Norethindrone-d6 is the deuterium labeled Norethindrone. Norethindrone is a female progestin approved by FDA for the treatment of endometriosis, uterine bleeding caused by abnormal hormone levels, and secondary amenorrhea.
Hydrocortisone buteprate (Hydrocortisone probutate) is a medium potent, non-halogenated double-ester of hydrocortisone with a favorable benefit/risk ratio for the treatment of inflammatory skin disorders. Hydrocortisone buteprate (Hydrocortisone probutate) is available as a 0.1% cream or ointment formulation[1].
SPDP-PEG4-acid is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
Coumalic acid is a valuable platform compound which can be prepared from malic acid. Coumalic acid can be used in the flavours, fragrances and cosmetics industries, as polymer components, and as pharmaceutical scaffolds displaying anti-bronchial and -malarial activity[1].
(±)-Vesamicol hydrochloride ((±)-AH5183 hydrochloride) is a potent vesicular acetylcholine transport inhibitor with a Ki of 2 nM. (±)-Vesamicol hydrochloride also displays high affinity for σ1 and σ2 receptors with Kis of 26 nM and 34 nM, respectively[1][2].
(Rac)-Arnebin 1 ((Rac)-β,β-Dimethylacrylalkannin) is the racemate of β,β-Dimethylacrylalkannin and/or β,β-Dimethylacrylshikonin. β,β-Dimethylacrylalkannin and β,β-Dimethylacrylshikonin are napthoquinones isolated from Arnebia nobilis. β,β-Dimethylacrylshikonin has anti-tumor activity[1].
trans-Clopenthixol ((E)-Clopenthixol) dihydrochloride is an antibiotic agent, without neuroleptic effect. trans-Clopenthixol can be used to inhibit Pseudomonas aeruginosa and Plasmodium falciparum in vitro[1][2].
Nebracetam hydrochloride, a nootropic M1-muscarinic agonist, induces a rise of intracellular Ca2+ concentration. Nebracetam hydrochloride exhibits an EC50 of 1.59 mM for elevating [Ca2+]i[1].
Cycloguanil hydrochloride, the active metabolite of Proguanil, acts on malaria schizonts in erythrocytes and hepatocytes[1].
Eupatoletin is a flavonol compound isolated from Eupatorium ligustrinum D.C.[1].
1alpha, 25-Dihydroxy VD2-D6 is a deuterated form of vitamin D.
Cyanidin, an antioxidant, has protective effect on DNA cleavage, free radical scavenging activity and significant inhibition of XO activity[1].
Netupitant N-oxide is the metabolite of Netupitant, which is a highly selective NK1 receptor antagonist.
IST5-002, a potent Stat5a/b inhibitor, selectively inhibits transcriptional activity of Stat5a/b (IC50s: 1.5 μM for Stat5a, 3.5 μM for Stat5b). IST5-002 inducs cell apoptotic and death of prostate cancer cells and chronic myeloid leukemia (CML) cells. IST5-002 can be used in the research of prostate cancer and chronic myeloid leukemia (CML)[1].
Beauveriolide III is an inhibitor of lipid droplet formation in mouse macrophages[1].
Jacquilenin is a natural product that can be isolated from the flowers of Picris hieracioides L.[1].
Taq DNA polymerase is a thermostable DNA polymerase that can be used in PCR[1].
Brombuterol D9 (Bromobuterol D9) is a deuterium labeled Brombuterol. Brombuterol is a β-adrenergic receptor agonist[1].
1,2-Dioleoyl-sn-glycero-3-phospho-L-serine sodium is a ubstitute for Phosphoserine/phosphatidylserine. 1,2-Dioleoyl-sn-glycero-3-phospho-L-serine sodium can be used in lipid mixtures with DOPC and DOPE as effective nontoxic and nonviral DNA vectors[1].
Mebendazole-d3 is the deuterium labeled L-Methionine-34S[1].
5-Hydroxycytosine-13C,15N2 is the 13C and 15N labeled 5-Hydroxycytosine[1].
Exendin-3 is a biologically active peptides isolated from venoms of the Gila monster lizards, Heloderma horridurn .
Ferron (8-Hydroxy-7-iodo-5-quinolinesulfonic acid) has antiseptic and antifungal activity. Ferron can prevent skin and mucosa bacterial irritations and inflammations[1].
Pinacyanol iodide is a fluorescent cyanine dye. Pinacyanol iodide exhibits ultrafast excited state isomerization[1].
Metallo-β-lactamase-IN-7 is a potent VIM-Type metallo-β-lactamase inhibitor with IC50s of 0.019 μM, 13.64 μM, 0.38 μM for VIM-2, VIM-1 and VIM-5. Metallo-β-lactamase-IN-7 potentiate antibacterial activity of Meropenem against the Gram-negative bacterial strains[1].
Ac-Nle-Pro-Nle-Asp-AMC is a specific substrate for 26S proteasome. Ac-Nle-Pro-Nle-Asp-AMC can be used for the 26S proteasome caspase-like activity analysis[1][2][3].
Z-Gly-Pro-Arg-4MβNA is the cleavage of the substrate of thrombin to release free 4-methoxy-2-naphthylamine (4MβNA). Free 4MβNA can be captured by 5-nitrosalicylaldehyde to produce an insoluble yellow fluorescent and marks the site of thrombin activity[1].
(D)-PPA 1 is a hydrolysisresistant d-peptide antagonist. (D)-PPA 1 serves as a potent PD-1/PD-L1 inhibitor. (D)-PPA 1 binds to PD-1 with the affinity 0f 0.51 μM with in vitro and in vivo efficacy[1].
15-PGDH-IN-1 is a potent and orally active 15-PGDH inhibitior. 15-PGDH-IN-1 has inhibition activity against recombinant human 15-PGDH with an IC50 value of 3 nM. 15-PGDH-IN-1 can be used for the research of tissue repair and regeneration[1].
Lasmiditan (COL-144; LY573144) is a high-affinity, highly selective 5-HT1F receptor agonist(Ki=2.1 nM), compared with Ki of 1043 nM and 1357 nM at the 5-HT(1B) and 5-HT(1D) receptors, respectively.IC50 value: 2.1 nM (Ki, 5-HT1F); >1000 nM (Ki, 5-HT1B/5-HT1D) [1]Target: 5-HT1F receptorin vitro: In vitro binding studies Lasmiditan showed a K(i) value of 2.21 nM at the 5-HT(1F) receptor, compared with K(i) values of 1043 nM and 1357 nM at the 5-HT(1B) and 5-HT(1D) receptors, respectively, a selectivity ratio greater than 470-fold. Lasmiditan showed higher selectivity for the 5-HT(1F) receptor relative to other 5-HT(1) receptor subtypes than the first generation 5-HT(1F) receptor agonist LY334370. Unlike the 5-HT(1B/1D) receptor agonist sumatriptan, lasmiditan did not contract rabbit saphenous vein rings, a surrogate assay for human coronary artery constriction, at concentrations up to 100 μM [1].in vivo: In two rodent models of migraine, oral administration of lasmiditan potently inhibited markers associated with electrical stimulation of the trigeminal ganglion (dural plasma protein extravasation, and induction of the immediate early gene c-Fos in the trigeminal nucleus caudalis) [1]. Two RCTs in the phase II development of lasmiditan was reviewed. In the intravenous placebo-controlled RCT, lasmiditan doses of 2.5-45 mg were used, and there was a linear association between headache relief (HR) rates and dose levels (P < 0.02). For lasmiditan 20 mg, HR was 64 % and for placebo it was 45 % (NS). In the oral placebo-controlled RCT, lasmiditan doses of 50, 100, 200 and 400 mg were used. For HR, all doses of lasmiditan were superior to placebo (P < 0.05). For lasmiditan 400 mg, HR was 64 % and it was 25 % for placebo. Adverse events (AEs) emerging from the treatment were reported by 22 % of the patients receiving placebo and by 65, 73, 87 and 87 % of patients receiving 50, 100, 200 and 400 mg, respectively [2].