Alfuzosin hydrochloride is an α1 adrenergic receptor antagonist used to treat benign prostatic hyperplasia (BPH).Target: α1 adrenergic receptorAlfuzosin, a new quinazoline derivative, acts as a selective and competitive antagonist of alpha 1-adrenoceptor-mediated contraction of prostatic, prostatic capsule, bladder base and proximal urethral smooth muscle, thereby reducing the tone of these structures. Consequently, urethral pressure and resistance, bladder outlet resistance, bladder instability and symptoms associated with benign prostatic hyperplasia are reduced. A limited range of clinical studies have shown oral alfuzosin to be more effective than placebo (in studies of < or = 6 months duration), to have sustained effects on long term administration (< or = 30 months), and to be comparable with the alpha 1-adrenoceptor antagonist prazosin, in the symptomatic treatment of benign prostatic hyperplasia.Oral alfuzosin 7.5 to 10 mg/day in divided doses appears to be a promising first-line agent for symptomatic treatment of noncomplicated mild to moderate benign prostatic hyperplasia in patients with a high dynamic component to their obstruction. In addition, alfuzosin offers an alternative to prostatectomy (the current 'gold standard') in patients who require surgery but are unfit for this treatment, and in patients requiring symptomatic relief while awaiting surgery.
PKCη pseudosubstrate inhibitor,myristoylated is cell permeable and can be used to study the mechanism of action of PKCη[1].
hCAI/II-IN-2 (compound 2b) is a potent dual hCA I/II inhibitor with Ki values of 40.97, 15.15 and 61.88 nM for hCA I, hCA II and hCA Ⅸ. hCAI/II-IN-2 possesses anti-hypoxic activity against acute mountain sickness (AMS) and low cellular activity[1].
Cromolyn is a mast cell stabilizer. Cromolyn has the potential for the research of bronchial asthma, allergic rhinitis, and certain allergic eye conditions such as vernal conjunctivitis, keratitis, and keratoconjunctivitis[1].
FGFR3-IN-5 is a potent and selective FGFR3 inhibitor with IC50 values of 3, 44, and 289 nM for FGFR3, FGFR2, and FGFR1, respectively. FGFR3-IN-5 can be used in research of cancer[1].
Eptazocine (Sedapain) is a κ-opioid receptor agonist and μ-opioid receptor antagonist. Eptazocine has the effect of relieving pain[1].
20:1 SM (d18:1/20:1)-d9 is deuterium labeled 20:1 SM (d18:1/20:1).
Lactodifucotetraose (Difucosyllactose) is a tetrasaccharide isolated from human milk. Lactodifucotetraose constitutes of D-glucose, 1 D-galactose, and L-fucose[1].
L-Valine allyl ester p-toluenesulfonate salt is a valine derivative[1].
HZ-1157 inhibits HCV NS3/4A protease with an IC50 of 1.0 μmol/L. HZ-1157 (4a) has a high dengue virus inhibitory activity (EC50 = 0.15 μM) and is a relatively nontoxic (CC50 > 10 μM) dengue antiviral agent[1][2].
Silydianin is an active constituent of Silybium marianum, with exhibit anti-collagenase, antitumor and anti-elastase activities. Silydianin is a natural protein tyrosine phosphatase 1B (PTP1B) with an IC50 of 17.38 μM. Silydianin has inhibitory effect on the in vitro production and release of oxidative products[1][2][3].
11-Dehydroxygrevilloside B is a glucopyranoside.
Fmoc-NH-PEG6-CH2CH2COOH is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].
KHK-IN-2 is a potent and selective ketohexokinase (KHK) inhibitor with an IC50 of 0.45 μM.
Perisesaccharide C is an oligosaccharide isolated from the root barks of Periploca sepium.
Bis-propargyl-PEG12 is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
Phenol Red sodium salt is a water soluble pH indicator used in the 6.8 (yellow) to 8.2 (red) range.
H-Phe(4-I)-OH is a phenylalanine derivative[1].
5-HT6R antagonist 2 (compound 29) is a 5-HT6 receptor antagonist[1].
Leucomalachite green-d6 is the deuterium labeled Fmoc-Gly-OH[1].
SCH 58261 is the adenosine A2A receptor competitive antagonist. Displays 323-, 53- and 100-fold selectivity over A1, A2B and A3 receptors, respectively.target: adenosine A2A receptorIC50: 15 nM [3]in vitro: NK cells were cultured in NK cell media and preincubated with or without 1 uM SCH58261 30 min before simulation with indicated concentrations of IL-18 (R & D Systems) and IL-12p70 (Australian Biosearch) in the presence or absence of NECA (1 uM) or CGS-21680 (100 nM).[1]in vivo: it was demonstrated that the selective antagonist of the A2Areceptor, SCH58261, administered i.p. starting from the early minutes after ischemia induction, reduces ischemic brain damage and neurological deficit 24 h thereafter. vehicle-rats received saline with Tween 80 (1 %) administered (i.p.) .SCH58261 (0.01 mg/kg, i.p.), administered twice/day for 7 days [2]
Tridihexethyl (Pathilon) chloride is an orally active anticholinergic agent and mAChR antagonist, shows activities of antimuscarinic and anticholinergic. Tridihexethyl chloride shows pronounced antispasmodic and antisecretory effects on the gastrointestinal tract. Tridihexethyl chloride can be used in studies of peptic ulcer disease and acquired nystagmus [1][2].
HIV-1 Rev (34-50) is a 17-aa peptide derived from the Rev-responsive element (RRE)-binding domains of Rev in HIV-1, with anti-HIV-1 activity.
KRAS inhibitor 11 is a first-in-class, high-affinity, noncovalent allosteric KRAS inhibitor, disrupts KRAS-Raf interaction with Kd of 1.2 uM; binds to activated KRAS with sub-micromolar affinity and disrupts effector binding, thereby inhibiting KRAS signaling and cancer cell growth; dose-dependently decreases both p-ERK and p-cRaf levels in BHK cells expressing KRASG12D and KRASG12V, suggesting inhibition of RAS signaling via the MAPK pathway.
PROTAC AR Degrader-4 comprises a cIAP1 ligand binding group, a linker and an androgen receptor (AR) binding group. PROTAC AR Degrader-4 is an AR degrader. Degradation inducers based on cIAP1 are called specific and non-genetic IAP-dependent protein erasers (SNIPERs)[1].
TP-7 (Selanc) is a heptapeptide with anxiolythic properties[1].
B-Raf IN 8 (compound 7g) is a potent B-Raf inhibitor, with an IC50 of 70.65 nM. B-Raf IN 8 exhibits antitumor activity against hepatocellular carcinoma (HEPG-2), colon carcinoma (HCT-116), mammary gland (MCF-7) and human prostate cancer (PC-3) cells, with IC50 values of 9.78, 13.78, 18.52 and 29.85 µM[1].
Dehydrocrebanine is an alkaloid that can be isolated from the tuber and leaves of Stephania venosa. Dehydrocrebanine has in vitro anti-cancer activity[1].
Lenacil is a selective uracil substituted herbicide used for control of both annual grasses, broad leafed weeds and some perennial weeds in sugarcane, apples, alfalfa, peaches, peacans, peppermints (Mentha piperita) and sugar beets. Lenacil can inhibit photosynthesis[1][2].
SAR-260301 is a selective PI3Kβ inhibitor with an IC50 of 23 nM.