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CAY10740 (hydrochloride) Sale

目录号 : GC47051

A neuropeptide with diverse biological activities

CAY10740 (hydrochloride) Chemical Structure

规格 价格 库存 购买数量
500 μg
¥496.00
现货
1 mg
¥942.00
现货
5 mg
¥3,975.00
现货
10 mg
¥6,956.00
现货

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Sample solution is provided at 25 µL, 10mM.

产品文档

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产品描述

CAY10740 is an analog of the protein arginine deiminase 4 (PAD4) inhibitor GSK484 .1 It decreases the viability of 4T1 cells by 85 and 98% when used at concentrations of 5 and 10 μM, respectively, which is more than five-fold as effective as GSK484.

1.Guo, Z., Shi, L., Wang, B., et al.Synthesis of reversible PAD4 inhibitors via copper-catalyzed C-H arylation of benzimidazoleSci. China Chem.62(6)592-596(2019)

Chemical Properties

Cas No. N/A SDF
Canonical SMILES COC1=C2C(N=C(C3=CC4=C(C=CC=C4)N3CC5=CC=CC=C5)N2C)=CC(C(N6CC[C@@H](O)[C@@H](N)C6)=O)=C1.Cl
分子式 C30H31N5O3.HCl 分子量 546.1
溶解度 DMF: 10mg/mL,DMF:PBS (pH 7.2) (1:2): 0.3mg/mL,DMSO: 5mg/mL,Ethanol: 0.3mg/mL 储存条件 Store at -20°C
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储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。
Shipping Condition 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。

溶解性数据

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1 mg 5 mg 10 mg
1 mM 1.8312 mL 9.1558 mL 18.3117 mL
5 mM 0.3662 mL 1.8312 mL 3.6623 mL
10 mM 0.1831 mL 0.9156 mL 1.8312 mL
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Research Update

Nalfurafine hydrochloride, a κ-Opioid Receptor Agonist, Induces Melanophagy via PKA Inhibition in B16F1 Cells

Cells 2022 Dec 29;12(1):146.PMID:36611940DOI:10.3390/cells12010146.

Selective autophagy controls cellular homeostasis by degrading unnecessary or damaged cellular components. Melanosomes are specialized organelles that regulate the biogenesis, storage, and transport of melanin in melanocytes. However, the mechanisms underlying melanosomal autophagy, known as the melanophagy pathway, are poorly understood. To better understand the mechanism of melanophagy, we screened an endocrine-hormone chemical library and identified nalfurafine hydrochlorides, a κ-opioid receptor agonist, as a potent inducer of melanophagy. Treatment with nalfurafine hydrochloride increased autophagy and reduced melanin content in alpha-melanocyte-stimulating hormone (α-MSH)-treated cells. Furthermore, inhibition of autophagy blocked melanosomal degradation and reversed the nalfurafine hydrochloride-induced decrease in melanin content in α-MSH-treated cells. Consistently, treatment with other κ-opioid receptor agonists, such as MCOPPB or mianserin, inhibited excessive melanin production but induced autophagy in B16F1 cells. Furthermore, nalfurafine hydrochloride inhibited protein kinase A (PKA) activation, which was notably restored by forskolin, a PKA activator. Additionally, forskolin treatment further suppressed melanosomal degradation as well as the anti-pigmentation activity of nalfurafine hydrochloride in α-MSH-treated cells. Collectively, our data suggest that stimulation of κ-opioid receptors induces melanophagy by inhibiting PKA activation in α-MSH-treated B16F1 cells.

Delirium due to the use of topical cyclopentolate hydrochloride

Ideggyogy Sz 2020 Jan 30;73(1-2):51-52.PMID:32057204DOI:10.18071/isz.73.0051.

Introduction - Our aim is to present a rare case where a child had delirium manifestation after instillation of cyclopentolate. Case presentation - A 7-year old patient was seen in our outpatient clinic, and cyclopentolate was dropped three times at 10 minutes intervals in both eyes. The patient suddenly developed behavioral disorders along with gait disturbance, and complained of visual hallucinations 20-25 minutes after the last drop. The patient was transferred to intensive care unit and 0.02 mg/kg IV. physostigmine was administered. The patient improved after minutes of onset of physostigmine, and was discharged with total recovery after 30 minutes. Conclusion - Delirium is a rare systemic side effect of cyclopentolate. The specific antidote is physostigmine, which can be used in severely agitated patients who are not responding to other therapies.

Copper-catalyzed three-component reaction of arylhydrazine hydrochloride, DABSO, and NFSI for the synthesis of arenesulfonyl fluorides

Org Biomol Chem 2021 Oct 27;19(41):8999-9003.PMID:34605502DOI:10.1039/d1ob01697k.

This paper reports a convenient copper-catalyzed three-component conversion of arylhydrazine hydrochlorides to arenesulfonyl fluorides in good yields under mild conditions, using 1,4-diazabicyclo [2.2.2]octane bis(sulfur dioxide) (DABSO) as a sulfonyl source and N-fluorobenzenesulfonimide (NFSI) as a fluorine source based on a radical sulfur dioxide insertion and fluorination strategy. Notably, arylhydrazine hydrochloride is used as a safe precursor of aryl radicals.

Rapid synthesis of alkoxyamine hydrochloride derivatives from alkyl bromide and N,N'- di- tert-butoxycarbonylhydroxylamine ((Boc)2NOH)

Synth Commun 2014 Aug 1;44(16):2344-2347.PMID:25368434DOI:10.1080/00397911.2014.895014.

The conventional route to alkoxyamine hydrochloride derivatives is by reaction of alkyl bromides with N-hydroxyphthalimide or N-hydroxysuccinimide followed by addition of hydrazine and HCl. Transformation of an alkyl bromide to the corresponding alkoxyamine hydrochloride can be accomplished more rapidly in high yield and without using hazardous hydrazine by reaction of (Boc)2NOH (N,N'-di-tert-butoxycarbonylhydroxylamine) and alkyl bromide followed by addition of HCl. Alkoxyamine hydrochlorides are powerful reagents in organic synthesis that can be used to synthesize alkoxyimino derivatives after condensation with a ketone or aldehyde.

1-[4-(2-Dimethylaminoethoxy)phenylcarbonyl]-3,5-Bis(3,4,5-Trimethoxybenzylidene)- 4-Piperidone hydrochloride and Related Compounds: Potent Cytotoxins Demonstrate Greater Toxicity to Neoplasms than Non- Malignant Cells

Med Chem 2022;18(9):1001-1012.PMID:35319387DOI:10.2174/1573406418666220322154110.

Background: The incidence of cancer has been increasing worldwide. Unfortunately, the drugs used in cancer chemotherapy are toxic to both neoplasms and normal tissues, while many available medications have low potencies. Conjugated α,β-unsaturated ketones differ structurally from contemporary anticancer medications , some of which have noteworthy antineoplastic properties. Objectives: This study aimed to design and synthesize highly potent cytotoxins with far greater toxicity to neoplasms than to non-malignant cells. Methods: A series of N-acyl-3,5-bis(benzylidene)-4-piperidone hydrochlorides 4a-n were prepared and evaluated against Ca9-22, HSC-2, HSC-3, and HSC-4 squamous cell carcinomas as well as against HGF, HPLF, and HPC non-malignant cells. QSAR and western blot analyses were performed. Results: The majority of compounds display submicromolar CC50 values towards the neoplasms; the figures for some of the compounds are below 10-7 M. In general, 4a-n have much lower CC50 values than those of melphalan, 5-fluorouracil, and methotrexate, while some compounds are equitoxic with doxorubicin. The compounds are far less toxic to the non-malignant cells, giving rise to substantial selectivity index (SI) figures. A QSAR study revealed that both potency and the SI data were controlled to a large extent by the electronic properties of the substituents in the arylidene aryl rings. Two representative compounds, 4f and 4g, caused apoptosis in HSC-2 cells. Conclusion: The compounds in series 4 are potent cytotoxins displaying tumor-selective toxicity. In particular, 4g with an average CC50 value of 0.04 μM towards four malignant cell lines and a selectivity index of 46.3 is clearly a lead molecule that should be further evaluated.