Brodimoprim (Ro 10-5970), a trimethoprim analogue, is an orally active dihydrofolate reductase inhibitor. Brodimoprim is highly active against a broad spectrum of gram-negative and gram-positive bacteria[1].
Polycarbophil can be used as an excipient, such as ointment base, release blocker, thickener, emulsifier. Pharmaceutical excipients, or pharmaceutical auxiliaries, refer to other chemical substances used in the pharmaceutical process other than pharmaceutical ingredients. Pharmaceutical excipients generally refer to inactive ingredients in pharmaceutical preparations, which can improve the stability, solubility and processability of pharmaceutical preparations. Pharmaceutical excipients also affect the absorption, distribution, metabolism, and elimination (ADME) processes of co-administered drugs[1].
TC-SP 14 (compound 14) is an orally active and potent S1P1 agonist (EC50 = 0.042 μM) with minimal activity at S1P3 (EC50 = 3.47 μM). TC-SP 14 significantly reduces blood lymphocyte counts and attenuates a delayed type hypersensitivity (DTH) response to antigen challenge[1].
Biotin-C5-NHS Ester is an alkyl/ether-based PROTAC linker that can be used in the synthesis of PROTACs[1].
Platyphyllenone is a narutal product that can be isolated from Alnus japonica[1].
2′-O-Methylphloretin (compound 3) is a flavonoid derivative. 2′-O-Methylphloretin can be isolated from the leaves of Melodorum siamensis. 2′-O-Methylphloretin inhibits the tumor cell line replication[1].
PROTAC Linker 9 is a PROTAC linker, which refers to the alkyl/ether composition. PROTAC Linker 9 can be used in the synthesis of a series of PROTACs. PROTACs contain two different ligands connected by a linker; one is a ligand for an E3 ubiquitin ligase and the other is for the target protein. PROTACs exploit the intracellular ubiquitin-proteasome system to selectively degrade target proteins[1].
ERD-3111 (Compound 44) is an orally active PROTAC ERα degrader (DC50: 0.5 nM). ERD-3111 inhibits tumor growth in the parental MCF-7 xenograft model with wild-type ER and two clinically relevant ESR1 mutated mice model. ERD-3111 can be used in the research of ER+ breast cancer[1].
(S,R,S)-AHPC-C7-amine (VH032-C7-amine) is a synthesized E3 ligase ligand-linker conjugate that incorporates the VH032 based VHL ligand and a linker used for estrogen-related receptor α (ERRα) PROTAC degrader[1].
Velneperit (S-2367) is a novel neuropeptide Y (NPY) Y5 receptor antagonist.Target: neuropeptide Y receptorVelneperit (S-2367) is a once-daily, oral, centrally acting, small molecule neuropeptide Y (NPY) Y5 receptor antagonist.
Santin is a flavonol isolated from Dodonaea uscosa[1].
5,8,11-Eicosatriynoic acid (ETI) is a lipoxygenase inhibitor that blocks LTC4 biosynthesis in mast cell tumor cells[1].
Raltitrexed is an antimetabolite drug used in chemotherapy, acting by inhibiting thymidylate synthase.
(S)-3-Benzyloxycarbonylamino-2-(Boc-amino)propionic acid is an alanine derivative[1].
TTP-8307 is a potent inhibitor of the replication of several Rhinoviruses and Enteroviruses, targets the nonstructural protein 3A, inhibits the replication of coxsackievirus B3 (CVB3 Nancy) with EC50 of 1.2 uM; 3A mutations V45A, I54F, and H57Y confer resistance to TTP-8307.
Sauristolactam, a natural aristolactam isolated from aerial portions of Saururus chinensis, has significant neuroprotective activity against glutamate-induced toxicity in primary cultured rat cortical cells[1]. Sauristolactam also inhibits the receptor activator of nuclear factor-κB ligand (RANKL)-induced osteoclastogenesis and has the potential to inhibit osteoclast differentiation[2].
5-Aminouridine can modify nucleobases and can be incorporated into the target DNA. 5-Aminouridine exhibits a wide range of biological activity and it inhibits the growth of tumors, fungi and viruses[1][2][3].
3-Azidopropylamine is a click chemistry reagent containing an azide group. 3-Azidopropylamine can react with the starch sugar of potato starch for complexation and transfection of plasmid DNA[1].
2-Phenethyl β-primeveroside is a phenplic that can be isolated from Callianthemum taipaicum[1].
Memantine-d6 hydrochloride is the deuterium labeled Memantine hydrochloride. Memantine (hydrochloride) (D-145 (hydrochloride)) is a moderate affinity, uncompetitive NMDA receptor antagonist, inhibit CYP2B6 and CYP2D6 with Ki of 0.51 nM and 94.9 μM, respectively[1].
FFA3 agonist 1 (Compound 24) is an agonist of free fatty acid receptor 3 (FFA3). FFA3 agonist 1 regulates the health effect of intestinal microbiota by activating FFA3[1].
Quinacrine mustard dihydrochloride is a fluorochrome. Quinacrine mustard dihydrochloride as a polycyclic aromatic agent can be used as mutagenic agent induces the mutants of bacteria. Quinacrine mustard dihydrochloride induces cell cycle arrest at G2/M-phase. Quinacrine mustard dihydrochloride has the potential for the research of plant, animal, or human chromosomes[1][2][3].
HIV-IN-1 (Compound 50) is a potent inhibitor of HIV. HIV-IN-2 has the potential for the research of HIV infection[1].
NCC-149 is a selective HDAC8 inhibitor and can be used for neural differentiation research[1].
Quarfloxin (CX 3543), a fluoroquinolone derivative with antineoplastic activity, targets and inhibits RNA pol I activity, with IC50 values in the nanomolar range in neuroblastoma cells. Quarfloxin disrupts the interaction between the nucleolin protein and a G-quadruplex DNA structure in the ribosomal DNA (rDNA) template[1].
Alclometasone (7a-Chloro-16a-methyl prednisolone) is a glucocorticoid and inhibits the release of pro-inflammatory mediators from leukocytes. Alclometasone can be used to relieve corticosteroid-responsive dermatoses, including atopic dermatitis, eczema, psoriasis and allergic dermatitis[1].
Xanthine oxidoreductase-IN-3 is an orally active xanthine oxidoreductase (XOR) inhibitor, with an IC50 of 26.3 nM. Xanthine oxidoreductase-IN-3 can be used for the research of acute hyperuricemia[1].
Azidoethyl-SS-PEG2-Boc is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
Mogroside I E1, a triterpenoid glycoside isolated from the extracts of Luo Han Guo, is a nonsugar sweetener. Mogrosides are sweeter than sucrose. Mogrosides exhibit antioxidant, antidiabetic and anticancer activities[1].
TP-030-2 is a RIPK1 inhibitor (human Ki=0.43 nM; mouse IC50=100 nM)[1][2].