undergoing

Inosine pranobex (Delimmun) has a number of immunomodulatory effects, including inducing T-lymphocyte differentiation, augmenting macrophage and NK cell functions, and stimulating IL-2 production. Through these effects and others, isoprinosine shows antiviral activity and has applications against subacute sclerosing panencephalitis. It also restores depressed immune responses in Y patients after irradiation and reduces the incidence of infection in leukemia patients undergoing chemotherapy. It is most commonly used to treat the rare measles complication subacute sclerosing panencephalitis in conjunction with intrathecal interferon therapy.

Prasugrel (CS-747) is a piperazine derivative and PLATELET AGGREGATION INHIBITOR that is used to prevent THROMBOSIS in patients with ACUTE CORONARY SYNDROME; UNSTABLE ANGINA and MYOCARDIAL INFARCTION, as well as in those undergoing PERCUTANEOUS CORONARY INTERVENTIONS.

Candoxatril (UK 79300) is an orally active neutral peptide endonuclease (NEP, EC 3.4.24.11) inhibitor that improves exercise capacity in patients with chronic heart failure undergoing angiotensin-converting enzyme inhibition.

TMC647055 Choline Hydroxide Salt is a novel and potent non-nucleoside inhibitor of the HCV NS5B polymerase which potentially for the treatment of HCV infection. It has nanomolar cellular potency (EC(50) of 82 nM) with minimal associated cell toxicity (CC(

Etelcalcetide hydrochloride (AMG 416 hydrochloride) is a synthetic peptide that serves as an allosteric modulator of the calcium-sensing receptor (CaSR), effectively reducing parathyroid hormone (PTH) levels in patients with secondary hyperparathyroidism undergoing hemodialysis.

AZ-Dyrk1B-33 (3-(2-Methyl-4-pyrimidinyl)-1-(phenylmethyl)-1H-pyrrolo[2,3-c]pyridine) is a potent and selective Dyrk1B kinase inhibitor with an IC50 of 7 nM.

RKS262 is a specific cyclin/CDK inhibitor. RKS262 was identified by structural optimization of Nifurtimox which is currently undergoing phase II clinical trials to treat high-risk neuroblastoma. In a NCI(60) cell-line assay RKS262 exhibited significant cytotoxicity in ovarian cancer cells and a variety of other cell lines exceeding effects of commercial drugs such as cisplatin, 5-FU, cyclophosphamide or sapacitabine. Various leukemia cell-lines were most sensitive (GI(50): ~ 10 nM) while several non-small cell lung cancer cell lines and few cell lines from other tissues were relatively resistant (GI(50) > 1 µM) to RKS262 treatment.

8-Bromo NAD+ serves as a prodrug for the cyclic ADP-ribose (cADPR) inhibitor, 8-bromo cADPR, undergoing conversion to its active form by the enzyme CD38. At a concentration of 1 mM, it effectively inhibits the rise in intracellular calcium levels and chemotaxis triggered by N-formyl-Met-Leu-Phe (fMLP) in mouse bone marrow-derived neutrophils. Furthermore, when applied at 100 µM, this compound reduces LPS-induced nitrite production and decreases the secretion of TNF-α and IL-2 in mouse primary microglial cells.

C17 Ceramide is a synthetic ceramide that contains a non-natural C17:0 fatty acid acylated to sphingosine. It has been used as a marker of arylsulfatase A and sphingolipid activator B activity in patients undergoing enzyme replacement therapy for the genetic disease metachromatic leukodystrophy.

SX-576 is undergoing further investigation as a potential therapy for pulmonary inflammation. It is also a potent non-competitive boronic acid-containing CXCR1/2 antagonists.

JM3A, a highly specific peptoid reagent, selectively targets cell surface vimentin (CSV) on early lung cancer cells undergoing tumor transformation. By conjugating with fluorophores [1], JM3A detects and stains CSV, enabling identification of these cells.

Compound 1059182-21-6 features a cyclic structure characterized by a nitrogen atom occupying an apex (corner) within the heterocycle. Its molecular scaffold integrates aromatic properties due to the presence of a conjugated system, while the inclusion of hydroxyl (-OH) groups confers reactive potential for subsequent modification. Additionally, a halogenated component, specifically a bromine atom, is attached to the aromatic ring, enhancing its propensity for undergoing further synthetic transformations.

Etelcalcetide (AMG 416) is a synthetic peptide that serves as an activator of the calcium-sensing receptor (CaSR) and is used as a calcimimetic drug for treating secondary hyperparathyroidism in patients undergoing hemodialysis.

Oleoyl-L-carnitine, a long-chain acylcarnitine, acts as a selective inhibitor of glycine transporter 2 (GlyT2; IC50 = 340 nM) while demonstrating significantly lesser affinity for GlyT1 (IC50 = >10,000 nM). Elevated plasma levels of this compound have been observed in patients suffering from chronic kidney disease or end-stage renal disease undergoing initial hemodialysis, correlating with an increased risk of cardiovascular mortality.

Ciprostene (free base) is a synthetic, chemically stable analog of prostacyclin (PGI2). In animal models, administration of ciprostene resulted in dose-dependent hypotension, tachycardia, and inhibition of ex vivo ADP-induced platelet aggregation. Ciprostene was evaluated in clinical trials in patients with peripheral vascular disease. It was found to reduce restenosis in patients with coronary artery disease undergoing therapeutic percutaneous transluminal coronary angioplasty.

Tariquidar is a P-glycoprotein inhibitor undergoing research as an adjuvant against multidrug resistance in cancer. Tariquidar non-competitively binds to the p-glycoprotein transporter, thereby inhibiting transmembrane transport of anticancer drugs.

Methyltetrazine-Maleimide, a cleavable ADC linker employed in the synthesis of antibody-drug conjugates (ADCs) [1], functions as a click chemistry reagent. It includes a Tetrazine group capable of undergoing an inverse electron demand Diels-Alder reaction (iEDDA) with TCO-containing molecules.

Methyltetrazine-PEG4-aldehyde serves as a cleavable 4-unit PEG ADC linker in antibody-drug conjugates (ADCs) synthesis [1]. It functions as a click chemistry reagent, featuring a Tetrazine group capable of undergoing an inverse electron demand Diels-Alder reaction (iEDDA) with TCO-containing molecules.

Palmitoleoyl-CoA lithium is the lithium salt form of Palmitoleoyl-CoA. It can be activated and transported to mitochondria for metabolism, specifically undergoing β-oxidation. Furthermore, it induces a permeability transition in cardiac mitochondrial membranes, leading to mitochondrial dysfunction. Palmitoleoyl-CoA lithium regulates metabolism through conformational control of the AMPK β1-isoform.

(R)-4-Amino-3-hydroxybutyric acid, also known as (R)-GABOB, acts as a modulator of GABA receptors, specifically binding to both GABAA and GABAB receptors and blocking GABA reuptake in rat brain synaptosomes. Additionally, it serves as a GABAC receptor agonist, triggering currents in patch-clamp assays with Xenopus oocytes that express the human receptor. In vivo studies reveal its capability to suppress electrical discharges in the amygdala in cats undergoing N-amidinobenzamide-triggered seizures, indicating its potential therapeutic application in managing seizure disorders.

CJ-15161 (free base), an opioid κ-receptor agonist, is undergoing development with Pfizer as an analgesic agent.

(R)-3-Hydroxy Midostaurin is a potent inhibitor of kinases,is a major metabolite of midostaurin undergoing by the hepatic CYP3A4 enzyme,has the potential for acute myeloid leukemia (AML).

DBCO-S-S-acid, a cleavable ADC linker for synthesizing antibody-drug conjugates (ADCs) [1], is a click chemistry reagent that features a DBCO group capable of undergoing strain-promoted alkyne-azide cycloaddition (SPAAC) with Azide-containing molecules.

α,α-Trehalose 6-phosphate (Tre6P) potassium is an intrinsic 6-phosphate derivative of α,α′-trehalose that acts as an intermediary metabolite, undergoing enzymatic conversion to the final metabolic product, α,α′-trehalose, via the enzyme Tre6P phosphatase (T6PP) [1].

2-Hexylthiophene, a weakly basic heteroaromatic compound, can enhance the molar absorption coefficient of ruthenium sensitizers by undergoing modification.

5-Aminoimidazole ribonucleotide (AIR) serves as an intermediate in purine biosynthesis, undergoing enzymatic modifications to form inosine monophosphate (IMP), which is subsequently converted into the purine bases adenine (A) and guanine (G) [1].

Efonidipine HCl (NZ-105) serves as both a T-type and L-type calcium channel blocker. This compound, distinct from other calcium channel blockers, notably increases N(6), 2'-O-dibutyryladenosine 3',5'-cyclic monophosphate (dbcAMP)-induced StAR mRNA and DHEA-S production in NCI-H295R adrenocortical carcinoma cells, actions reflective of adrenocorticotropic hormone. Efonidipine uniquely inhibits calcium channels by merging tonic and use-dependent blocking methods. Its inhibitory concentrations (IC50) for I(Ca(T)) and I(Ca(L)) are 0.35 micromol/l and 1.8 nmol/l, respectively. Clinically, efonidipine administered to hypertensive patients undergoing chronic hemodialysis (20-60 mg, twice daily) demonstrated comparable blood pressure control to amlodipine (2.5-7.5 mg, once daily) over a 12-week period without significantly altering pulse rate. Furthermore, efonidipine significantly improved left ventricular ejection fraction in heart failure models without affecting blood pressure, in addition to lowering the heart rate by about 10%.

ABI-231 is a potent, orally bioavailable tubulin inhibitor that interacts with the colchicine binding site and is currently undergoing clinical trials for prostate cancer. ABI-231, has an average IC50 = 5.2 nM against panels of melanoma and prostate cancer cell lines, is orally bioavailable, and strongly suppress melanoma tumors in vivo. ABI-231 holds great promise as a new generation of orally available tubulin inhibitor.

Etanterol is a phenethanolamine derivative and a β2 adrenoceptor agonist that was undergoing phase II trials in Italy as a bronchodilator with Valeas.

CJ-15161 hydrochloride is the salt form of CJ-15161 (free base), an opioid κ-receptor agonist, is undergoing development with Pfizer as an analgesic agent.

H-L-Lys(Norbornene-methoxycarbonyl)-OH hydrochloride is a norbornene-derivatized lysine capable of undergoing click-functionalization. This compound facilitates the mild and selective modification of proteins through a copper-free click reaction [1].

Tetrazine-PEG4-amine (hydrochloride) serves as a cleavable 4-unit PEG ADC linker and a click chemistry reagent in the synthesis of antibody-drug conjugates (ADCs) [1]. It features a Tetrazine group capable of undergoing an inverse electron demand Diels-Alder reaction (iEDDA) with molecules that contain TCO groups.