gpr-40 agonist 2

GPR40 Agonist 2 is a compound that functions as a GPR40 agonist and is utilized in diabetes research.

Dopamine D2 receptor agonist-2 (Dopamine D2 Receptor) is a ligand targeting the dopamine D2 receptor.

TREM2 agonist-2 (I-192) is an orally active and potent agonist of myeloid triggered receptor 2 (TREM2) for neurodegenerative disease research.

β2AR/M-receptor agonist-2 is a dual-function compound acting as a muscarinic antagonist and β2 adrenoceptor agonist (MABA). It demonstrates significant activity towards the β2 adrenoceptor with an EC50 of 3.7 nM and exhibits affinity for the human cloned M3 receptor with a Ki of 0.73 nM. This potent bronchodilator holds potential for research in chronic obstructive pulmonary disease (COPD) treatment.

S1R agonist 2 is a selective S1R agonist with a Ki of 88 nM for S2R and 1.1 nM for S1R and is protective against ROS and NMDA-induced neurotoxicity.

GPR35 agonist 2 (TC-G 1001) is a potent GPR35 agonist.The EC50 values of GPR35 agonist 2 in the β-arrestin and Ca2+ release assays were 26 and 3.2 nM, respectively.

HIF-2α agonist 2 is an HIF-2α agonist with an EC50 value of 1.68 μM for HIF-2α. HIF-2α agonist 2 can promote the stability of the ARNT A B ring in the 3z structure of HIF-2a-ARNT complex without cytotoxicity to 786-o-Reha-Luc cells. HIF-2α agonist 2 can be used in the study of oxygen metabolism and is closely related to the occurrence of cancer.

CB2 receptor agonist 2 (ZINC72105556) is a potent and selective agonist for the CB2 (cannabinoid type 2) receptor, Ki = 8.5 nM. CB2 receptor agonist 2 has high affinity and selectivity for CB2.

TLR7 agonist 2 (TLR7-IN-1) is a specific and effective Toll-like Receptor 7 (TLR7) agonist (LEC=0.4 μM).

GPR120 Agonist 2 is a potent and selective GPR120 receptor agonist.

Orexin 2 Receptor Agonist (OX2R) is an effective (EC50: 23 nM) and OX2R-selective (OX1R/OX2R EC50 ratio: 70) agonist.

GPCR agonist-2 (4-(Cyclopropylamino)-3-nitrobenzoic acid) is an agonist of the orphan human GPCR GPR109B.

GPR81 agonist 2 is a potent agonist targeting the GPR81 receptor, demonstrating EC50 values of 0.023 µM for hGPR81 and 0.123 µM for hGPR109A, respectively.

Glucocorticoid receptor agonist-2 (compound 21), a glucocorticoid receptor agonist with an IC50 value of 6.6 nM, serves as an active reference for ABBV-3373 [1] and is instrumental in the synthesis of anti-inflammatory ADC molecules.

ERRγ agonist-2 is a potent and selective ERRγ inverse agonist with a Kd value of 6.5 μM, inhibiting the expression of hepcidin, fibrinogen, and gluconeogenic genes. ERRγ agonist-2 exhibits antimicrobial, anti-coagulant, and antidiabetic activities [1].

CB1/2 agonist 4 (compound 24) is a CB1 full agonist (EC50: 15.09 nM) and a CB2 partial agonist (EC50: 1.16 nM). CB1/2 agonist 4 has significant anti-harm-sensing activity and also activates cannabinoid and TRPV1 receptors (IC50: 0.8 μM, EC50: 0.12 μM). , EC50: 0.12 μM).

FPR2 agonist 2 is a potent FPR2 agonist with blood-brain barrier permeability that acts on h-FPR2 (EC50: 0.13 nM), inhibiting the production of pro-inflammatory cytokines, counteracting changes in mitochondrial function, and inhibiting caspase-3 activity.

Compound 28.1, also known as TAS2R14 agonist-2, is a potent and selective inhibitor of TAS2R14, exhibiting an EC50 of 72 nM [1].

Compound 40 is a selective M1/M4 muscarinic antagonist with an IC50 of 19 nM for M1 receptors and 42 nM for M4 receptors [1].

GPR139 agonist-2 (compound 20a), a potent GPR139 agonist with an EC50 of 24.7 nM, has demonstrated efficacy in rescuing social interaction deficits and alleviating cognitive deficits in murine schizophrenia models, indicating its potential in antischizophrenia drug research [1].

Cisd2 agonist 2 (compound 6), with an EC50 of 191 nM, is an orally active activator of Cisd2, a protein whose levels are associated with nonalcoholic fatty liver disease (NAFLD). In vivo studies have demonstrated that Cisd2 agonist 2 exhibits no significant toxicity in heterozygous hepatocyte-specific Cisd2 knockout (Cisd2hKO-het) mice [1].

Orexin 2 Receptor Agonist 2 (ORA-2) is a specific agonist for the orexin 2 receptor.

TRβ agonist 2 (Compound 1) is a highly potent TRβ agonist that effectively reduces lipid accumulation in HepG2 cells and promotes lipolysis, offering comparable effects. With its promising attributes, TRβ agonist 2 emerges as a potential thyromimetic selectively targeting TRβ [1].

SARS-CoV-2-IN-40 (Compound 19) is a SARS-CoV-2 inhibitor that effectively suppresses the infection of Calu3 lung cells by the BA.1 and BA.5 variants, exhibiting half-maximal inhibitory concentrations (IC50s) of 100 nM and 160 nM, respectively [1].

GPR119 agonist 2 (compound 43), an orally active agonist of GPR119, exhibits favorable pharmacokinetic properties in rodents and has demonstrated efficacy in enhancing glucose tolerance in both mice and rats, indicating its potential in type 2 diabetes research [1].

PPARγ agonist 2 is a highly effective compound that acts as a partial agonist for PPARγ. It exhibits significant potential for utilization in metabolic disease research [1].

5-HT2A receptor agonist-2 is a potent compound that acts as an agonist on the serotonin 5-HT2 receptor, specifically stimulating the 5-HT 2A, 5-HT 2B, and 5-HT 2C receptors with EC50 values of 1.7 nM, 0.58 nM, and 0.50 nM, respectively [1].

Glucocorticoid receptor agonist 2 is a highly effective anti-inflammatory compound, derived from arylpyrazole, that actively binds to and activates the glucocorticoid receptor. This compound exhibits potent anti-inflammatory properties without disrupting insulin secretion.

CBR Agonist-2 is a CB1 agonist (CB1R; CB1 ligand) with an EC50 of 960 nM and Ki of 970 nM, making it a promising tool for studying diseases related to the endogenous cannabinoid system involving hCB1R.

Pparδ agonist 2 is an agonist of PPARδ.

Y4R Agonist-2 is a potent agonist of the Y4 receptor, exhibiting a K_i value of 0.033 nM.

Adenylyl cyclase type 2 agonist-1 is a potent adenylyl cyclase type 2 (AC2) agonist (EC50: 90 nM), and it is a potential lead compound in the fight against respiratory diseases.

AhR agonist 2 (Compound 12a) is a highly potent agonist of the aryl hydrocarbon receptor (AhR) with an EC50 of 0.03 nM, rapidly inducing nuclear AhR enrichment and initiating transcription of downstream genes to promote skin barrier repair. AhR agonist 2 shows promising potential for psoriasis research [1].

Compound 5, a selective GPR109a agonist, exhibits a pEC50 value of 5.53 [1].

EP4 receptor agonist 2 (compound 31) is a potent EP4 receptor agonist, demonstrating an EC50 value of 0.8 nM and K_i values of >100,000, 38,000, and 3.1 nM for the EP2, EP3, and EP4 receptors, respectively [1].

RXFP3 4 agonist 2 is a potent, non-peptidic bis-RXFP3 4 agonist that facilitates the interaction between RXFP3 and β-arrestin-2 and is useful for studying diseases caused by metabolic abnormalities.

CB1 Inverse Agonist 2, an orally active compound, serves as an inverse agonist for the Cannabinoid Receptor CB1. It effectively counteracts the hypothermia and anorexia induced by CP55940 in mouse models.

TGR5 agonist 2 (compound 19) serves as a highly potent TGR5 agonist, with an EC50 value of 0.27 µM [1].

S1P receptor agonist 2 (compound 1) is a selective agonist of the S1P5 receptor, exhibiting higher selectivity than for S1P1 and or S1P3 receptors. It is useful in the endogenous SIP signaling system and for mitigating or preventing central nervous system (CNS) diseases, including neurodegenerative diseases.

Compound 8, identified as a selective alpha4beta2 (α4β2) neuronal acetylcholine receptor (nAChR) agonist, demonstrates a dissociation constant (Kd) of 26 nM, indicating high affinity for this receptor subtype.

BMP agonist 2 has up-regulated bone morphogenetic protein BMP-2 expression activity in vivo and anti-osteoporosis effects, and also has ameliorated the symptoms of osteoporosis in SAMP6 mice.BMP agonist 2 is an osteoinductive cytokine that promotes the production of bone tissue, and can be used in the study of senile osteoporosis (SOP).

5-HT7 agonist 2 is a highly potent 5-HT7 receptor agonist with an IC50 value of 28.7 nM, and it holds promise for studying and understanding various Central Nervous System (CNS) disorders [1].

Ghrelin receptor full agonist-2 is a highly potent Ghrelin receptor full agonist.

S1PR1 agonist 2 is a potent activator of S1PR1 with potential applications in autoimmune disease research.

CB1 2 agonist 2 (compound 23) is a potent non-selective cannabinoid ligand with Ki values of 3.5 nM and 1.2 nM, respectively. It acts as a full agonist of CB1 and a competitive inverse agonist of CB2. BACE-IN-1 shares these properties, being a complete agonist of CB1 and a competitive inverse agonist of CB2.

μ opioid receptor agonist 2 (Compound H-3) is a MOR receptor agonist used for research on pain and pain-related diseases.

Compound 8b hydrochloride, a selective S1R agonist, exhibits affinity with K i s of 1.1 nM for S1R and 88 nM for S2R. It demonstrates neuroprotective effects against ROS and NMDA-induced neurotoxicity [1].

VDR agonist 2 (compound 16i), a vitamin D receptor (VDR) agonist, effectively inhibits TGF-β1-induced hepatic stellate cell (HSC) activation, demonstrating notable anti-hepatic fibrosis efficacy both in vitro and in vivo [1].

LXRβ agonist-2 is a highly potent and β-selective liver X receptor (LXRβ) agonist with an EC50 of 7 nM.