Doravirine is a novel non-nucleoside inhibitor of HIV-1 reverse transcriptase with potent activity against wild-type virus (95% inhibitory concentration 19 nM, 50% human serum). target:HIV [1]In vitro: Doravirine exhibits potent antiviral activity against wild-type virus and K103N, Y181C, and K103N/Y181C mutant viruses, with IC50 value of 12, 21, 31, and 33 nM, respectively. [1] MK-1439 exhibited similar antiviral activities against 10 different HIV-1 subtype viruses (a total of 93 viruses).[2]In vivo: Administration of 50 mg doravirine with a high-fat meal is associated with slight elevations in AUC time zero to infinity (AUC0-∞) and C24 h with no change in Cmax. Midazolam AUC0-∞ is slightly reduced by coadministration of doravirine (geometric mean ratio 0.82, 90% CI 0.70, 0.97). [3]
Elastase LasB-IN-1 (Compound 4b) has antibacterial activity. Elastase LasB-IN-1 (Compound 4b) is a selective elastase LasB inhibitor with an IC50 value of 76 nM[1].
1-O-Gentiobiosyl-3,7-dimethoxy-8-hydroxyxanthone (Compound 18) is a natural product that can be isolated from Swertia mussotii[1].
Dynorphin (2-17), amide (porcine) is a dynorphin derivative with some analgesic effects. Dynorphin is a class of opioid peptides produced by the precursor protein dynorphinogen and is involved in pain, addiction and mood regulation[1].
Biotin-TAT (47-57), biotin tagged TAT, is a transactivator of transcription. Biotin-TAT (47-57) is one of the most widely used PTDs into different primary cells is ATP- and temperature-dependent, indicating the involvement of endocytosis[1][2].
Lisinopril is angiotensin-converting enzyme inhibitor, used in treatment of hypertension, congestive heart failure, and heart attacks.Target: ACELisinopril is a potent, competitive inhibitor of angiotensin-converting enzyme (ACE), the enzyme responsible for the conversion of angiotensin I (ATI) to angiotensin II (ATII). ATII regulates blood pressure and is a key component of the renin-angiotensin-aldosterone system (RAAS). Lisinopril may be used to treat hypertension and symptomatic congestive heart failure, to improve survival in certain individuals following myocardial infarction, and to prevent progression of renal disease in hypertensive patients with diabetes mellitus and microalbuminuria or overt nephropathy [1, 2].
3-Butylidenephthalide (Butylidenephthalide) is a phthalic anhydride derivative identified in Ligusticum chuanxiong Hort, and has larvicidal activity (LC50 of 1.56 mg/g for Spodoptera litura larvae)[1].
PA452, retinoic X receptor (RXR) specific antagonist, inhibits the effect of Retinoic acid (RA) on Th1/Th2 development[1].
α-Helical Corticotropin Releasing Factor (9-41) is a corticotropin releasing factor (CRF) antagonist. α-Helical Corticotropin Releasing Factor (9-41) decreases plasma growth hormone (GH) values in vivo[1][2].
Odoratisol B is a natural product that can be isolated from Machilus odoratissima NEES[1].
Decoglurant (RO4995819) is a negative allosteric modulator of mGluR2 and mGluR3. Decoglurant is developed as an antidepressant[1].
GHRF, mouse, a mouse growth hormone-releasing factor, is a peptide containing 44 amino acids. GHRF, mouse stimulates the release and synthesis of growth hormone[1].
MC-AlkyMC-Alkyl-Hydrazine is a noncleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].
Boc-D-Tyr-OH is a tyrosine derivative[1].
(Rac)-Nutlin-3 (Rebemadlin), an active enantiomer of Nutlin-3, is a potent murine double minute (MDM2) inhibitor (IC50=90 nM). (Rac)-Nutlin-3 inhibits MDM2-p53 interactions and stabilizes the p53 protein, and induces cell autophagy and apoptosis. (Rac)-Nutlin-3 has the potential for the study of TP53 wild-type ovarian carcinomas[1][2].
Bezafibrate is an agonist of PPAR, with EC50s of 50 μM, 60 μM, 20 μM for human PPARα, PPARγ and PPARδ, and 90 μM, 55 μM, 110 μM for murine PPARα, PPARγ and PPARδ, respectively; Bezafibrate is used as an hypolipidemic agent.
Olmesartan ethyl ester (compound 11) is an Olmesartan impurity. Olmesartan (RNH-6270) is an angiotensin II receptor (AT1R) antagonist used to in the high blood pressure study[1].
Lu AF27139 is a novel rodent-active and CNS-penetrant P2X7 receptor antagonist. Lu AF27139 is highly selective and potent against rat, mouse, and human forms of the receptors. The rat pharmacokinetic profile is favorable with high oral bioavailability, modest clearance (0.79 L/(h kg)), and good CNS permeability. Importantly, Lu AF27139 was without effect in standard in vitro and in vivo toxicity studies. Lu AF27139 is a valuable tool for probing the role of the P2X7 receptor in rodent models of CNS diseases.
BMS-345541 is a selective inhibitor of the catalytic subunits of IKK (IKK-2 IC50=0.3 μM, IKK-1 IC50=4 μM). BMS-345541 binds at an allosteric site of IKK.
ABMA is a novel broad-spectrum inhibitor of intracellular toxins and pathogens, efficiently protects cells against various toxins and pathogens including viruses, intracellular bacteria and parasite; protects mice from nasal instillation of an LD90 of ricin; provokes Rab7-positive late endosomal compartment accumulation in mammalian cells without affecting other organelles.
Lamivudine (BCH-189) salicylate is an orally active nucleoside reverse transcriptase inhibitor (NRTI). Lamivudine salicylate can inhibit HIV reverse transcriptase 1/2 and also the reverse transcriptase of hepatitis B virus. Lamivudine salicylate can penetrate the CNS[1][2].
(Z)-Hexadec-9-enoic acid, a composition of fatty acid, is implicated in the prevention of death from cerebrovascular disorders in SHRSP rats.
BIBR 1087 SE is an intermediate metabolite of dabigatran etexilate.
Sulfameter-d4 (Sulfametoxydiazine-d4; 5-Methoxysulfadiazine-d4)is the deuterium labeledSulfameter(HY-B0213)[1]. Sulfameter (Sulfametoxydiazine; 5-Methoxysulfadiazine) is an effective long-acting sulfonamide antibiotic with antibacterial activities. Sulfameter can be used for the research of urinary tract infections and lepriasis[2].
MoTP is a specific platelet activating factor receptor antagonist and can induce melanocyte ablation. MoTP can be used for the research of cancer.
Sulfinalol is an orally active β-adrenoceptor antagonist with direct vasodilator activity[1].
Regaloside B is a phenylpropanoid isolated from Lilium longiflorum. Regaloside B can inhibit the expression of iNOS and COX-2, has anti-inflammatory activity[1][2].
7-Methylguanine is a metabolite of DNA methylation. It can be generated by methylating agents, and used as a probe of protein–DNA interactions and a key component of DNA sequencing method.
Raloxifene-d10-1 is the deuterium labeled Raloxifene[1]. Raloxifene (Keoxifene) is a benzothiophene-derived selective estrogen receptor modulator (SERM). Raloxifene has estrogen-agonistic effects on bone and lipids and estrogen-antagonistic effects on the breast and uterus. Raloxifene is used for breast cancer and osteoporosis research[2].
Potassium tert-butyl malonate is an intermediate in the synthesis of malonate monoester potassium salt[1].