Almotriptan is a 5-HT1B/1D-receptor agonist used to treat migraine.IC50:Target: 5-hydroxytryptamine1B/1D (5-HT1B/1D) ReceptorAlmotriptan is a selective 5-hydroxytryptamine1B/1D (5-HT1B/1D) receptor agonist, used for the treatment of Migraine attacks in adults. Almotriptan showed low nanomolar affinity for the 5-HT(1B) and 5-HT(1D) receptors in several species, including the human, while affinity for 5-HT receptors other than 5-HT(1B/1D) was clearly less. Almotriptan did not exhibit significant affinity for several non-5-HT receptors studied up to 100 microM. Almotriptan inhibited forskolin-stimulated cyclic AMP accumulation in HeLa cells transfected with 5-HT(1B) or 5-HT(1D) human receptors [1]. Almotriptan had a mild antiemetic effect and a slight, transient diuretic effect in dogs, although the latter effect is probably of no clinical relevance. In addition, no effect on the respiratory system of conscious guinea pigs was observed following almotriptan treatment. These results indicate that almotriptan has a favourable safety profile with respect to the central nervous, renal and respiratory systems [2].
Zalypsis (PM00104) has anti-tumor activity. Zalypsis binds to DNA and shows cytotoxicity. Zalypsis inhibits cell cycle and transcription, and leads to double stranded DNA breaks[1][2].
ME1111 is an antifungal agent that is active against dermatophytes. ME1111 is an inhibitor of the succinate dehydrogenase of Trichophyton species. ME1111 has an excellent ability to penetrate human nails and is used for onychomycosis research[1][2].
Juncutol is a potent inducible nitric oxide synthase (iNOS) inhibitor. Juncutol decreases the LPS (HY-D1056)-stimulated iNOS protein expression[1].
CXCR2 antagonist 8 is a potent and selective CXCR2 antagonist. CXCR2 antagonist 8 can be used for insulin resistance research[1].
KRAS G12C inhibitor 57 (Compound 50) is a potent, selective, covalent and orally active KRAS G12C inhibitor with an IC50 of 0.21 μM in KRAS G12C/SOS1 binding assay. KRAS G12C inhibitor 57 induces cancer cell apoptosis[1].
Chlorhexidine is an antibacterial used as an antiseptic and for other applications.Target: AntibacterialChlorhexidine belongs to a group of medicines called antiseptic antibacterial agents. It is used to clean the skin after an injury, before surgery, or before an injection. Chlorhexidine is also used to clean the hands before a procedure. It works by killing or preventing the growth of bacteria on the skin.
Murpanicin (murraxocin) 是一种香豆素,是一种热敏瞬时受体电位香草酸 2 (TRPV2) 通道抑制剂。Murpanicin具有明显的抗炎、杀虫作用。
L-Arginine-13C ((S)-(+)-Arginine-13C) hydrochloride is the 13C-labeled L-Arginine hydrochloride. L-Arginine hydrochloride ((S)-(+)-Arginine hydrochloride) is the nitrogen donor for synthesis of nitric oxide, a potent vasodilator that is deficient during times of sickle cell crisis.
Omidenepag,a pharmacologically active form of Omidenepag Isopropyl, is a selective, non-prostanoid EP2 receptor agonist, with an EC50 of 1.1 nM. Omidenepag shows binding affinities (IC50) 10 nM for h-EP2[1].
Fluorogestone acetate is a progesterone compound. Fluorogestone acetate inhibits ovulation and synchronizes the estrous cycle in cattle by inhibiting the release of luteinizing hormone (LH) from the pituitary gland[1].
AGN 193109 is a retinoid analog, and acts as a specific and highly effective antagonist of retinoic acid receptors (RARs), with Kds of 2 nM, 2 nM, and 3 nM for RARα, RARβ, and RARγ, respectively.
Zibotentan (ZD4054) is an orally administered, potent and specific ETA-receptor (endothelin A receptor) antagonist (IC50 = 21 nM). IC50 value: 21 nM Target: ETA receptorZibotentan is capable of inhibiting or reducing the multitude of effects that are evoked by ET-1 activation of the ETA receptor and which promote tumor survival, growth and progression. Zibotentan (ZD4054) treatment produced significant inhibition of tumor growth in ovarian and breast xenografts.
Benzyl alcohol-d1 is the deuterium labeled Benzyl alcohol[1].
3-Methylcyclohex-2-en-1-ol, isolated fromDendroctonus, is a potent antiaggregative pheromone[1].
Irloxacin (Pirfloxacin) is a quinolone antibacterial agent. Irloxacin shows greater activity with an acid pH. Irloxacin has a good in vitro antimicrobial spectrum against both gram-positive and gram-negative bacteria. Orally active[1].
GSK2239633A is a CC-chemokine receptor 4 (CCR4) antagonist, which inhibits the binding of [125I]-TARC to human CCR4 with a pIC50 of 7.96 ± 0.11.
GDC-0834 is a potent and selective BTK inhibitor. GDC-0834 inhibits BTK with an in vitro IC50 of 5.9 and 6.4 nM in biochemical and cellular assays, respectively, and in vivo IC50 of 1.1 and 5.6 μM in mouse and rat, respectively.
H-Gly-His-Arg-Pro-NH is a biologically active polypeptide that can be found by peptide screening. Peptide screening is a research tool that pools active peptides primarily by immunoassay. Peptide screening can be used for protein interaction, functional analysis, epitope screening, especially in the field of drug research and development[1].
Semicarbazide hydrochloride, a derivative of urea, possesses antiviral, antiinfective and antineoplastic through binding to copper or iron in cells[1].
eFT508 is a potent, highly selective, and orally bioavailable MNK1 and MNK2 inhibitor, with IC50s of 1-2 nM against both isoforms.
SLM6031434 hydrochloride is a highly selective sphingosine kinase 2 (SphK2) inhibitor with Kis of 0.4 μM, 0.5 μM, >20 μM, 22 μM for mSphK2, rSphK2, mSphK1 and rSphK1, respectively. SLM6031434 hydrochloride decrease Sphingosine 1-phosphate (S1P) levels in U937 monocytic leukemia cells. SLM6031434 hydrochloride has the potential for renal fibrosis research[1][2].
Solifenacin Succinate(YM905; Vesicare) is a muscarinic receptor antagonist.IC50 value:Target: muscarinic receptorSolifenacin succinate (YM905; Vesicare) is a prescription medication used to treat certain bladder problems.
ACTH (4-9) is an adrenocorticotropic hormone (ACTH) fragment. ACTH (4-9) is the 4-9 sequence fragment of ACTH[1][2].
Maleic hydrazide-d2 is the deuterium labeled Maleic hydrazide[1]. Maleic hydrazide is extensively used as a systemic plant growth regulator and as a herbicide. Maleic hydrazide acts as an inhibitor of the synthesis of nucleic acids and proteins[2][3].
Uralenol is a natural PTP1B inhibitor (IC50=21. 5 μM) from Broussonetia papyrifera. PTP1B have been shown to play a major role in the dephosphorylation of the insulin receptor in many cellular and biochemical studies[1].
Dapansutrile (OLT1177) is a potent, selective and orally active inhibitor of NLRP3 inflammasome. Anti-inflammatory, analgesic activity[1].
DOTAP Transfection Reagent is a cationic derivative of trimethylammonium attached to two 18-carbon fatty acid tails, each with a single alkene group. 18:1 TAP is a cationic liposome-forming compound useful for the transfection of DNA, RNA, and other negatively charged molecules into eukaryotic cells. Reagent grade, for research use only.
Frexalimab (SAR441344; INX-021) is a monoclonal antibody targeting the CD40 ligand (CD40L). Frexalimab has the potential for multiple sclerosis research[1].
PTGR2-IN-1 is a potent PTGR2 inhibitor with an IC50 of ~0.7 μM. PTGR2-IN-1 increases 15-keto-PGE2-dependent PPARγ transcriptional activity in PTGR2-transfected HEK293T cells[1].