refractory

Eliapixant (BAY 1817080) (BAY 1817080) is a potent and selective P2X3 receptor antagonist, with an IC50 of 8 nM. Eliapixant can be used for the research of refractory chronic cough.

Brentuximab, a chimeric antibody targeting CD30, is a naked antibody to Brentuximab vedotin. It possesses antitumor activity and may be used to study relapsed or refractory Hodgkin's lymphoma.

DRF-1042, an orally active camptothecin analog, exhibits anticancer and insecticidal activities by inhibiting DNA topoisomerase I. It has been studied for its efficacy against solid tumors, including prostate and colon cancers.

DRF-1042 HCl is an orally active camptothecin analog with antitumor activity, inhibits DNA topoisomerase I, and is used in the study of refractory solid tumors.

Etripamil (MSP-2017) displays atrioventricular nodal conduction and prolongs atrioventricular nodal refractory periods by inhibiting calcium ion influx through the calcium slow channels in the atrioventricular node cells. Etripamil is an antagonist of short-acting L-type calcium-channel. It has a rapid onset of action designed for intranasal administration. It is also used to treat Paroxysmal Supraventricular Tachycardia.

XRP44X (XRP 44X) is a potent inhibitor of Ras-Net (Elk-3) pathway.

NSC-639829 is an anti-tumor compound that requires a solubilizing agent for dissolution.

Propafenone (Propafenonum) is only found in individuals that have used or taken this drug. It is an antiarrhythmia agent that is particularly effective in ventricular arrhythmias. It also has weak beta-blocking activity. The drug is generally well tolerated. The electrophysiological effect of propafenone manifests itself in a reduction of upstroke velocity (Phase 0) of the monophasic action potential. In Purkinje fibers, and to a lesser extent myocardial fibers, propafenone reduces the fast inward current carried by sodium ions, which is responsible for the drugs antiarrhythmic actions. Diastolic excitability threshold is increased and effective refractory period prolonged. Propafenone reduces spontaneous automaticity and depresses triggered activity. At very high concentrations in vitro, propafenone can inhibit the slow inward current carried by calcium but this calcium antagonist effect probably does not contribute to antiarrhythmic efficacy.

Dofetilide (UK 68789) is a sulfonamide class III antiarrhythmic agent and potassium channel blocker. Dofetilide selectively blocks cardiac ion channels of the rapid component of the delayed rectifier potassium current Ikr. This antiarrhythmic agent prolongs cardiac action potential duration and effective refractory period due to delayed repolarization without affecting conduction velocity. This results in a normal sinus rhythm. Dofetilide is used in the treatment of atrial fibrillation and flutter.

ROS inducer 3 is a reactive oxygen species inducer, a fungicide used to study refractory plant bacterial diseases, and inhibits actinobacteria.

1. Flavokawain B (Flavokavain B) has potent anti-inflammatory activity, can significantly inhibit production of NO and PGE2 in LPS-induced RAW 264.7 cells. 2. Flavokawain B, the hepatotoxic constituent from kava root, induces GSH-sensitive oxidative stress through modulation of IKK NF-κB and MAPK signaling pathways. 3. Flavokawain B induces apoptosis, has the potential usefulness of FKB for prevention and treatment of hormone-refractory prostate cancer in an adjuvant setting. 4. Flavokawain B acts through ROS generation and GADD153 up-regulation to regulate the expression of Bcl-2 family members, thereby inducing mitochondrial dysfunction and apoptosis in HCT116 cells.

Molibresib besylate (GSK 525762C) is a selective and potent inhibitor of the bromodomain and extra-terminal (BET) family of proteins with potential anticancer activity for the study of refractory hematologic malignant diseases.Molibresib besylate generates reactive oxygen species (ROS), which potentiate ATM activation.

Parsaclisib (INCB050465) is a potent and selective inhibitor of PI3Kδ(IC50 of 1 nM at 1 mM ATP)

BAY1238097, a potent and selective bromodomain and extra-terminal motif (BET) inhibitor with anticancer activity, exhibits strong antiproliferative effects in AML (Acute Myeloid Leukemia) and MM (Multiple Myeloma) models. BAY1238097 is useful for studying advanced refractory malignancies.

Valemetostat tosylate is a dual inhibitor of EZH1 2 and used in the research of relapsed refractory peripheral T-cell lymphoma.

Valemetostat (DS-3201) is an EZH1 2 inhibitor that can be used to study relapsed refractory peripheral T-cell lymphoma.

EC0489 is a small molecule-drug conjugate (SMDC) that combines folic acid and desacetyl vinblastine hydrazide, serving as a high-affinity ligand for the folate receptor (FR) in refractory or metastatic tumors.

Lycopodine, a bioactive compound derived from Lycopodium clavatum spores, effectively inhibits the proliferation of HeLa cells through the induction of apoptosis. This process is mediated by caspase-3 activation. In refractory prostate cancer cells, Lycopodine triggers apoptosis by modulating 5-lipoxygenase and depolarizing the mitochondrial membrane potential, without altering p53 activity.

Orvepitant maleate is an effective, selective, and well-tolerated neurokinin-1 receptor (NK-1) antagonist (pKi: 10.2 for human neurokinin-1 receptor). Orvepitant maleate has the potential for depressive disorder and chronic refractory cough (CRC) treatmen

FLT3 HDAC-IN-1 is a dual inhibitor targeting FLT3 and HDAC, with IC50 values of 30.4 nM for FLT3 and 52.4, 14.7 nM for HDAC1 3, respectively. It induces apoptosis in MV-4-11 cells and exhibits antiproliferative effects against BaF3 cells transformed by FLT3 mutations. FLT3 HDAC-IN-1 is useful for research on refractory solid tumors and hematological malignancies.

TBC-3711 is a potential endothelin ETA receptor antagonist aimed at treating refractory hypertension.

Etripamil (MSP-2017) hydrochloride is a fast-acting L-type calcium channel blocker used in the study of paroxysmal supraventricular tachycardia (PSVT). By inhibiting calcium ion influx through slow calcium channels, etripamil hydrochloride slows atrioventricular nodal conduction and extends the atrioventricular nodal refractory period.

Lonitoclax is an inhibitor of B-cell lymphoma 2 (Bcl-2). It demonstrates antitumor activity in B-cell and myeloid malignancy models comparable to Venetoclax. Lonitoclax holds potential for research in relapsed or refractory chronic lymphocytic leukemia (CLL), small lymphocytic lymphoma, and certain low-grade lymphomas.

Clifutinib (Compound 9e) is an orally active, selective inhibitor of FMS-like tyrosine kinase 3 (FLT3-ITD) with an IC50 of 15.1 nM. It inhibits FLT3-ITD kinase activity and blocks downstream signaling pathways, including RAS/MAPK, PI3K/AKT, and JAK/STAT5. Clifutinib induces apoptosis in FLT3-ITD mutated acute myeloid leukemia (AML) cells and is a potential candidate for research in relapsed/refractory FLT3-ITD positive AML.