Tacrine is a potent acetylcholinesterse (AChE) inhibitor (IC50=109 nM), also acting as a CYP1A2 substrate drug. Tacrine exhibits certain hepatotoxicity in some individuals. Tacrine can be used for researching Alzheimer's disease (AD)[1][2][3].
S-30-Hydroxygambogic acid is polyprenylated xanthone epimer that can be isolated from gamboges of Garcinia hanburyi. S-30-Hydroxygambogic acid shows cytotoxicities to Human Leukemia K562 cell lines of IC50 values of 4.49 and 3.61 μM for K562/R and K562/S, respectively. S-30-Hydroxygambogic acid can be used for the research of cancer[1].
Disopyramide (Dicorantil) is a class IA antiarrhythmic drug with efficacy in ventricular and atrial arrhythmias. Disopyramide blocks the fast inward sodium current of cardiac muscle and prolongs the duration of cardiac action potentials. Disopyramide inhibits HERG encoded potassium channels. Disopyramide also exhibits complex protein binding, and has a potent negative inotropic action[1][2][3].
Lathyrol is a natural product, and is used for cancer treatment.
Cefditoren pivoxil is a new-third generation cephalosporin antibiotic that has a broad spectrum of activity against Gram-positive and Gram-negative bacteria, including common respiratory and skin pathogens.Target: AntibacterialCefditoren pivoxil, a new-third generation cephalosporin antibiotic that has recently been granted approval in Spain, shows important activity over a large part of the pathogens causing skin, soft tissue and respiratory tract infections, including Gram-negative and Gram-positive bacteria. Cefditoren is also marketed under the name Meiact. Cefditoren has a broad spectrum of activity and has been used to treat bacterial infections of the skin and respiratory tract including bronchitis, pneumonia, and tonsillitis. The following represents MIC susceptibility data for a few medically significant microorganisms.Cefditoren has shown excellent in vitro activity against the Gram-positive pathogens penicillin-susceptible and -intermediate Streptococcus pneumoniae, S. pyogenes and methicillin-susceptible Staphylococcus aureus. Cefditoren was inactive against methicillin-resistant S. aureus. Of the important Gram-negative pathogens, cefditoren had potent antibacterial effects against beta-lactamase-positive and -negative Haemophilus influenzae, H. parainfluenzae and beta-lactamase-positive and -negative Moraxella catarrhalis.
VU0080241 is a positive allosteric modulator (PAM) of the metabotropic glutamate receptor subtype 4 (mGluR4), with an EC50 of 4.6 μM[1].
Stepharine, an natural alkaloid, directly interactes with TLR4 and binds to the TLR4/MD2 complex (TLR4 inhibitor). Stepharine possesses anti-aging, anti-viral and anti-hypertensive effects[1].
CXCR4 antagonist 7 (Compound PARA-B) is a CXCR4 antagonist with the IC50 of 9.3 nM. CXCR4 antagonist 7 can be used for the research of HIV infection, inflammatory diseases, cancer, and WHIM syndrome[1].
Fedovapagon is a selective vasopressin V2 receptor (V2R) agonist with an EC50 of 24 nM, which is being developed for the treatment of nocturia[1].
BI-1950 is a potent, selective LFA-1 antagonist that inhibits the binding of LFA-1 to ICAM-1 with Kd value of 9 nM; displays >1,000 fold selectivity against the most closely related b2-integrin Mac-1 and b1-integrin function; inhibits the production of IL-2 in human PBMC and whole blood with IC50 value of 3 nM and 120 nM, respectively; exhibits an attractive DMPK profile, BI-1950 is a excellent molecule for testing pharmacological hypotheses in vitro and in vivo.
alpha-Man-TEG-N3 is a click chemistry reagent containing an azide group[1].
Spisulosine (ES-285) is an antiproliferative (antitumoral) compound of marine origin. Spisulosine inhibits the growth of the prostate PC-3 and LNCaP cells through intracellular ceramide accumulation and PKCζ activation[1].
Gumokimab (AK 111) is a monoclonal antibody targeting IL-17A, which can be used in the study of psoriasis, ankylosing spondylitis. Gumokimab competitively blocks the binding of human IL-17A to IL-17R.
Boc-D-Pen(Mob)-OH is a phenylalanine derivative[1].
Thymosin β10Arg is a thymosin β4-like peptide that contains an additional amino acid, arginine, inserted following lysine-38[1].
Eleutheroside E, a principal component of Eleutherococcus enticosus, has anti-inflammatory and protective effects in ischemia heart. IC50 value:Target:In vitro: Treatment of 10 μM Eleutheroside E (EE) for 24 h increased basal glucose uptake as well as improved TNF-α-mediated suppression of glucose uptake. [2]In vivo: To investigate the effect of Eleutheroside E (EE) on arthritis, the CIA model in DBA/1 mice was used. Compared to vehicle-treated CIA mice, 15 mg/kg TG treatment and 30 and 60 mg/kg EE treatment obviously decreased the arthritis scores and body weight loss in CIA mice (P<0.01) [1].
[Tyr12] Somatostatin 28 (1-14) is an analogue of Somatostatin-28 (1-14) (HY-P1499). Somatostatin-28 (1-14) is an N-terminal fragment of the neuropeptide somatostatin-28[1].
Stauprimide is a staurosporine analog that promotes embryonic stem cell (ESC) differentiation. Stauprimide is a non-broad spectrum inhibitor that binds to the MYC transcription factor NME2 and blocks its nuclear localization in ESCs, which results in down-regulation of MYC transcription[1].
ARQ 531 is a reversible non-covalent inhibitor of Bruton’s Tyrosine Kinase (BTK), with IC50s of 0.85 nM and 0.39 nM for WT-BTK and C481S-BTK, respectively.
SNIPER(BRD)-1, consists of an IAP antagonist LCL-161 derivative and a BET inhibitor, (+)-JQ-1, connected by a linker. SNIPER(BRD)-1 induces the degradation of BRD4 via the ubiquitin-proteasome pathway. SNIPER(BRD)-1 also degrades cIAP1 , cIAP2 and XIAP with IC50s of 6.8 nM, 17 nM, and 49nM, respectively[1].
5,6-Didehydroginsenoside Rd is a dammarane-type saponin isolated from the dried roots of Panax notoginseng[1].
Daltroban (BM-13505) is a selective and specific thromboxane A2 (TXA2) receptor antagonist. Daltroban increase intracellular calcium in vascular smooth muscle cells. Daltroban shows protective effect in reperfusion injury[1][2].
TC-N 1752 is a potent and orally active inhibitor of Nav1.7, with IC50s of 0.17 μM, 0.3 μM, 0.4 μM, 1.1 μM and 2.2 μM at hNav1.7, hNav1.3, hNav1.4, hNaV1.5 and rNav1.8, respectively. TC-N 1752 also inhibits tetrodotoxin-sensitive sodium channels. TC-N 1752 shows analgesic efficacy in the Formalin model of pain[1][2][3].
L-Methionine hydrochloride is a Methionine (HY-13694) derivative[1].
NLRP3-IN-2, an intermediate substrate in the synthesis of glyburide, inhibits the formation of the NLRP3 inflammasome in cardiomyocytes and limits the infarct size following myocardial ischemia/reperfusion in the mouse, without affecting glucose metabolism[1].
Ustusolate C is a drimane sesquiterpene that can be isolated from Aspergillus ustus 094102. Ustusolate C exhibits moderate cytotoxicity against A549 cells with an IC50 of 10.5 μM[1].
G-418 (disulfate) is an aminoglycoside antibiotic similar in structure to gentamicin B1, which blocks polypeptide synthesis by inhibiting the elongation step in both prokaryotic and eukaryotic cells.
Riociguat-d6 (BAY 632521-d6) is the deuterium labeled Riociguat. Riociguat is an oral stimulator of soluble guanylate cyclase (sGC) used in the treatment of pulmonary hypertension[1][2].
(((9H-Fluoren-9-yl)methoxy)carbonyl)-D-threonine is a threonine derivative[1].
Bevemipretide is a biodegradable silica hydrogel composite. Bevemipretide can be used for ocular indication[1].