ca2+ channel antagonist

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).

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.

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.

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).

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.

GPR34 receptor antagonist 2 (Tyrosine, N-[(2E)-3-(4'-chloro[1,1'-biphenyl]-4-yl)-1-oxo-2-propen-1-yl]-O-(phenylmethyl)-) is an anti-inflammatory agent.

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.

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).

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.

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].

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).

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

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).

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].

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].

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).

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

Y2-Antagonist-2 is a novel, selective, soluble non-peptidic NPY Y2 receptor antagonist with enhanced CNS exposure.

Mu opioid receptor antagonist 2 (compound 25) is a potent and selective mu opioid receptor (MOR) antagonist that permeates the blood-brain barrier (Ki: 0.37 nM, EC50: 0.44 nM), and can be used to study opioid use disorder (OUD).

CCR8 antagonist 2 is a potent inhibitor of CCR8 (C-C Motif chemokine receptor 8), predominantly expressed on Treg and Th2 cells, and not on Th1 cells. CCR8 antagonist 2 can be used for the treatment of CCR8-mediated diseases (e.g., cancer and or neuropathic pain).

ERRα antagonist-2 (Compound 11) is a potential reverse agonist of ERRα (estrogen receptor-related receptor α) with an IC50 of 0.80 μM. It can inhibit the migration and invasion of ER-negative MDA-MB-231 cells and inhibits the growth of breast cancer in vivo.

Compound 121, a D3R/MOR antagonist with K i values of 361 nM and 85.2 nM for D3R and MOR respectively, has the potential for analgesic effects through MOR partial agonism and may reduce opioid-misuse liability through D3R antagonism [1].

SSTR5 antagonist 2 is a highly potent, oral active and selective antagonist of somatostatin (receptor) subtype 5 (SSTR5),with potential to treat type 2 diabetes mellitus (T2DM).

GnRH antagonist 2 (formula I) is a potent GnRH receptor antagonist with valuable applications in endometriosis research [1].

A1AR antagonist 2 (compound 18h) is a potent antagonist of the A1 adenosine receptor (AR) with Ki values of 1.49, 10.2, and 50.1 nM for hA1, hA2A, and hA2B, respectively [1].

SSTR5 antagonist 2 hydrochloride is a potent, orally active, selective antagonist of the growth hormone inhibitory hormone (receptor) subtype 5 (SSTR5), with potential for investigation in type 2 diabetes.

LPA5 antagonist 2 (compound 65) is a highly water-soluble LPA5 antagonist that significantly reduces nociception and can be used to study inflammatory and neuropathic pain.

A3AR antagonist 2 is a potent antagonist of the human A3 adenosine receptor, exhibiting a Ki value of 4.54 nM.

Galectin-3, a β-galactoside-specific carbohydrate recognition protein (lectin), facilitates the migration of B-cell precursor acute lymphoblastic leukemia (BCP-ALL) cells and demonstrates resistance to pharmaceutical interventions.

CCK-B Receptor Antagonist 2 is a potent and orally active antagonist of Gastrin CCK-B (IC50: 0.43 nM). It also inhibits gastrin CCK-A activity (IC50: 1.82 μM).

RXR antagonist 2 is a potent antagonist of RXR (Ki: 0.391 μM, Kd: 0.281 μM). RXR antagonist 2 has shown research potential for RXR-related diseases.

MrgprX2 antagonist-2 is a potent antagonist of MrgprX2. It holds potential for investigating skin inflammatory disorders.

CCR4 antagonist 2 (Compound 31) is a novel, potent, orally bioavailable small molecule antagonist of CC chemokine receptor 4 (CCR4) that inhibits Treg trafficking into the Tumor Microenvironment without suppressing the number of Treg in healthy tissues. CCR4 antagonist 2 (Compound 31) exhibits IC50 values of Ca2+ flux and [chemotaxis] CTX at 40 nM and 70 nM, respectively.

Calcium Channel antagonist 4 is a voltage-gated calcium channel inhibitor (IC50 : 5-20 μM).

Compound 29 is a 5-HT6R antagonist that acts by inhibiting the 5-HT6 receptor.

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.

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.