L-Arginine-13C6,15N4 ((S)-(+)-Arginine-13C6,15N4) hydrochloride is the 13C- and 15N-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.
Lercanidipine-d3 hydrochloride is the deuterium labeled Lercanidipine. Lercanidipine is a lipophilic third-generation dihydropyridine-calcium channel blocker (DHP-CCB). Lercanidipine has long lasting antihypertensive action and reno-protective effect[1][2][3].
Lp-PLA2-IN-6 (compound 18), a tetracyclic pyrimidinone compound, is a potent Lp-PLA2 inhibitor with a pIC50 of 10.0 for rhLp-PLA2. Lp-PLA2-IN-6 has the potential for neurodegenerative related diseases research[1].
VPLSLYSG is an octapeptide that can be degraded by matrix metalloproteinase-9 (MMP-9), MMP-1 and MMP-2. VPLSLYSG has potential applications in MMP substrates[1][2][3].
Epigomisin O is isolate from the fruits of Schisandra plants[1].
Zolimomab aritox (H65-RTA) is an immunocoupling compound consisting of a ricin (RTA) chain, a ribosomal inhibitory protein, coupled to a monoclonal antibody (H65) against the pan-T-cell antigen CD5. Zolimomab aritox has anticancer activity and can be used in cutaneous T-cell lymphoma studies[1].
Prohexadione (BX-112 free acid) is a plant growth regulator. Prohexadione inhibits gibberellin biosynthesis of plants[1][2].
Cytidoline sodium salt is an intermediate in the synthesis of phosphatidylcholine which is a component of cell membranes and also exerts neuroprotective effects.
KW-8232, an orally active anti-osteoporotic agent, and can reduces the biosynthesis of PGE2[1].
Hydrazine-d6 (sulfate) is the deuterium labeled Hydrazine sulfate[1].
Dehydroeburicoic acid monoacetate (Compound 18) is a lanostane triterpenoid isolated from Wolfiporia cocos[1].
h-NTPDase8-IN-1 (compound 2d) is a sulfamoyl-benzamides based and selective inhibitor for h-NTPDases8 (IC50=0.28 μM). h-NTPDases8 is involved in a variety of physiological and pathological functions，such as thrombosis，diabetes，inflammation，and cancer[1].
AQ-13 dihydrochloride is an aminoquinoline antimalarial drug that is effective against chloroquine-resistant strains of Plasmodium falciparum.
Bromo-PEG6-alcohol is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
XT-2 peptide is an antimicrobial peptide derived from skin secretions of Xenopus tropicalis. XT-2 peptide has strong activity against E.coli, the vaule of MIC is 8 μM[1].
CB2 receptor agonist 3 is a robust and selective CB2 cannabinoid agonist with Kis of 7.6 and 900 nM for CB2 and CB1, respectively. CB2 receptor agonist 3 significantly increases P-ERK 1/2 expression in HL-60 cells[1].
Swietemahalactone is a natural compound isolated from Swietenia mahagoni. Swietemahalactone exhibits antibacterial activity aganist E. coli[1].
(1R)-IDH889 is the inactive isomer of IDH889 (HY-112289), and can be used as an experimental control. IDH889 is an orally available, brain penetrant, allosteric and mutant specific inhibitor of isocitrate dehydrogenase 1 (IDH1). IDH889 has potent selectivity for IDH1 R132* mutations, with IC50s of 0.02 μM, 0.072 μM and 1.38 μM for IDH1R132H, IDH1R132C and IDH1wt, respectively. IDH889 shows potent cellular inhibition of R-2-hydroxyglutarate (2-HG) production with an IC50 of 0.014 μM[1].
(±)-Vasicine is the racemate of Vasicine. Vasicine (Peganine), isolated from Peganum harmala seeds, significantly inhibits H+-K+-ATPase activity in vitro with an IC50 of 73.47 μg/mL. Anti-ulcer activity. Vasicine shows significant anti-secretory, antioxidant and cytoprotective effect[1].
Lomitapide-d8 is deuterium labeled Lomitapide. Lomitapide (AEGR-733; BMS-201038) is a potent inhibitor of microsomal triglyceride-transfer protein (MTP) with an IC50 of 8 nM in vitro.
Lipoamido-PEG3-OH is a PEG-based PROTAC linker can be used in the synthesis of PROTACs. Lipoamido-PEG3-OH (compound TA-TEG-G2CN) can be used in the formation of a highly stable, dendronized gold nanoparticle (AuNP)-based drug delivery platform[1].
GSK1838705A is a potent and reversible IGF-IR and the insulin receptor inhibitor with IC50s of 2.0 and 1.6 nM, respectively. It also inhibits ALK with an IC50 of 0.5 nM.
2-Selenouracil is a useful specialized photosensitizer for photodynamical therapy[1].
Tetra-N-acetylchitotetraose elicits plant defense systems. Tetra-N-acetylchitotetraose is a component of the hpo-chitoo gosacchaπdes (LCOs) secreted from Rhizobia. Tetra-N-acetylchitotetraose is also a substrate for the Rhizobium leguminosarum nodulation protein NodB, a CO deacetylase[1].
Xanthiazone is a thiazinedione[1].
Bicyclomycin benzoate is an antibiotic exhibiting activity against a broad spectrum of Gram-negative bacteria and against the Gram-positive bacterium.
2-Desoxy-4-epi-pulchellin (compound 13) is a compound isolated from dichloromethane-soluble portion of Polygonum hydropiper[1].
PRMT5-IN-29 is a potent and orally active PRMT5 Inhibitor with an IC50 of 1.5 μΜ. PRMT5-IN-29 has the potential for advanced cancers research[1].
(R)-Etodolac-d4 is the deuterium labeled (R)-Etodolac[1].
Saxagliptin H2O(BMS477118 H2O) is a selective and reversible DPP4 inhibitor with IC50 of 26 nM and Ki of 1.3 nM.IC50 value: 26 nM [1]Target: DPP4in vitro: Saxagliptin has an inhibition constant Ki of 1.3 nM for DPP4 inhibition, which is 10-fold more potent than either vildagliptin or sitagliptin (another two DPP4 inhibitors) with Ki of 13 and 18 nM. In addition, Saxagliptin demonstrates greater specificity for DPP4 than for either the DPP8 or DPP9 enzymes (400- and 75- fold, respectively). The active metablite of saxagliptin is two-fold less potent than the parent. Both Saxagliptin and its metabolite are highly selective (>4000-fold) for the prevention of DPP4 compared with a range of other proteases (selectivity of sitagliptin and vildagliptin for DPP4 is >2600 and <250-fold, respectively, compared with DPP8 and DPP9) [2]. Saxagliptin reduces the degradation of the incretin hormone glucagon-like peptide-1, thereby enhancing its actions, and is associated with improved β-cell function and suppression of glucagon secretion.in vivo: Saxagliptin is highly effective at eliciting marked dose-dependent enhancements in glucose clearance in the dose range 0.13-1.3 mg/kg in ob/ob mice relative to controls. Saxagliptin dose-dependently elevate plasma insulin significantly at 15 min post-oGTT, with concomitant improvement in the glucose clearance curves at 60 min post-oGTT [4].