ro31-8425 hydrochloride

Ro 31-8220 Mesylate (Bisindolylmaleimide IX mesylate) is a pan-PKC inhibitor for PKC-α/βI/βII/γ/ε (IC50: 5/24/14/27/24 nM), and also shows potent inhibition against MSK1, MAPKAP-K1b, S6K1, and GSK3β.

Bisindolylmaleimide X hydrochloride (BIM-X hydrochloride) is a potent and selective PKC inhibitor. It is also a potent CDK2 antagonist (IC50: 200 nM).

Potent trace amine 1 (TA1) receptor agonist (EC50 values are 0.12, 35 and 17-85 nM for mouse, rat and human receptors, respectively). Increases wakefulness and reduces REM and NREM sleep duration in wild type mice. Inhibits spontaneous locomotor activity in dopamine transport (DAT) knockout mice. Espinoza et al (2018) Biochemical and functional characterization of the trace amine-associated receptor 1 (TAAR1) agonist RO5263397. Front.Pharmacol. 9 645 PMID:29977204 |Galley et al (2015) Discovery and characterization of 2-aminooxazolines as highly potent, selective, and orally active TAAR1 agonists. ACS.Med.Chem.Letts. 7 192 PMID:26985297 |Schwartz et al (2017) Trace amine-associated receptor 1 regulates wakefulness and EEG spectral composition. Neuropsychopharmacology. 42 1305 PMID:27658486

Ro 31-8830, a derivative of Ro 31-8425, has in vivo anti-inflammatory activity.

NR2B-containing NMDA receptors antagonist

Ro 41-1049 hydrochloride is a reversible and selective inhibitor of monoamine oxidase-A (Kd: 16.5 and 64.4 nM, respectively).

Ro 31-0313 is a metabolite of Ro 03-8799, radiation sensitizing agent.

Ro 32-0432 hydrochloride is a protein kinase C inhibitor.

Ro 31-0052 is a bioactive chemical.

Ro 31-4639 is a phospholipase A2 inhibitor in vitro.

Selective prostacyclin IP receptor antagonist (pKi = 8.3). Exhibits no affinity at other prostanoid receptors (EP1-4, FP and TP) in a radioligand binding assay. Demonstrates analgesic activity in rats. Orally bioavailable. Clark et al (2004) Discovery and SAR development of 2-(phenylamino) imidazolines as prostacyclin receptor antagonists. Bioorg.Med.Chem.Lett. 14 1053 PMID:15013022 |Jones et al (2006) Investigation of the prostacyclin (IP) receptor antagonist RO1138452 on isolated blood vessel and platelet preparations. Br.J.Pharmacol. 149 110 PMID:16880763 |Bley et al (2006) RO1138452 and RO3244794: characterization of structurally distinct, potent and selective IP (prostacyclin) receptor antagonists. Br.J.Pharmacol. 147 335 PMID:16331286

Ro 31-7837 is an opener of potassium channel.

Ro 31-2201 is a potent inhibitor of angiotensin converting enzyme.

Ro 31-8875 is a biochemical.

Ro 363 hydrochloride is an effective, highly selective agonist of β 1-adrenoceptor. Ro 363 hydrochloride is an effective inotropic stimulant. Ro 363 hydrochloride is a cardiovascular regulator, which can reduce diastolic blood pressure and significantly increase myocardial contractility.

Talviraline is a RNA-directed DNA polymerase inhibitor. HBY 097 is a highly potent inhibitor of HIV-1 replication and HIV-1 induced cell killing in a variety of human cell lines as well as in fresh human peripheral blood lymphocytes and macrophages.

Ro 31-1118 is a partial agonist of beta-adrenoceptor.

Ro 31-8472 is an angiotensin-converting enzyme (ACE) inhibitor and an analog of cilazaprilat.

Ro 31-9790 is a synthetic inhibitor of metalloproteinase (MMP).

Ro 8-4304 hydrochloride is a NMDA receptor antagonist.

Ro 31-8220 is a potent inhibitor of PKC with IC 50 s of 5, 24, 14, 27, 24 and 23 nM for PKCα, PKCβI, PKCβII, PKCγ, PKCε and rat brain PKC, respectively. Ro 31-8220 also significantly inhibits MAPKAP-K1b, MSK1, S6K1 and GSK3β with IC50s of 3, 8, 15, and 38 nM, respectively without effect on MKK3, MKK4, MKK6 and MKK7.