3’-Deoxy-3’-α-C-methyl-5-fluorouridine is a purine nucleoside analogue. Purine nucleoside analogs have broad antitumor activity targeting indolent lymphoid malignancies. Anticancer mechanisms in this process rely on inhibition of DNA synthesis, induction of apoptosis, etc[1].
Syk-IN-3, a potent spleen tyrosine kinase (Syk) inhibitor, extracted from patent WO2011075515A1, compound example 152, has an IC50 of 1 nM[1].
Spiradine F is a main alkaloidal component of spiraea japonioa L. fil. Spiradine F derivative can inhibit platelet-activating factor (PAF)-induced platelet aggregation[1][2].
Disodium phosphate is also known as Na2HPO4 to adjust pH of liquid. Disodium phosphate can be used as an excipient, such as buffer, chelating agent. 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][2].
Xanthurenic acid is a putative endogenous Group II metabotropic glutamate receptor agonist, on sensory transmission in the thalamus.
CVT-12012 is a potent and orally bioavailable stearoyl-coA desaturase (SCD) inhibitor, with IC50s of 38 nM, 6.1 nM for rat microsomal and human HEPG2, respectively.
C8 Dihydroceramide is a negative control of C8 Ceramide. C8-Ceramide (N-Octanoyl-D-erythro-sphingosine) is a cell-permeable analog of naturally occurring ceramides. C8-Ceramide has anti-proliferation properties and acts as a potent chemotherapeutic agent. C8-Ceramide stimulates dendritic cells to promote T cell responses upon virus infections. C8-Ceramide induces slight activation of protein kinase (PKC) in vitro[1][2][3][4].
AS19 is a potent, selective 5-HT7 receptor agonist with an IC50 value of 0.83 nM and a Ki of 0.6 nM. AS19 is selective for 5-HT7 over 5-HT1A, 5-HT1B, 5-HT1D, and 5-HT5A receptors (Kis = 89.7 nM, 490 nM, 6.6 nM and 98.5 nM, respectively). AS19 enhances memory consolidation and reverses Scopolamine- or Dizocilpine-induced amnesia[1][2][3].
N-(2,4-Dinitrophenyl)-L-leucine is a leucine derivative[1].
Methsuximide is an anticonvulsant agent. Methsuximide is effective in petit mal, psychomotor and focal motor attacks[1].
2’,3’-Bis(O-(t-butyldimethylsilyl)-5-methoxyuridine is a purine nucleoside analog. Purine nucleoside analogs have broad antitumor activity targeting indolent lymphoid malignancies. Anticancer mechanisms in this process rely on inhibition of DNA synthesis, induction of apoptosis, etc[1].
Parthenosin (Quercetin 3-O-β-D-glucuronide butyl ester) is a flavonoid, that can be isolated from the aerial parts of Calligoum polygonoides. Parthenosin shows cytotoxic activity against HepG2 and MCF-7 cell lines with IC50 values of 60.46 and 61.4 μg/mL, respectively[1].
Odiparcil (SB-424323) is an orally active beta-d-thioxyloside analog with antithrombotic activity associated with a reduced risk of adverse bleeding events. Odiparcil (SB-424323) is indirect thrombin inhibitor that exerts its anticoagulant effect through activation of antithrombin II (heparin cofactor II) [1][2].
Basiliximab (CHI 621) is a recombinant chimeric murine/human IgG1 monoclonal anti-interleukin-2 receptor antibody. Basiliximab can be used for the research of renal transplantation[1].
1-Nitropyrene-d9 is the deuterium labeled 1-Nitropyrene[1].
Losartan-d2 is the deuterium labeled Losartan[1]. Losartan is an angiotensin II receptor antagonist, competing with the binding of angiotensin II to AT1 receptors with IC50 of 20 nM[2].
Nuclear Fast Red, an anthraquinone dye, is commonly used in conjunction with an excess of aluminum ions as a red nuclear counterstain. Nuclear fast red has been used as a histochemical and colorimetric reagent for calcium[1]. Nuclear fast red as highly sensitive "off/on" fluorescent probe for detecting guanine[2].
Iinerixibat (GSK2330672) is a highly potent, nonabsorbable ASBT(apical sodium-dependent bile acid transporter) inhibitor (hASBT IC50=42 ± 3 nM) which lowers glucose in an animal model of type 2 diabetes and shows excellent developability properties for evaluating the potential therapeutic utility of a nonabsorbable ASBT inhibitor for treatment of patients with type 2 diabetes.
IRS1-derived peptide is a biological active peptide. (This is a peptide fragment (979-989) of the insulin receptor substrate-1 containing the sequence motif YMXM known to bind to the two domains of SH2 on the 85kDa subunit of phosphoinositide 3-kinase.)
Mogrol is a biometabolite of mogrosides, and acts via inhibition of the ERK1/2 and STAT3 pathways, or reducing CREB activation and activating AMPK signaling.
Masitinib mesylate is a novel inhibitor for Kit and PDGFRα/β with IC50 of 200 nM and 540 nM/800 nM, and has weak inhibition to ABL and c-Fms.
N-Methylpiperazine-d11 is the deuterium labeled N-Methylpiperazine[1].
PDE5-IN-7 (compound 8) is a selective phosphodiesterase 5 (PDE 5) inhibitor with an IC50 value of 5 nM, while an IC50 of 300 nM for PDE 1[1].
Glycine Sulfate is a Glycine (HY-Y0966) derivative[1].
Bensulfuron-methyl-d6 is a deuterated Bensulfuron-methyl (HY-B0870) (sulfonylurea pesticides). Bensulfuron-methyl-d6 can be used as an internal standard for the determination of pesticide residues by LC-MS[1].
BIX-01338 hydrate is a histone lysine methyltransferase inhibitor.
TMP920 is a highly potent and selective RORγt antagonist. TMP920 inhibits RORγt binding to the SRC1 peptide with an IC50 of 0.03 μM[1].
Epicoccone B, firstly reported from C. globosum, exhibits the DPPH free radical scavenging ability with IC50 value of 10.8 μM, and has potent α-glucosidase inhibition with IC50 value of 27.3 μM. Anti-HIV activity[1][2].
Glycyuralin E is a natural product that can be isolated from Glycyrrhiza uralensis[1].
Oleoyl-D-lysine is a selective Glycine Transporter-2 (GlyT2) inhibitor based on lipid. Oleoyl-D-lysine reverses neuropathic pain in mice, shows antidrowsiness effect on chronic neuropathic pain. Oleoyl-D-lysine is safe and effective without respiratory depression[1].