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AF-353 (Ro-4), an effective and orally bioavailable antagonist of the P2X3/P2X2/3 receptor, inhibits human and rat P2X3 (pIC50= 8.0).

Sulfamethoxazole-d4 (Ro4-2130 D4) is a deuterium labeled Sulfamethoxazole, which can be used for isotope tracing.Sulfamethoxazole is a sulfonamide antimicrobial agent.

RO495 (CS-2667), a potent inhibitor of TYK2, inhibits TYK2 with IC50 of 1.5nM as tested in cell-based pharmacological assays

Ro4368554 is a selective 5-HT6 antagonist capable of crossing the blood-brain barrier. It can reverse memory deficits caused by scopolamine and tryptophan depletion. Ro4368554 is applicable for research related to memory impairments.

Ro4491533 is a potent and selective negative allosteric modulator for group II of the metabotropic glutamate receptors (mGluR2/3).

RO4988546 is a potent negative allosteric modulator of mGlu₂/₃.

RO4987655 (RG7167) is an orally active and highly selective MEK inhibitor (IC50: 5.2 nM for MEK1/MEK2).

RO4929097 (RG-4733), a γ secretase inhibitor (IC50: 4 nM), inhibits cellular processing of Aβ40 and Notch (EC50: 14/5 nM).

RO4927350 is a potent and highly selective non-ATP-competitive MEK1/2 inhibitor. RO4927350 selectively blocks the MAPK pathway signaling both in vitro and in vivo, which results in significant antitumor efficacy in a broad spectrum of tumor models. RO4927350 inhibits not only ERK1/2 but also MEK1/2 phosphorylation. In cancer cells, high basal levels of phospho-MEK1/2 rather than phospho-ERK1/2 seem to correlate with greater sensitivity to RO4927350. Furthermore, RO4927350 prevents a feedback increase in MEK phosphorylation, which has been observed with other MEK inhibitors. RO4927350 represents a novel therapeutic modality in cancers with aberrant MAPK pathway activation.

RO4583298 is a highly potent dual NK1/NK3 receptor antagonist with in vivo activity.

[D-Pro4,D-Trp7,9,Nle11] Substance P (4-11) is a potent neurokinin NK1 antagonist that effectively inhibits the actions of gold-protein-substance P (GPSP) and substance P (SP), demonstrating its efficacy in neutralizing their effects [1].

[D-Pro4,D-Trp7,9] Substance P (4-11) acts as a potent Substance P antagonist, significantly reducing plasma aldosterone (ALDO) concentrations[1].

[D-Pro4,D-Trp7,9,10] Substance P (4-11) is a potent antagonist of the tachykinin family of neuropeptides [1].

[Dehydro-Pro4] Substance P (4-11) is a peptide segment of Substance P. This compound, predominantly secreted by neurons, plays a key role in several biological processes, including nociception, inflammation, and immune response.

7-Chlorokynurenic acid (7-chloro-4-hydroxy-2-carboxyquinoline) is an effecitve and selective antagonist of NMDA receptor with IC50 of 0.56 μM for the glycine B coagonist site. 7-Chlorokynurenic acid inhibits the reuptake of glutamate into synaptic vesicles with a Ki of 0.59 μM and shows antinociceptive actions after neuraxial delivery.

Lirequinil (Ro 41-3696) is a small molecule GABAA receptor agonist utilized in the study of neurological disorders.

(-)-OPC-51803 is an antidiuretic hormone V2 receptor agonist used in the treatment of nocturia and urinary incontinence.

Sembragiline (EVT-302) is a selective MAO-B inhibitor for the study of Alzheimer's disease (AD).

4-(2-chloro-4-methoxy-5-methylphenyl)-N-[(1A)-2-cyclopropyl-1-(3-fluoro-4-methylphenyl)ethyl]-5-methyl-N-(2-propyn-1-yl)-2-thiazolamine is an enantiomeric counterpart of SSR-125543. SSR-125543 is a potent CRF-R1 antagonist with Ki = 1.0 nM for human CRF-R1.

R547 (Ro 4584820) is a potent ATP-competitive inhibitor of CDK1/2/4 with Ki of 2 nM/3 nM/1 nM. It is less potent to CDK7 and GSK3α/β, while inactive to other kinases. Phase 1.

(Iso)-RJW100 is a potent liver receptor homolog 1 (LRH-1, NR5A2) and steroidogenic factor-1 (SF-1, NR5A1) agonist with pEC 50 s of 6.4 and 7.2, respectively.

11β-HSD1 inibitor 19 shows inhibitory activities for hHSD1 and mHSD1 with IC50s of 16 nM and 10 nM.

MET kinase-IN-2, a selective and potent MET kinase inhibitor, demonstrates oral bioavailability and exhibits an IC50 value of 7.4 nM. It also possesses antitumor activity[1].

IMT1B (LDC203974) is an orally administered, specific noncompetitive allosteric inhibitor of mitochondrial RNA polymerase (POLRMT), effectively suppressing mitochondrial DNA (mtDNA) expression and conferring anti-tumor properties.