(±)-WB 4101 is a potent antagonist of noradrenaline. (±)-WB 4101 interacts with protein in smooth muscle. (±)-WB 4101 makes drug and receptor bind tightly[1].
DS-3801b is a potent and non-macrolide agonist of GPR38. DS-3801b is expected to be novel gastrointestinal prokinetic agents for the research of functional gastrointestinal disorders such as gastroparesis and chronic constipation[1].
H-Ser-Gln-OH is a biologically active peptide.
Cyanine5.5 alkyne chloride, a near-infrared (NIR) fluorescent dye, is an alkyne modified Cyanine5.5 (Ex=680 nm, Em=710 nm). Cyanine5.5 alkyne chloride can react with azides for Click Chemistry labeling[1].
UNC9995 is a β-arrestin2-biased agonist of dopamine receptor Drd2. UNC9995 inhibits NLRP3 inflammasome activation by enhancing β-arrestin2-NLRP3 interaction, thus prevents neuronal degeneration. Futhermore, UNC9995 activates the Drd2/β-arrestin2 signaling to prevent inflammation-related genes transcription-induced by JAK/STAT3. UNC9995 improves depressive behavior in mouse model, and improves astrocytes dysfunctions[1].
Terazosin is a selective alpha1-antagonist used for treatment of symptoms of benign prostatic hyperplasia (BPH).Target: Alpha-1 Adrenergic ReceptorTerazosin is selective for alpha 1A-adrenoceptors which appear to dominate in the human prostate; the therapeutic relevance of this selectivity remains to be assessed in clinical studies [1]. Administration of terazosin 1 mg orally for 28 d. Terazosin initially shifted the dose-response curve of phenylephrine to the right, with a significant increase in ED50 for phenylephrine from a control value of 102 to 759 ng/min on day 1 of terazosin (P < 0.001). The mean Kd of terazosin was estimated as 11 +/- 15 nM in the first few days of treatment. This study demonstrates that pharmacological tolerance to the alpha 1-adrenoceptor blocking action of terazosin occurs in man and may be responsible for loss in efficacy with chronic therapy [2].
2,6-Dimethylpyrazine is a key aroma compound in Boletus edulis[1].
Kisspeptin 13 is a GPR54 and GnRH receptor activator, an endogenous active isoform. Kisspeptin 13 enhances memory and can be used in Alzheimer's disease research[1].
Brevianamide F , also known as cyclo-(L-Trp-L-Pro), belongs to a class of naturally occurring 2,5-diketopiperazines.Brevianamide F possess interesting breast cancer resistance protein inhibitory activity.[1] brevianamide F once used as aromatic substrate. [2]
Milpocitide is a low-density lipoprotein receptor (human LDL receptor, LDLR), (293-333)-peptide fragment (EGF-like domain 1)[1].
3-Keto petromyzonol, a main component of Sea lamprey male sex pheromones, modulates both synthesis and release of gonadotropin releasing hormone (GnRH), and subsequently, hypothalamic-pituitary-gonadal (HPG) output in immature sea lamprey[1].
C12-200 is a benchmark ionizable cationic lipidoid along with helper lipids. C12-200 is commonly used for mRNA delivery[1][2].
Dimethyl pimelate-d4 is the deuterium labeled Dimethyl pimelate[1].
Blonanserin dihydrochloride is a potent and orally active 5-HT2A and dopamine D2 receptor antagonist, with Ki values of 0.812 and 0.142 nM, respectively. Blonanserin dihydrochloride is usually acts as an atypical antipsychotic agent, and can be used for the research of extrapyramidal symptoms, excessive sedation, or hypotension[1][2].
Iodoacetamide-PEG3-azide is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
α-Lactose (α-D-Lactose) is the major sugar present in milk. Lactose exists in the form of two anomers, α and β. The α form normally crystallizes as a monohydrate[1][2].
Terbutryn-d5 is the deuterium labeled Terbutryn[1].
Benzenecarboximidamide, hydrochloride, hydrate (1:1:x) (Benzamidine hydrochloride hydrate) is a reversible competitive trypsin-like serine proteases inhibitor with Kis of 20, 21, 97, 110, 320 and 750 μM against Tryptase, Trypsin, uPA, Factor Xa, Thrombin and tPA, respectively[1][2].
Uridylate kinase is a member of the nucleoside mono-phosphate (NMP) kinase family and catalyzes the reaction ATP+NMP?ADP+NDP with moderate specificity for UMP[1].
Fenitrothion, one of the most widely used organophosphorus pesticides, is a cholinesterase inhibiting insecticide/acaricid. Fenitrothion is widely used, as a broad-spectrum insecticide, on cotton crops, vegetables crops, fruit crops, and field crops especially paddy. Fenitrothion leads to accumulation of nitrophenols[1][2].
Antioxidant agent-4 (Compound 2) is an effective antioxidant molecule with antilipid peroxidative activity[1].
GPS491 (EC50 = 0.47 μM) suppresses expression of the HIV-1 structural protein Gag and alters HIV-1 RNA accumulation, decreasing the abundance of RNAs encoding the structural proteins while increasing levels of viral RNAs encoding the regulatory proteins.
Betamethasone (hydrochloride) is a glucocorticoid steroid with anti-inflammatory and immunosuppressive properties.Target: Glucocorticoid ReceptorBetamethasone (hydrochloride) is the hydrochloride of betamethasone, which is a potent glucocorticoid steroid with anti-inflammatory and immunosuppressive properties. Unlike other drugs with these effects, betamethasone does not cause water retention. The median (range) IC50 value for betamethasone butyrate propionate evaluated in the streptococcal pyrogenic enterotoxin A-stimulated peripheral-blood mononuclear cells was 291.6 (0.001-1171.5) ng/ml, which was significantly higher than the value 0.072 (0.01-222.5) ng/ml found in concanavalin A-stimulated peripheral-blood mononuclear cells (P=0.0245) [1]. Children exposed prenatally to betamethasone (n = 121) did not differ in systolic or diastolic blood pressure from children exposed to placebo (n = 102) (mean difference: systolic: -1.6 mm Hg; 95% confidence interval: -4.1 to 0.8 mm Hg; diastolic: -0.3 mm Hg; 95% confidence interval: -2.5 to 1.8 mm Hg) [2]. Intra-articular corticosteroid injection of 6 mg of betamethasone acetate/betamethasone sodium phosphate at the knee joint was not significantly associated with SAI at the time points tested [3].Clinical indications: Dermatitis; Discoid lupus erythematosus; Eczema; Lichen; Prurigo; PsoriasisToxicity: Symptoms of overdose include burning, itching, irritation, dryness, folliculitis, hypertrichosis, acneiform eruptions, hypopigmentation, perioral dermatitis, allergic contact dermatitis, maceration of the skin, secondary infection, skin atrophy, striae, and miliaria.
Polzastobart (JTX-8064) is a humanized IgG4 monoclonal antagonist antibody that selectively binds LILRB2 and prevents it from binding its ligands, classical and non-classical MHC I molecules. Polzastobart enhances pro-inflammatory cytokine production in macrophages by blocking the ability of LILRB2 to bind HLA-A/B and/or HLA-G, a marker of immunotolerance on cancer cells. Polzastobart is a macrophage immune checkpoint inhibitor[1].
Halazone is an atypical antimicrobial sulfonamide derivative and a carbonic anhydrase II inhibitor with a Kd value of 1.45 µM. Halazone protects sodium channels from inactivation. Halazone is widely used for disinfection of drinking water[1][2].
Siccanin is a succinate dehydrogenase (SDH) inhibitor (IC50=0.9 μM) with species-selective activity. Siccanin also is a antibiotic against pathogenic fungi[1].
Nitrilotriacetic acid-d9 is the deuterium labeled Nitrilotriacetic acid[1]. Nitrilotriacetic acid is an aminotricarboxylic acid. Nitrilotriacetic acid can be used as a chelating agent, forming coordination compounds with metal ions[2].
2’-Deoxy-2’-fluoro-alpha-D-arabinoguanosine 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].