Phenylglyoxylic acid (sodium) is the sodium salt form of Phenylglyoxylic acid. Phenylglyoxylic acid as a biomarker of exposure to ethylbenzene and styrene (EB/S)[1].
KRas G12C inhibitor 2 is a compound that inhibits KRas G12C, extracted from patent US 20180072723 A1.
ALR-6 is an antagonist of the 5-lipoxygenase (5-LOX) activating protein FLAP and has anti-inflammatory activity. ALR-6 potently inhibits 5-LOX product formation (>80%) in pro-inflammatory M1-MDM and has no significant effect on direct inhibition of 5-LOX[1].
1a,1b-Dihomo prostaglandin E1 (1a,1b-Dihomo PGE1) is a class of prostaglandin compound[1].
Grazoprevir hydrate (MK-5172 hydrate) is a selective inhibitor of Hepatitis C virus NS3/4a protease with broad activity across genotypes and resistant variants, with Kis of 0.01 nM (gt1b), 0.01 nM (gt1a), 0.08 nM (gt2a), 0.15 nM (gt2b), 0.90 nM (gt3a), respectively.
γ-Costic acid (compound 13）is a kind of terpenoid. γ-Costic acid can be obtained by chemical transformation. γ-Costic acid has effective antifeedant and cytotoxic doses with EC50 0.5 μg/ml against L. decemlineata[1].
RP-001 hydrochloride is a picomolar short-acting S1P1 (EDG1) selective agonist, with an EC50 of 9 pM. RP-00 hydrochloride induces internalization and polyubiquitination of S1P1. RP-001 hydrochloride has little activity on S1P2-S1P4 and only moderate affinity for S1P5[1].
NODAGA-tris(t-Bu ester) (NODAG) is a NODAGA derivative. NODAGA-tris(t-Bu ester) can be used to label peptides, antibodies, etc., and subsequently radiolabeled for PET imaging[1].
Aliskiren hemifumarate(CGP 60536) is a direct renin inhibitor with IC50 of 1.5 nM.IC50 value: 1.5 nM [1]Target: reninin vitro: Aliskiren hemifumarate appears to bind to both the hydrophobic S1/S3-binding pocket and to a large, distinct subpocket that extends from the S3-binding site towards the hydrophobic core of renin. Oral bioavailability of Aliskiren hemifumarate is 2.4% in rats, 16% in marmosets and about 2.5% in humans [2].in vivo: Aliskiren hemifumarate (< 10 mg/kg, oral) inhibits plasma renin activity and lowers blood pressure in sodium-depleted marmosets[3].Once-daily oral treatment with Aliskiren hemifumarate lowers blood pressure effectively, with a safety and tolerability profile, in patients with mild-to-moderate hypertension[4].
Flusilazole (DPX-H6573), an organosilane fungicide, has broad-spectrum antifungal effect. Flusilazole exhibits curative and preventative activities and is recommended for use in agriculture and horticulture[1].
Dolutegravir-d6 (S/GSK1349572-d6) is the deuterium labeled Dolutegravir. Dolutegravir (S/GSK1349572) is a highly potent and orally bioavailable HIV integrase strand transfer inhibitor with an IC50 of 2.7 nM for HIV-1 integrase-catalyzed strand transfer. Dolutegravir (S/GSK1349572) inhibits HIV-1 viral replication with an IC50 of 0.51 nM in peripheral blood mononuclear cells. Dolutegravir retains a high potency against the HIV-1 Y143R, N155H, and G140S/Q148H mutants (EC50=3.6-5.8 nM)[1][2][3].
Oxyfenamate has anti-anxiety actions for use in anxiety neuroses.
Mosapride citrate is a gastroprokinetic agent that acts as a selective 5HT4 agonist.Target: 5HT4 Mosapride is a gastroprokinetic agent that acts as a selective 5HT4 agonist. The major active metabolite of mosapride, known as M1, additionally acts as a 5HT3 antagonist, which accelerates gastric emptying throughout the whole of the gastrointestinal tract in humans, and is used for the treatment of gastritis, gastro-oesophageal reflux disease, functional dyspepsia and irritable bowel syndrome. It is recommended to be taken on an empty stomach (i.e. at least one hour before food or two hours after food).In addition to its prokinetic properties, mosapride also exerts anti-inflammatory effects on the gastrointestinal tract which may contribute to some of its therapeutic effects. Mosapride also promotes neurogenesis in the gastrointestinal tract which may prove useful in certain bowel disorders. The neurogenesis is due to mosapride's effect on the 5-HT4 receptor where it acts as an agonist.Its common side effects include dry mouth, abdominal pain, dizziness, headache, insomnia, malaise, nausea, diarrhoea and sometimes constipation. Unlike some other prokinetic agents, mosapride has little effect on potassium channels, no effect on hERG transfected cells, and no effect on cardiovascular function that could be detected in tests on humans. Due to the pharmacokinetics of mosapride, it would take 1,000 - 3,000 times the therapeutic dose to elicit cardiovascular effects.
Fluvoxamine maleate is an antidepressant which functions pharmacologically as a selective serotonin reuptake inhibitor.Target: SSRIsFluvoxamine (maleate) is the maleate salt form of fluvoxamine, which is effective in inhibiting 5-HT uptake by blood platelets and brain synaptosomes. The antagonism by fluvoxamine of the reserpine-induced lowering of the pentamethylenetetrazole convulsive threshold can be regarded as due to an effect upon 5-HT uptake. In contrast to the effects of desmethylimipramine and imipramine, no stimulatory effects are found in rats when rapidly acting reserpine-like compounds are given following a dose of fluvoxamine [1]. fluvoxamine appears to improve combat-related PTSD symptoms but not depressive symptoms. The high attrition rate and lack of a placebo group limits the conclusions of our study. Controlled studies of fluvoxamine in the treatment of PTSD are warranted [2]. Fluvoxamine was less potent at decreasing ethanol self-administration when food was available concurrently versus when ethanol was available in isolation [ED50: 4.0 (2.7-5.9) and 5.1 (4.3-6.0)]. Effects on food were similar under each condition in which food was available. The results demonstrate that the potency of fluvoxamine in reducing ethanol-maintained behavior depends on whether ethanol is available in isolation or in the context of concurrently scheduled food reinforcement [3].Clinical indications: Depression; Obsessive compulsive disorder; Social phobia " FDA Approved Date: December 5, 1994Toxicity: Anorexia, Constipation, Dry mouth, Headache, Nausea, Nervousness, Skin rash, Sleep problems, Somnolence, Liver toxicity, Mania, Increase urination, Seizures, Sweating increase, Tremors, or Tourette's syndrome.
DiBAC4(3) is a voltage-sensitive fluorescent dye (λex=490 nm, λem=505 nm).
Velpatasvir (VEL, GS-5816) is a novel pan-genotypic hepatitis C virus (HCV) nonstructural protein 5A (NS5A) inhibitor with activity against genotype 1 (GT1) to GT6 HCV replicons.target: NS5A
Erlotinib D6 hydrochloride (CP-358774 D6 hydrochloride) a deuterium labeled Erlotinib Hydrochloride. Erlotinib Hydrochloride inhibits purified EGFR kinase with an 50 of 2 nM[1].
Nampt-IN-8 (Compound 10d) is an NAMPT inhibitor with an IC50 of 0.183 μM. Nampt-IN-8 is also a relatively good NQO1 substrate. Nampt-IN-8 induces cell apoptosis and ROS[1].
Abaecin is an antibacterial response peptide. Abaecin shows specific activity against an Apidaecin-resistant Xanthomonas strain[1].
Timapiprant sodium (OC000459 sodium) is a potent, selective, and orally active D prostanoid receptor 2 (DP2, also known as CRTH2) antagonist. Timapiprant sodium (OC000459 sodium) potently displaces [3H] PGD2 from human recombinant DP2 (Ki=13 nM), rat recombinant DP2 (Ki=3 nM), and human native DP2 (Ki=4 nM). Timapiprant sodium (OC000459 sodium) inhibits mast cell activation of Th2 lymphocytes and eosinophils[1].
Riliprubart (SAR445088) is an anti-C1s humanized monoclonal antibody that inhibits activated C1s in the proximal portion of the classical complement system. Riliprubart selectively inhibits activated C1s and prevents the enzymatic action of C1 on its substrates C4 and C2, thus inhibiting the formation of the classical pathway C3 convertase, C4b2a[1].
PAK-IN-1 is a PAK inhibitor that displays group II selectivity. PAK-IN-1 inhibits PAK4, PAK5 and PAK6 with IC50s of 7.5, 36, 126 nM, respectively.
DIM-C-pPhCO2Me is a nuclear receptor 4A1 (NR4A1) antagonist[1]. Antineoplastic activity[1].
Temporin C is an antimicrobial peptide against Legionella pneumophila[1].
Sirtuin modulator 3 (compound 129) is a N-phenyl benzamide derivative, acts as a sirtuin modulator[1].
DMA-IN-1 is a DNA adenine methyltransferase (DAM) inhibitor, IC50: 48 μM. DMA-IN-1 inhibits Caulobacter growth with an MIC of 35 μM[1].
3-CPs is a serotype capsular polysaccharide which can interfere with antibody-mediated bacterial killing.
PD-1/PD-L1-IN-28 (compound 3) is an immune checkpoint inhibitor of PD-1/PD-L1 signaling pathway (IC50=0.744 µM). PD-1/PD-L1-IN-28 shows good research potential in tumor immunity[1].
3-(4-hydroxy-3,5-dimethoxyphenyl)-1,2-propanediol (Compound 8) is a phenolic glucoside.3-(4-hydroxy-3,5-dimethoxyphenyl)-1,2-propanediol is isolated from the stems of natural Xylosma controversum[1].
BI-135585 is a potent, selective and orally active 11β-hydroxysteroid dehydrogenase 1 (11β-HSD1) inhibitor with an IC50 of 13 nM. BI-135585 exhibits >1000-fold selectivity over other hydroxysteroid dehydrogenases. BI-135585 can be used for type 2 diabetes research[1][2].