indacaterol not only enhances bronchodilation but also exhibits a unique mechanism of action by inhibiting NF-κB activity in a β-arrestin2-dependent manner. This dual functionality helps mitigate lung inflammation, prevent further pulmonary damage, and improve lung function in patients with chronic obstructive pulmonary disease (COPD). Beyond its respiratory applications, indacaterol has also emerged as a valuable tool in cardiovascular disease research, offering insights into its broader therapeutic effects. Its multifaceted pharmacological profile positions indacaterol as a promising candidate for addressing complex disease mechanisms and advancing treatment strategies in both respiratory and cardiovascular fields.
DC7197 ML 161 Featured Inhibitor of protease-activated receptor 1 (PAR1)-mediated platelet activation (IC50 = 0.26 μM for the inhibition of platelet P-selectin expression on human platelets). Thought to act allosterically. Also inhibits thrombin-induced platelet activation.
DC8996 Isoprenaline HCl Isoprenaline Hydrochloride is a non-selective beta-adrenergic agonist and structurally similar to adrenaline.
DCAPI1080 Istradefylline (KW-6002) Featured Istradefylline(KW6002) is a very potent, selective and orally active adenosine A2A receptor antagonist(Ki=2.2 nM) in experimental models of Parkinson's disease.
DC8304 Isoxazole 9(ISX9) Featured ISX-9 is a small molecule inducer of adult neural stem cell differentiation both in vitro and in vivo.
DC10283 IT1t dihydrochloride Featured IT1t dihydrochloride is a potent CXCR4 antagonist; inhibits CXCL12/CXCR4 interaction with an IC50 of 2.1 nM.
DC10306 IT1t IT1t is a potent CXCR4 antagonist; inhibits CXCL12/CXCR4 interaction with an IC50 of 2.1 nM.
DC10095 JD5037 Featured JD5037 is an inverse agonist of peripheral cannabinoid 1 (CB1) receptors (Ki = 0.35 nM).
DC9524 JDTic (dihydrochloride) JDTic 2Hcl is a highly selective antagonist for the κ-opioid receptor; without affecting the μ- or δ-opioid receptors.
DC10971 JMS-17-2 Featured JMS-17-2 is a potent and selective antagonist of CX3CR1 with IC50 of 0.32 nM, displays significant selectivity for CX3CR1 over other chemokine receptors such CXCR2, CXCR1, and CXCR4 (IC50>1 uM).
DC7843 JNJ 42153605 Featured JNJ 42153605 is a positive allosteric modulator of the metabotropic glutamate 2 receptor.
DC12374 JNJ-10229570 Featured JNJ-10229570 (JNJ10229570) is a novel potent, selective melanocortin receptor MC1R and MC5R antagonist with binding IC50 of 270 nM and 200 nM, respectively.
DC8140 JNJ31020028 Featured JNJ-31020028 is a selective brain penetrant antagonist of neuropeptide Y2 receptor with high affinity(pIC50=8.07, human; pIC50=8.22 rat); >100-fold selective versus human Y1/Y4/Y5 receptors.
DC12166 JNJ-5207852 Featured JNJ-5207852 is a selective and potent histamine H3 receptor (H3R) antagonist, with pKis of 8.9, 9.24 for rat and human H3R, respectively.
DC9271 JNJ-63533054 Featured JNJ-63533054 is a potent and selective agonist of hGPR139 with an EC50 = 16 nM.

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