calcium channel antagonist 2

Calcium Channel antagonist 2 is a calcium channel antagonist (IC50=5-20 μM) that can be used to study diseases due to Ca2+ channels like pain and diabetes.

Calcium 2-hydroxy-4-(methylthio)butanoate (Calcium 2-hydroxy-4-(calcium hydroxymethionine)) is a solid, water-soluble, weakly acidic nutrition enhancer (based on its pKa). This compound, also known as 2-Hydroxy-4-(methylthio)butanoic acid, has been primarily detected in urine and is mainly located in the cytoplasm and adiposome of cells.

A2B receptor antagonist 2 hydrochloride is an antagonist of adenosine receptor A2B (Ki = 2.30 μM for rA1, 6.8 μM for rA2A, 3.44 μM for hA2B).

Calcium channel-modulator-1, a calcium channel-modulator (IC50: 0.8 μM), specializes in blocking aortic constriction.

AMPA receptor antagonist-2 is an AMPA receptor antagonist.

TLR7 8 9 antagonist 2 is an orally active and highly bioavailable vTLR7 8 9 antagonist. It inhibits HEK hTLR7, HEK hTLR8, and HEK hTLR9 with IC50s of 0.011 μM, 0.029 μM, and 0.052 μM, respectively. TLR7 8 9 antagonist 2 can be used to study auto-inflammatory diseases such as systemic lupus erythematosus or lupus nephritis.

CRTh2 antagonist 2 is a selective and potent CRTH2 antagonist, IC50≤10 nM. CRTh2 antagonist 2 can be used to study the direction of androgenic alopecia.

2-Hydroxy atorvastatin calcium salt is a hydroxy metabolite of atorvastatin calcium salt, a potent HMG-CoA reductase inhibitor (IC50 = 8 nM).

Sigma-1 receptor antagonist 2 is a more potent and selective antagonist of the sigma-1 receptor (σ1 R, Ki = 3.88 nM) compared to the sigma-2 receptor (Ki = 1288 nM).

AHR antagonist 2 is an antagonist of the aryl hydrocarbon receptor. The IC50s for human AHR and mouse AHR are 0.885 and 2.03 nM, respectively.

Bcl-xL antagonist 2 is an effective and selective antagonist of Bcl-xL with an IC50 of 91 nM and a Ki of 65 nM. Bcl-xL antagonist 2 induces apoptosis in cancer cells and can be used in studies about chronic lymphocytic leukemia and non-Hodgkin’s lymphoma.

CB1 antagonist 2 (AM4113) is caimabinoid 1 (CB1) antagonist which inhibits CB1 in vivo with an IC50 of 25.5 nM.

MCHR1 antagonist 2 is an inhibitor of melanin-concentrating hormone receptor 1 (MCH1-R, IC50 = 65 nM) and also inhibits hERG.

GPVI antagonist 2 (Compound 1) is a potential Glycoprotein VI (GPVI) antagonist, showing activity against collagen (IC50: 0.35 μM), CRP (IC50: 0.80 μM), convulxin (IC50: 195.2 μM), and thrombin (IC50: 81.38 μM), and is a promising anti-platelet agent.

Calcium Channel antagonist 3 is a voltage-gated calcium channel inhibitor (IC50 : 5-20 μM).

ET Receptor Antagonist 2 (Compound 16j) is an orally active ET receptor antagonist with an IC50 of 0.22 nM, suitable for pulmonary arterial hypertension (PAH) research. It has been shown to mitigate monocrotaline-induced PAH in a rat model [1].

5-HT3 antagonist 2 is an antagonist of 5-HT3 receptor.

NOD1/2 Antagonist-1 is a potent dual inhibitor of nucleotide-binding oligomerization domain-like receptors 1 and 2 (NOD1/2), displaying inhibitory concentrations (IC50) of 1.13 μM for NOD1 and 0.77 μM for NOD2. It exhibits an acceptable half-life (T1/2) of 67.6 minutes. Additionally, NOD1/2 Antagonist-1 enhances the antitumor efficiency of Paclitaxel (PTX).

KCa1.1 channel activator-2, a hybrid derivative of Quercetin, selectively stimulates the vascular KCa1.1 channels. This compound demonstrates significant myorelaxant activity.

Protease-Activated Receptor-1 Antagonist 2 is an orally active antagonist of protease-activated receptor-1 (PAR-1), demonstrating significant potency with an IC 50 of 7 nM. It exhibits favorable pharmacokinetic characteristics, making it valuable in cardiovascular disease (CVD) research, including studies on atherosclerosis and restenosis [1].

T-Type calcium channel inhibitor 2 (compound 6g) is a potent inhibitor of the T-type calcium channel, specifically acting on Cav3.1 (α1G) with an IC50 of 31.0 μM, Cav3.2 (α1H) with an IC50 of 83.1 μM, and Cav3.3 (α1I) (α1H). T-Type calcium channel inhibitor 2 exhibited cytotoxicity against A549 and HCT-116 cells with IC50s of 5.0 μM and 6.4 μM, respectively.

AT1R antagonist 2 is a potent AT1R selective ligand with good AT1R affinity (Ki: 26 nM).

N-type calcium channel blocker-1 is an orally active analgesic agent with a high affinity for functionally blocking N-type calcium channels.

NMDA receptor antagonist 2 is a highly potent and orally active NR2B subtype-selective antagonist of the N-methyl-D-aspartate (NMDA) receptor, with an IC50 of 1.0 nM and a Ki value of 0.88 nM. This compound is valuable in scientific investigations of neuropathic pain and Parkinson’s disease.

CXCR2 antagonist 2 is a potent CXCR2 antagonist for cancer immunotherapy, exhibiting an IC50 value of 95 nM.

The compound is an A1 A3 adenosine receptor antagonist that aids in the treatment of (neurological) inflammatory diseases.

GRPR antagonist-2 is a potent antagonist of the gastrin-releasing peptide receptor (GRPR) and exhibits anticancer effects with cytotoxicity to HGC-27 cells (IC50: 0.77 μM) and Pan02 cells (IC50: 2.5 μM).

Compound A-26, also known as FXR antagonist 2, is a diarylamide derivative that functions as a moderate FXR antagonist. It is utilized in researching hyperlipidemia and type 2 diabetes [1].

EP2 receptor antagonist-2 (CID891729) is a compound that blocks EP2 receptor activation by PGE2 and reduces lactate dehydrogenase (LDH) release induced by N-methyl-D-aspartate (NMDA).

5-HT2A antagonist 2 is an orally active, selective 5HT2A antagonist with an IC50 of 14 nM. It exhibits good chemical, hepatocyte, and plasma stability, without significant cytotoxicity in cell lines VERO, HFL-1, L929, NIH3T3, CHO-K1 [1].

Compound 43, also known as β-AR antagonist 2, is an antagonist of β-AR with an IC50 of 0.17 μM. It inhibits the growth of mouse A549 xenograft tumors and demonstrates cardioprotective efficacy against DOX-induced heart failure in C57 mice [1].

A2B receptor antagonist 2 is an antagonist of adenosine receptor A2B (Ki = 2.30 μM for rA1, 6.8 μM for rA2A, 3.44 μM for hA2B).

AR antagonist 2 (compound 58) is a potent inhibitor of the androgen receptor (AR) with an IC50 of 0.95 μM.

GPR84 Antagonist 2, a potent and selective GPR84 antagonist (IC 50 = 8.95 nM), demonstrates oral activity and significantly enhances potency in calcium mobilization assays. It effectively inhibits neutrophil and macrophage chemotaxis following GPR84 activation, highlighting its research potential for ulcerative colitis.

Sodium Channel Inhibitor 2 [Sodium Channel inhibitor 2] is a blocker of sodium channels.

LXR antagonist 2 (compound 10rr) is a potent LXR (liver X receptor) inverse agonist, targeting LXRβ (IC50: 0.36 μM) and LXRα (IC50: 2.25 μM). It serves as an adipogenesis inhibitor, downregulating LXR target genes SREBP-1c, ACC, FAS, and SCD-1, and demonstrates hypolipidemic activity in Triton WR-1339-induced hyperlipidemic mice.

Dopamine D3 receptor antagonist-2 is a dopamine D3 receptor-selective compound (Ki=2.16 nM) that exhibits potential therapeutic effects in CNS disorders.

Estrogen receptor antagonist 2 is a selective down-regulator of the estrogen receptor, with research potential for breast cancer disease. Estrogen (E2) and estrogen alpha receptor (ERα) are important drivers of breast cancer development.

LPA2 antagonist 2 is a selective and potent LPA2 antagonist (IC50: 28.3 nM) with potential anticancer activity, inhibits LPA3, and can be used in the study of cancer.

Compound 4h, also known as 5-HT7R antagonist 2, is a selective inhibitor of the 5-HT7R that disrupts both G protein and β-arrestin signaling pathways. It exhibits a K_i value of 67 nM, with IC_50 values of 2.59 μM in cAMP assays and 39.57 μM in Tango tests. This antagonist is noted for its potential to mitigate repetitive behaviors associated with autism spectrum disorder (ASD) and to foster the restoration of neurogenesis impaired by ASD [1]. Pharmacokinetic analysis in ICR male mice following intravenous and intraperitoneal administration shows a T_max of 0.08 hours and 0.25 hours, a T_1 2 of 0.77 hours and 1.06 hours, and a C_max of 33.07 ng mL and 156.44 ng mL, respectively. The AUC_last was recorded at 28.31 ng·h mL and 143.27 ng·h mL, with a clearance rate (CL) of 41.61 L h kg for intravenous administration. The volume of distribution at steady state (V_ss) was 32.43 L kg, the mean residence time (MRT) was 0.79 hours and 0.93 hours, and the bioavailability (F) was calculated at 50.60% [1].

GPR183 antagonist-2 (compound 32), a selective antagonist of GPR183, exhibits excellent water solubility and pharmacokinetic properties. This compound effectively diminishes paw and joint swelling, and reduces gene expression of pro-inflammatory cytokines (MCP-1, MMPs, and VEGF) in a dose-dependent manner within a collagen-induced arthritis (CIA) mouse model. GPR183 antagonist-2 is applicable in researching autoimmune diseases [1].

LTB4 antagonist 2, a carboxamide-acid compound, serves as an antagonist to leukotriene B4 (LTB4) with potential anti-inflammatory properties, exhibiting high affinity for the LTB4 receptor and an inhibitory concentration (IC50) of 439 nM [1].

Compound 25b, an FPR1 antagonist, exhibits potent inhibition of the formyl peptide receptor 1 with an IC50 of 70 nM. It concurrently hampers cell proliferation and triggers apoptosis, diminishing cell growth and migration, yet paradoxically augments angiogenesis [1].

H4R Antagonist 2, a potent Furo[3,2-d]pyrimidine derivative, serves as a histamine H4 receptor antagonist and holds potential for research into rheumatoid arthritis [1] (page 68).

Compound 39, also known as CB2 receptor antagonist 2, is a potent CB2 antagonist exhibiting an IC50 of 0.33 μM. It engages in strong interactions with residues L17, W6.48, V6.51, and C7.42 [1].

A2A receptor antagonist 2 is a highly selective and potent antagonist of the adenosine A2Areceptor (IC50: 8.3 nM).

NRP1 antagonist 2 (Compound 1) acts as an NRP1 antagonist.

GCGR Antagonist 2, a Furan-2-carbohydrazide, serves as an orally active antagonist of the glucagon receptor. It exhibits affinity for the human glucagon receptor (hGluR) with a dissociation constant (Kd) of 2.3 nM and demonstrates inhibitory activity against the rat receptor with a half-maximal inhibitory concentration (IC50) of 0.43 nM. Additionally, this compound effectively prevents glucagon-stimulated glycogenolysis.