Sarcosine is a glycine transporter type 1 (GlyT) inhibitor and an N-methyl-D-aspartate (NMDA) receptor co-agonist at the glycine binding site.
BLT-1, a thiosemicarbazone copper chelator, is a selectively scavenger receptor B, type 1 (SR-BI) inhibitor. BLT-1 inhibits the transfer of lipids between high-density lipoproteins (HDL) and cells mediated by SR-BI. BLT-1 has pro-inflammatory functions through neutrophil recruitment[1][2][3].
D-Heptamannuronic acid, an alginate oligomer, is produced by marine brown algae and by a limited range of Gram negative bacteria. D-Heptamannuronic acid can be used for the research of pain and vascular dementia[1][2][3][4].
Propylparaben sodium is an antimicrobial agent, preservative, flavouring agent[1].
GW 4064 is a potent FXR agonist with EC50 of 65 nM.
AZD9496 is a potent and selective estrogen receptor (ERα) antagonist with an IC50 of 0.28 nM.
GRGDSP, a synthetic linear RGD peptide, is an integrin inhibitor.
DHAPC is a phospholipid that is very sensitive to oxidation[1].
Calcitriol is the most active metabolite of vitamin D and also a vitamin D receptor (VDR) agonist.
DIPPA (hydrochloride) is an irreversible, long-lasting, selective and high affinity κ-opioid receptor antagonist. DIPPA (hydrochloride) can be used for the research of anxiety and antidepressant[1][2][3][4].
DMAPT (Dimethylamino Parthenolide), a water soluble analogue of Parthenolide (PTL), is an oral active NF-κB inhibitor, with a LD50 of 1.7 μM for cell population in AML cells. Has potential anti-cancer and anti-metastatic effect[1].
BIBS 39 is a new nonpeptide angiotensin II (AII) receptor antagonist.Target: Angiotensin Receptorin vitro: BIBS 39 displaces [125I] AII from its specific binding sites with a Ki value of 29 ± 7 nM for the AII subtype 1 (AT1) receptor and a Ki value of 480 ± 110 nM for the AII subtype 2 (AT2) receptor. BIBS 222 shows a Ki value of 20 ± 7 nM for the AT1 subtype and a Ki value of 730 ± 170 nM for the AT2 subtype. BIBS 39 is 17 times more selective for the AT1 subtype and BIBS 222 37 times. BIBS 39 shifts the AII concentration-contractile response curves in isolated rabbit aorta to the right in a parallel fashion. [1]in vivo: In pithed rats, BIBS 39 dependently shifts the dose-response curve of AII to the right without affecting the maximal response. BIBS 222 also causes parallel shifts to the right but a significant reduction of the maximal responses was observed at 3 and 10 mg/kg i.v. These results show that the benzimidazole derivatives BIBS 39 is a potent and selective AII receptor antagonists. Substitution with a benzimidazole moiety results into a considerable loss of selectivity for the AT1 receptor subtype compared with an imidazole moiety as, for instance, in DuP 753.[1] BIBS 39 is a new nonpeptide angiotensin receptor blockers that has affinity for both AT1- and AT2-receptors, is also a potent antagonist of the cardiovascular effects of AII in pithed rabbits. [2]
BV02 is a potent 4-3-3 PPI (14-3-3 protein–protein interaction) inhibitor. BV02 shows cytotoxicity for hematopoietic cells expressing the IM (imatinib mesylate)-sensitive wild type Bcr-Abl and the IM-resistant T315I mutation. BV02 has the potential for the research of chronic myeloid leukemia[1][2].
Protoapigenin is a flavonoid, that can be isolated from the aerial parts of Macrothelypteris torresiana[1].
Setogepram (PBI-4050) acts as an orally active agonist for GPR40 and as an antagonist or inverse agonist for GPR84[1]. Setogepram (PBI-4050) decreases renal, liver and pancreatic fibrosis[1][2]. Setogepram (PBI-4050) exerts anti-fibrotic, anti-inflammatory and anti-proliferative actions[2].
AZD4635 is a novel adenosine 2A receptor (A2AR) inhibitor with a Ki of 1.7 nM.
Dibutepinephrine is a sympathomimetic molecular[1].
(R)-TTBK1-IN-1 is a potent, selective and brain-penetrant tau tubulin kinase 1 (TTBK1) inhibitor. (R)-TTBK1-IN-1 is an enantiomer of TTBK1-IN-1 (HY-134968). (R)-TTBK1-IN-1 can be used in the research of alzheimer’s disease and related tauopathies[1].
4-(Dodecylamino)phenol (p-DDAP) is an anticancer agent. 4-(Dodecylamino)phenol has anti-tumor activity and can suppress proliferation, arrest the cell cycle and induce apoptotic cell death. 4-(Dodecylamino)phenol can be used for the research of cancer, such as prostate cancer[1][2].
Meropenem is a carbapenem antibiotic, which displaying a broad spectrum of antibacterial activity.Target: AntibacterialMeropenem, a new parenteral carbapenem demonstrated increased activity as compared to imipenem against 336 strains of Neisseria gonorrhoeae, 119 strains of Haemophilus influenzae, and 110 strains of H. Ceftriaxone and ciprofloxacin demonstrated activity superior to that of both carbapenems while the activity of ceftazidime was similar to that of meropenem [1]. Meropenem, like imipenem and various experimental penems, may overcome the resistance problems presented by Class I beta-lactamases [2]. MEROPENEM was rapidly penetrated to the pleural effusion and was retained for a more prolonged time in the pleural effusion than in the blood of patients with accumulated pleural effusion, and it suggested the usefulness of MEROPENEM in antibacterial therapy for patients with pleurisy causing accumulation of pleural effusion [3].Clinical indications: Appendicitis; Bacterial infection; Bacterial meningitis; Bacterial pneumonia; Bacterial respiratory tract infection; Bacterial skin infection; Bacterial urinary tract infection; Bacteroides fragilis infection; Bacteroides infection; Bacteroides thetaiotaomicron infection; Complicated skin and skin structure infectionFDA Approved Date: July 1996Toxicity: In mice and rats, large intravenous doses of meropenem (2200-4000 mg/kg) have been associated with ataxia, dyspnea, convulsions, and mortalities.
Variotin is an Anti-Fungal Agent. Variotin has a strong antibiotic activity on dermatophytes such as Trichophyton, Microsporum, and Epidermophyton, and also pathogenic fungi in internal mycosis such as Blastomyces and Cryptococcus[1].
Pseudoaspidin is isolated from the ferns of the class Pterophyta or Filicinae[1].
GW842166X is a potent and selective cannabinoid receptor 2 (CB2) agonist with IC50 values of 63 and 91 nM for human and rat CB2, respectively.
Fmoc-Asn(Dmcp)-OH is an asparagine derivative[1].
ML335 is a selective activator of both TREK-1 and TREK-2.
Pectolinarin, isolated from Cirsium chanroenicum, possesses anti-inflammatory activity[1]. Pectolinarin inhibits secretion of IL-6 and IL-8, as well as the production of PGE2 and NO. Pectolinarin suppresses cell proliferation and inflammatory response and induces apoptosis via inactivation of the PI3K/Akt pathway[2].
Heptaminol hydrochloride is a vasoconstrictor, used in the treatment of low blood pressure, particularly orthostatic hypotension.in vivo: In the rat, Heptaminol hydrochloride prevents orthostatic hypotension, and increases the noradrenaline plasma concentration. In bovine chromaffin cells maintained in primary cultures, Heptaminol hydrochloride is found to be a competitive inhibitor of noradrenaline uptake.[1]
5-Nitrobarbituric acid is a herpes simplex virus type-1 (HSV-1) inhibitor (IC50=1.7 μM)[1].
Fmoc-NH-PEG6-alcohol is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs). Fmoc-NH-PEG6-alcohol is extracted from patent WO2016030791, example comp 91[1].
Polyoxyl 40 stearate can be used as an excipient. 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].