Faropenem daloxate is the first oral penem in a new class of beta-lactam antibiotics.IC50 Value: Target: AntibacterialFaropenem daloxate is useful for penem and antibiotics. Faropenem medoxomil has excellent in vitro activity against Streptococcus pneumoniae, Haemophilus influenzae and other key pathogens implicated in acute bacterial rhinosinusitis. Clinical studies have demonstrated that, in the treatment of acute bacterial rhinosinusitis in adults, 7 days of treatment with faropenem medoxomil is as clinically and bacteriologically effective as 10 days of treatment with cefuroxime axetil. One study showed faropenem medoxomil to be superior to cefuroxime axetil. Overall, the safety profile of faropenem medoxomil is similar to that of most comparators.
Trandolapril D5 (RU44570 D5) is a deuterium labeled Trandolapril (RU44570). Trandolapril is an orally active angiotensin converting enzyme (ACE) inhibitor for hypertension and congestive heart failure (CHF)[1].
Hemiphroside B is found in Lagotis integra[1].
Lidamidine hydrochloride (WHR-1142A) is an α2-adrenergic receptor agonist and antidiarrheal agent[1].
Methylsticin is a kavalactone isolated from the kava roots. Methylsticin exhibit osteoclast formation inhibitory activity[1].
MCHr1 antagonist 2 is an antagonist of melanin concentrating hormone receptor 1, with an IC50 of 65 nM; MCHr1 antagonist 2 also inhibits hERG, with an IC50 of 4.0 nM in IMR-32 cells.
Scutebata B (compound 4) is a neoclerodane diterpenoid iaolated from the whole plant of Scutellaria barbata. Scutebata B has cytotoxic activities with IC50 values of 10.27～28.48 μM[1].
Senkyunolide I, isolated from Ligusticum chuanxiong Hort, is an anti-migraine compound. Senkyunolide I protects rat brain against focal cerebral ischemia-reperfusion injury by up-regulating p-Erk1/2, Nrf2/HO-1 and inhibiting caspase 3[1][2].
Ursodeoxycholic acid-13C is the 13C labeled Ursodeoxycholic acid. Ursodeoxycholic acid (Ursodeoxycholate) is a secondary bile acid issued from the transformation of (cheno)deoxycholic acid by intestinal bacteria, acting as a key regulator of the intestinal barrier integrity and essential for lipid metabolism. Ursodeoxycholic acid acts as signaling molecule, exerting its effects by interacting with bile acid activated receptors, including G-protein coupled bile acid receptor 5 (TGR5, GPCR19) and the farnesoid X receptor (FXR). Ursodeoxycholic acid can be used for the research of a variety of hepatic and gastrointestinal diseases. Orally active[1][2].
H-Leu-Trp-Met-Arg-OH is a tetrapeptide. H-Leu-Trp-Met-Arg-OH can be used as a substrate for aminopeptidase-mediated hydrolysis studies[1].
Britannilactone diacetate shows potential antiinflammatory, antibacterial, antihepatitic, antidiabetes, and antitumor activities.
LOE 908 hydrochloride is a non-selective cation channel (NSCC) inhibitor[1].
(S)-2-((S)-2-((S)-2-Amino-3-methylbutanamido)-3-(4-hydroxyphenyl)propanamido)-3-methylbutanoic acid is a valine derivative[1].
Rotigotine is a full agonist of dopamine receptor, a partial agonist of the 5-HT1A receptor, and an antagonist of the α2B-adrenergic receptor, with Kis of 0.71 nM, 4-15 nM, and 83 nM for the dopamine D3 receptor and D2, D5, D4 receptors, and dopamine D1 receptor.
3’-O-t-Bulyldimethylsilylthymidine is a purine nucleoside analog. Purine nucleoside analogs have broad antitumor activity targeting indolent lymphoid malignancies. Anticancer mechanisms in this process rely on inhibition of DNA synthesis, induction of apoptosis, etc[1].
Boc-beta-t-butyl-d-alanine is an intermediate, can be used in the synthesis of peptides and other amino acids[1].
CHK1-IN-2 is a checkpoint kinase 1 (CHK1) inhibitor, with an IC50 of 6 nM.
Sulindac sulfide is a noncompetitive γ-secretase inhibitor, with an IC50 of 20.2 μM for γ42-secretase activity.
Acetazolamide sodium is the sodium salt of Acetazolamide. Acetazolamide is a carbonic anhydrase (CA) IX inhibitor with an IC50 of 30 nM for hCA IX. Acetazolamide has diuretic, antihypertensive and anti-gonococcal activities[1][4][5][6].
Thioether-cyclized helix B peptide, CHBP can improve metabolic stability and renoprotective effect through inducing autophagy via inhibition of mTORC1 and activation of mTORC2[1].
Cinchonain IIa is an antioxidant agent with EC50s of 6.8 μM and 26.5 μM for DPPH and PMS-NADH[1].
Polaprezinc is an orally bioavailable chelate composed of zinc and L-carnosine, with potential gastroprotective, anti-oxidant, anti-ulcer and anti-inflammatory activities.
Bacopaside I, a saponin isolated from Bacopa monniera, exbibits antioxidant properties and free radical scavenging capacity and exerts antidepressant-like effect[1].
[Thr28, Nle31]-Cholecystokinin (25-33) is a biological active peptide. (Cholecystokinin (CCK) acts both as a hormone and a neurotransmitter and is found in the GI system and the central nervous system. It is a satiety peptide that inhibits food intake.This Cholecystokinin (CCK) analog retains all the bioactivities of CCK8, but was found to be remarkably more stable in acidic media and unaffected by air oxidation due to Met replacements (Thr 28 and Nle31 were substituted for Methionine). The predominant conformation contains a gamma-turn centered on Thr4, separated by Gly5 from a helical segment that comprises the C-terminal residues.)
5’-O-Acetyl-2’,3’-dideoxy-2’,3’-didehydro-5-fluoro-uridine is a purine nucleoside analog. Purine nucleoside analogs have broad antitumor activity targeting indolent lymphoid malignancies. Anticancer mechanisms in this process rely on inhibition of DNA synthesis, induction of apoptosis, etc[1].
Boc-NH-PEG4-C2-Boc is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
Nerindocianine is a fluorescent diagnostic contrast agent. Nerindocianine is highly hydrophilic and is primarily metabolized by the kidneys, allowing for a non-invasive intraoperative ureteral imaging[1].
Bursin is a peptide that can be isolated from the bursa of Fabricius of chicken. Bursin induces the phenotypic differentiation of mammalian and avian B precursor cells. Bursin also increases cyclic guanosine monophosphate in cells of the human B-cell line Daudi[1].
JAK-IN-31 (Example 75) is a JAK inhibitor with IC50 ranges of ≤0.01µM, ≤0.01µM, 0.01-0.1 µM and ≤0.01µM for JAK1, JAK2, JAK3 and Tyk2 respectively. JAK-IN-31 can be used in cancer research[1].
NNC63-0532 is a novel non-peptide nociceptin receptor (ORL1) agonist, with EC50s of 305?nM. NNC63-0532 plays important roles in many disorders such as pain, drug addiction[1].