1239578-80-3
1239578-80-3
Chemical Structure
NP-1815-PX sodium
- CAS No.: 1239578-80-3
- Formula:C21H13N4NaO3S
- Molecular Weight:424.41
InChIKey: MIBCQKIVVIBTLQ-UHFFFAOYSA-M
SMILES: O=C1NC2=C(N(C(C1)=O)C3=CC=CC(C4=NOC(N4[Na])=S)=C3)C=CC5=C2C=CC=C5
Biological Activity: NP-1815-PX sodium is an orally active dual inhibitor of P2X4 and prostaglandin TP receptors, with an IC50 of 0.26 μM against human P2X4 receptors. NP-1815-PX sodium specifically inhibits ATP-mediated prostaglandin production, TP receptor-induced calcium elevation, and the canonical/non-canonical NLRP3 inflammasome signaling pathway. NP-1815-PX sodium selectively blocks smooth muscle contractions induced by ATP, U46619 (HY-108566) and prostaglandin F2α. NP-1815-PX sodium not only produces anti-allodynic effects in vivo, but also significantly alleviates symptoms of DNBS (HY-W324435)-induced colitis (such as weight loss and tissue damage). NP-1815-PX sodium exerts anti-inflammatory effects by downregulating IL-1β levels and Caspase-1 activity. NP-1815-PX sodium is used in studies related to asthma and inflammatory bowel disease (colitis)[1][2].
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
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NP-1815-PX sodium | 99.51% | NP-1815-PX sodium is an orally active dual inhibitor of P2X4 and prostaglandin TP receptors, with an IC50 of 0.26 μM against human P2X4 receptors. NP-1815-PX sodium specifically inhibits ATP-mediated prostaglandin production, TP receptor-induced calcium elevation, and the canonical/non-canonical NLRP3 inflammasome signaling pathway. NP-1815-PX sodium selectively blocks smooth muscle contractions induced by ATP, U46619 (HY-108566) and prostaglandin F2α. NP-1815-PX sodium not only produces anti-allodynic effects in vivo, but also significantly alleviates symptoms of DNBS (HY-W324435)-induced colitis (such as weight loss and tissue damage). NP-1815-PX sodium exerts anti-inflammatory effects by downregulating IL-1β levels and Caspase-1 activity. NP-1815-PX sodium is used in studies related to asthma and inflammatory bowel disease (colitis). | ||||||||||||||||||||
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Triflubazam | Triflubazam is an anti-anxiety agent. Triflubazam can be used for the research of sleep disorder. | |||||||||||||||||||||
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DPQZ | DPQZ is an anti-tubulin agent that inhibits cell separation and induces cell cycle arrest at the G2/M phase. In addition, DPQZ induces caspase-dependent apoptosis of HSC-3 cells by inhibiting Ras/Raf and activating MAP kinase. DPQZ can be used in the study of oral cancer. | |||||||||||||||||||||
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MY-673 | 98.60% | MY-673 is a colchicine binding site inhibitor (CBSI), that inhibits tubulin polymerization. MY-673 inhibits the ERK signaling pathway, which in turn affects SMAD4 protein expression levels in the TGF-β/SMAD pathway. MY-673 inhibited cell proliferation, migration and induced apoptosis in vivo and in vitro. | ||||||||||||||||||||
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NP-1815-PX | NP-1815-PX is an orally active dual inhibitor of P2X4 and prostaglandin TP receptors, with an IC50 of 0.26 μM against human P2X4 receptors. NP-1815-PX specifically inhibits ATP-mediated prostaglandin production, TP receptor-induced calcium elevation, and the canonical/non-canonical NLRP3 inflammasome signaling pathway. NP-1815-PX selectively blocks smooth muscle contractions induced by ATP, U46619 (HY-108566) and prostaglandin F2α. NP-1815-PX not only produces anti-allodynic effects in vivo, but also significantly alleviates symptoms of DNBS (HY-W324435)-induced colitis (such as weight loss and tissue damage). NP-1815-PX exerts anti-inflammatory effects by downregulating IL-1β levels and Caspase-1 activity. NP-1815-PX is used in studies related to asthma and inflammatory bowel disease (colitis). | |||||||||||||||||||||
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MRS4596 | MRS4596 is a potent and selective P2X4 receptor antagonist with an IC50 value of 1.38 μM for human P2X4 receptor. MRS4596 has neuroprotective and neuro-rehabilitative activities in ischemic stroke model. MRS4596 can be used in research of ischemic stroke . | |||||||||||||||||||||
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MRS4719 | MRS4719 is a potent P2X4 receptor antagonist with an IC50 value of 0.503 μM for human P2X4 receptor. MRS4719 can reduce infarct volume and reduce brain atrophy, showing neuroprotective and neuro-rehabilitative activities in ischemic stroke model. MRS4719 also reduces ATP-induced [Ca2+]i influx in primary human monocyte-derived macrophages. MRS4719 can be used to research ischemic stroke. | |||||||||||||||||||||
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JNU-0921 | 99.77% | JNU-0921 is a potent and orally active CD137 agonist. JNU-0921 increases the mRNA expression of IFN-γ and GZMB. JNU-0921 induces luciferase activity with an EC50 value of 64.07 nM.JNU-0921 enhances effector and memory function of cytotoxic CD8+ T cells (CTLs) and alleviates their exhaustion. JNU-0921 also skews polarization of helper T cells toward T helper 1 type and enhances their activity to boost CTL function. JNU-0921 shows anticancer activity. | ||||||||||||||||||||
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N-(3-Fluoranthenyl)maleimide | N-(3-Fluoranthyl)maleimide is a thiol fluorescent probe with a lifetime of 20 nsec. N-(3-Fluoranthyl)maleimide has a maximum excitation wavelength of 370 nm and can be used to study the time-dependent processes of biopolymers. | |||||||||||||||||||||
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N-(1-Pyrenyl)maleimide | N-(1-Pyrenyl)maleimide is a biochemical reagent that can be used as a biological material or organic compound for life science related research. | |||||||||||||||||||||
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Clobazam impurity 4 | Clobazam impurity 4 is an impurity of Clobazam. | |||||||||||||||||||||
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References
- [1]. Obara K, et al. Effects of NP-1815-PX, a P2X4 Receptor Antagonist, on Contractions in Guinea Pig Tracheal and Bronchial Smooth Muscles. Biol Pharm Bull. 2022;45(8):1158-1165. [Content Brief]
- [2]. D’Antongiovanni V, et al. RETRACTED ARTICLE: Anti-inflammatory Effects of Novel P2X4 Receptor Antagonists, NC-2600 and NP-1815-PX, in a Murine Model of Colitis[J]. Inflammation, 2022, 45(4): 1829-1847.
