Ropinirole hydrochloride(SKF101468 hydrochloride) a selective dopamine D2 receptor inhibitor with IC50 of 29 nM.Target: Dopamine D2 ReceptorRopinirole (50 mg/kg, i.p.) causes biphasic spontaneous locomotor activity in mice. Ropinirole (0.05-1.0 mg/kg SC) dose-dependently inhibits the dyskinesias induced by 2-di-n-propylamino-5,6-di-hydroxytetralin in mice. Ropirtirole, at doses of 1 and 10 μg, injected unilaterally directly into the striatum of the rat causes marked, contralateral (away from the side of injection) asymmetry and circling in mice. Ropinirole (0.05-1.0 mg/kg SC or 0.1 mg/kg PO) reverses all motor and behavioural deficits induced by MPTP in marmosets [1]. Ropinirole (2 mg/kg, i.p.) for 7 days increases GSH, catalase and SOD activities in the striatum and protected striatal dopaminergic neurons against 6-hydroxydopamine (6-OHDA) in mice [2]. Ropinirole (0.2 mg/kg, i.p.) improves the use of previously akinetic forelimb and produced robust circling behavior in lesioned rats with striatal over-expression of both D2R and D3R compared to lesioned animals that received blank vector. The subtherapeutic dose of ropinirole generates only modest motor effects in lesioned rats with sole over-expression of D2R or D3R [3]. Ropinirole (1-8 mg t.i.d.) is rapidly and completely absorbed with oral bioavailability of 55%, clearance of 780 mL/min, elimination half-life of 6 hours in healthy volunteer. Since the major route of elimination for Ropinirole is by the CYP enzyme system, mainly by CYP1A2 and also by CYP3A4, inhibition of the former and possibly the latter may reduce the agent's clearance and lead to drug accumulation [4].
(E)-β-Farnesene (trans-β-Farnesene) is a volatile sesquiterpene hydrocarbon which can be found in Phlomis aurea Decne essential oil. (E)-β-Farnesene can be used as a feeding stimulant for the sand fly Lutzomyia longipalpis[1][2].
Bexarotene D4 is a deuterium labeled Bexarotene (LGD1069). Bexarotene (LGD1069) is a selective retinoid X receptors (RXR) agonist for the treatment of cutaneous T-cell lymphoma[1][2][3][4][5].
DCG066 is a G9a inhibitor in vitro.
Alfuzosin 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.
Mad1 (6-21) is the 6-21 fragment of Mad1 protein. Mad1 (6-21) binds to mammalian Sin3A PAH2 with a Kd of ~29 nM[1].
N-Caffeoylputrescine,(E)- is a caffeic acid amide found in the tobacco plants (Nicotiana tabacum L.)[1].
Ammonium iron(III) citrate (Ammonium ferric citrate), a physiological form of nonetransferrin-bound iron, induces intracellular iron overload to cause ferroptosis[1]. Ammonium iron(III) citrate can enhance protein production[2].
AS-1763 is a potent, selective, noncovalent, and orally available inhibitor of Bruton’s tyrosine kinase (IC50 = 0.85 nM).
GAT-211 (GAT211) is a selective cannabinoid 1 receptor (CB1R) positive allosteric modulator with pKb of 7.26, Arrestin2 EC50 of 775 nM; engages CB1R allosteric site(s), enhances the binding of the orthosteric full agonist [3H]CP55,490, and reduces the binding of the orthosteric antagonist/inverse agonist [3H]SR141716A; displayed both PAM and agonist activity in HEK293A and Neuro2a cells expressing human recombinant CB1R (hCB1R) and in mouse-brain membranes rich in native CB1R.
N-Mal-N-bis(PEG4-NH-Boc) is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
16(R/S)-Hydroxy-3,13Z-kolavadien-15,16-olide-2-one (compound 9) is a diterpene compound isolated from the unripe fruits of Polyalthia longifolia var. pendula[1].
Quetiapine sulfoxide is a metabolite of Quetiapine, which is an atypical antipsychotic compound.
DMNQ is a redox cycling agent that generates both superoxide and hydrogen peroxide intracellularly in a concentration dependent manner. DMNQ increases ROS generation[1].
Zelenectide (BCY8116) is a Bicycle peptide targeting to Nectin-4, which is a cell adhesion molecule. Zelenectide serves as a Bicycle tumor-targeted immune cell agonist[1].
ERB-196 is a nonsteroidal selective estrogen receptor-β (ERβ) agonist.
N,N-Dimethylformamide (DMF) is widely used as a drug solvent. N,N-Dimethylformamide is a dipolar protophilic solvent with physicochemical properties that makes it suitable as solvent for capillary electrophoresis (CE)[1][2].
BnO-PEG4-OH is a PEG-based PROTAC linker can be used in the synthesis of PROTACs.
CC-115 hydrochloride is a potent and dual DNA-PK and mTOR kinase inhibitor with IC50s of 13 nM and 21 nM, respectively. CC-115 blocks both mTORC1 and mTORC2 signaling.
Saredutant is a selective NK2 receptor antagonist.
Chlorthal-dimethyl used as a pesticide intermediate.
Carviolin is a compound isolated from the mycelia of the ascomycete Neobulgaria pura. Carviolin inhibits the formation of appressoria in germinating conidia of Magnaporthe grisea on inductive (hydrophobic) surface. Carviolin exhibits moderate cytotoxic, but no antifungal, antibacterial, or phytotoxic activities[1].
Temocapril-d5 is the deuterium labeled Temocapril. Temocapril is an angiotensin-converting enzyme (ACE) inhibitor. Temocapril hydrochloride can be used for the research of hypertension, congestive heart failure, acute myocardial infarction, insulin resistance, and renal diseases[1][2].
Filanesib (ARRY-520) is a synthetic kinesin spindle protein (KSP) inhibitor with IC50 of 6 nM.
Tetrazine-Ph-PEG5-NHS ester is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
TP4 (Nile tilapia piscidin) is an orally active piscidin-like antimicrobial peptide. TP4 inhibits multiple gram positive and negative strains (MIC: 0.03-10 μg/mL). TP4 shows hemolytic activities. TP4 enhances immune response, antioxidant activity, and intestinal health against bacterial infections. TP4 also has anti-tumor effect, and induces necrosis by triggering mitochondrial dysfunction in cancer cells[1][2][3].
4-Cumylphenol is a polycarbonate chain terminator. 4-Cumylphenol is widely used as a material for polycarbonate plastics, surfactants, fungicides and preservatives. 4-Cumylphenol also induces lipid accumulation in mouse adipocytes[1][2][3].
Tetramethylthiuram monosulfide (TMTM) is an active compound. Tetramethylthiuram monosulfide (TMTM) can be used for the research of rubber and various biochemical studies[1][2].
LEM-14 is a specific inhibitor of histone lysine methyltransferase NSD2 (MMSET/WHSC1) with in vitro IC50 of 132 uM, and that is inactive against the closely related NSD1 and NSD3.
Coronarin A is an orally active natural compound that inhibits mTORC1 and S6K1 to increase IRS1 activity. Coronarin A shows anti-inflammatory activity and can also be used for type 2 diabetes mellitus research[1].