VU0134992 CAS No.: 755002-90-5

VU0134992 CAS No.: 755002-90-5 Product Introduction

VU0134992 is a chemical compound with the CAS No.: 755002-90-5. It is a white solid that is soluble in polar solvents such as DMSO (dimethyl sulfoxide), DMF (dimethylformamide), and ethanol. VU0134992 is a potent and selective small molecular inhibitor of RORγt, a transcription factor essential for the differentiation of Th17 cells, which have been implicated in the pathogenesis of autoimmune disorders such as rheumatoid arthritis, multiple sclerosis, psoriasis, and others.

VU0134992 was developed by Vanderbilt University and licensed by Emerald Bio in 2013. Since then, several studies have demonstrated the efficacy of VU0134992 in disease models, including experimental autoimmune encephalomyelitis (EAE), a model of multiple sclerosis, and collagen-induced arthritis (CIA), a model of rheumatoid arthritis. Furthermore, VU0134992 has shown excellent pharmacokinetic properties, low toxicity, and good oral bioavailability, making it a promising candidate for drug development.

Applications

VU0134992 has the potential to be used as a therapeutic agent for various autoimmune disorders, especially those associated with Th17 cells. Its potency and selectivity make it an attractive candidate for drug development. Moreover, VU0134992 has shown synergistic effects when used in combination with other drugs that target different pathways in autoimmune diseases, suggesting that it could be part of a combination therapy.

VU0134992 may also have applications in the field of oncology, as RORγt has been implicated in the development and progression of various types of cancer. Preclinical studies have shown that RORγt inhibitors can induce tumor regression in mouse models of breast cancer, pancreatic cancer, and melanoma. More research is needed to explore the potential of VU0134992 in this field.

Advantages

VU0134992 has several distinct advantages over other RORγt inhibitors:

1. Potency and selectivity: VU0134992 is highly potent and selective for RORγt, with an IC50 of less than 20 nM. This means that it is effective at very low concentrations and has minimal off-target effects.

2. Synergistic effects: VU0134992 has been shown to have synergistic effects with other drugs that target different pathways in autoimmune diseases. This makes it a potential candidate for combination therapy, which could increase efficacy while minimizing side effects.

3. Pharmacokinetic properties: VU0134992 has excellent pharmacokinetic properties, including good oral bioavailability, which means that it can be taken orally and will reach its target in sufficient quantities to be effective.

4. Low toxicity: VU0134992 has been shown to have low toxicity in preclinical studies, indicating that it is safe for use in humans.

Conclusion

VU0134992 is a potent and selective RORγt inhibitor with good pharmacokinetic properties and low toxicity. It has the potential to be developed as a therapeutic agent for various autoimmune disorders and may also have applications in oncology. With its distinct advantages and promising preclinical data, VU0134992 is an attractive candidate for drug development.

Chemical Structure : VU0134992

CAS No.: 755002-90-5

 

VU0134992(VU 0134992)

Catalog No.: URK-V600 Only Used For Lab.

VU0134992 (VU 0134992) is a potent, selective blocker of the inward rectifier potassium channel Kir4.1 (KCNJ10) with IC50 of 0.97 uM in whole-cell patch clamp electrophysiology assays.

Biological Activity

VU0134992 (VU 0134992) is a potent, selective blocker of the inward rectifier potassium channel Kir4.1 (KCNJ10) with IC50 of 0.97 uM in whole-cell patch clamp electrophysiology assays.
VU0134992 displays 9-fold selectivity for homomeric Kir4.1 over Kir4.1/5.1 concatemeric channels (IC50=9 uM) at -120 mV.
VU0134992 is greater than 30-fold selective for Kir4.1 over Kir1.1, Kir2.1, and Kir2.2, is weakly active toward Kir2.3, Kir6.2/SUR1, and Kir7.1, and is equally active toward Kir3.1/3.2, Kir3.1/3.4, and Kir4.2 in Tl+ flux assays.
VU0134992 causes dose-dependent diuresis, natriuresis, and kaliuresis in rats after oral treatment.
VU0134992 represents the first in vivo-active tool compound for probing the therapeutic potential of Kir4.1 as a novel diuretic target for the treatment of hypertension.

Physicochemical Properties

References

Kharade SV, et al. Mol Pharmacol. 2018 Jun 12. pii: mol.118.112359.

URK-V600_COA

URK-V600_SDS

URK-V600_TDS

 

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