Ivermectin (MK-933) - Moligand™, 10mM in DMSO , Allosteric modulator of nicotinic acetylcholine receptor α7 subunit;Allosteric modulator of P2X4;Allosteric modulator of P2X7, CAS No.70288-86-7, Allosteric modulator of nicotinic acetylcholine receptor α7 subunit;Allosteric modulator of P2X4;Allosteric modulator of P2X7

CAS: 70288-86-7 Cat. No.: I407954 Peso molecular: 875.09 Número EC: 274-536-0

GRADE & PURITY Moligand™, 10mM in DMSO

Synonyms

no

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Descripción general

Information

Ivermectin (MK-933, IVM) is a glutamate-gatedchloride channel(GluCls) activator, used as a broad-spectrum antiparasitic drug. Ivermectin (MK-933, IVM) is a specific positive allosteric effector ofP2X4andα7 nicotinic acetylcholine receptors (nAChRs). Iverm
In vitro

Ivermectin has potent antiviral activity towards both HIV-1 anddengue virus, both of which are strongly reliant on importin α/β nuclear import, with respect to the HIV-1 integrase and NS5 (non-structural protein 5) polymerase proteins respectively. Ivermectin binds to a novel site on the GABAA receptor and allosterically enhances the affinity of the GABA binding site in mouse hippocampal embryonic neurons. Ivermectin disrupts neurotransmission processes regulated by GluCl activity by binding to nematode glutamate-gated chloride channels (GluCls). Ivermectin decreases the amount of protein released from microfilariae.

In vivo

Ivermectin (1.25-10 mg/kg, intraperitoneal) significantly reduces 24-h alcohol consumption and intermittent limited access (4-hours) binge drinking, and operant alcohol self-administration (1-h). Ivermectin also produces a significant reduction in 24-h saccharin consumption, but does not alter operant sucrose self-administration. Ivermectin improves mouse survival rate induced by a lethal dose of LPS. Ivermectin significantly decreases the production of TNF-alpha, IL-1ss and IL-6 in vivo and in vitro. Ivermectin suppresses NF-kB translocation induced by LPS.
Cell Data

cell lines：

Concentrations：

Incubation Time：

Powder Purity:≥96%

Specifications

Sinónimos

no

Especificaciones y pureza

Moligand™, 10mM in DMSO

Mecanismos bioquímicos y fisiológicos

Ivermectin (MK-933, IVM) is a glutamate-gated chloride channel (GluCls) activator, used as a broad-spectrum antiparasitic drug. Ivermectin (MK-933, IVM) is a specific positive allosteric effector of P2X4 and α7 nicotinic acetylcholine receptors (nAChRs).

Condiciones de almacenamiento de almacenamiento

Store at -80°C

Enviado en

Dry ice packs + Cold packs

Este producto requiere envío en cadena de frío. Los servicios terrestres y otros servicios económicos no están disponibles.

Grado

Moligand™

Tipo de acción

ALLOSTERIC MODULATOR

Mecanismo de acción

Allosteric modulator of nicotinic acetylcholine receptor α7 subunit;Allosteric modulator of P2X4;Allosteric modulator of P2X7

Nombres e identificadores

• Isómeros SMILES: CC[C@H](C)[C@@H]1[C@H](CC[C@@]2(O1)C[C@@H]3C[C@H](O2)C/C=C(/[C@H]([C@H](/C=C/C=C/4\CO[C@H]5[C@@]4([C@@H](C=C([C@H]5O)C)C(=O)O3)O)C)O[C@H]6C[C@@H]([C@H]([C@@H](O6)C)O[C@H]7C[C@@H]([C@H]([C@@H](O7)C)O)OC)OC)\C)C
• WGK Alemania: 3
• Peso molecular: 875.09
• Reaxy-Rn: 29304044
• Reaxys-RN_link_address: https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=29304044&ln=

Objetivos asociados (humanos)

CHRNA7 Tchem Neuronal acetylcholine receptor subunit alpha-7 (1 Activities)

Discover Target: CHRNA7

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

P2RX4 Tchem P2X purinoceptor 4 (1 Activities)

Discover Target: P2RX4

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

P2RX7 Tchem P2X purinoceptor 7 (0 Activities)

Discover Target: P2RX7

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

Propiedades químicas y físicas

• Solubilidad: Solubility (25°C) In vitro DMSO: 26 mg/mL (199.84 mM); Water: 5 mg/mL (38.43 mM); Ethanol: 26 mg/mL

Referencias

1. Song Lianjun, Wang Youyi, Li Qingyue, Wang Jinkui, Gao Tian, An Zhaohuan, Liu Qinfang, Mao Yexuan, Bu Tong, Huang Xianqing, Ma Yan, Wang Zhanhui, Zhang Xiya.  (2023)  Production of monoclonal antibody against tylosin and tilmicosin with homogeneous cross-reactivity and its application in lateral flow immunoassay.  MICROCHIMICA ACTA,  191  (1): (1-12).  [PMID:38114730] [10.1007/s00604-023-06132-z]

2. Chen Jing, Huang Shuting, Li Huawen, Li Yun, Zeng Haishan, Hu Jiemei, Lin Yanchun, Cai Huihua, Deng Pengfei, Song Ting, Guan Tian, Zeng Haoyu, Liu Mubiao.  (2022)  STAT3 inhibitor BBI608 reduces patient-specific primary cell viability of cervical and endometrial cancer at a clinical-relevant concentration.  Clinical & Translational Oncology,  25  (3): (662-672).  [PMID:36422798] [10.1007/s12094-022-02970-0]

3. Gu Yu-Xin, Yan Tian-Ci, Yue Zi-Xuan, Li Min-Hui, Zheng Hui, Wang Shu-Ling, Cao Jun.  (2022)  Dispersive Micro-solid-Phase Extraction of Acaricides from Fruit Juice and Functional Food Using Cucurbituril as Sorbent.  Food Analytical Methods,  15  (5): (1356-1367).  [PMID:] [10.1007/s12161-021-02209-8]

4. Guanqiong Na, Xiaofei Hu, Yaning Sun, Sharon Kwee, Guangxu Xing, Yunrui Xing, Gaiping Zhang.  (2020)  A highly sensitive monoclonal antibody−based paper sensor for simultaneously detecting valnemulin and tiamulin in porcine liver.  JOURNAL OF FOOD SCIENCE,  85  (6): (1681-1688).  [PMID:32418205] [10.1111/1750-3841.15136]

5. Ding Ke, Tian Hailong, Li Lei, Wang Zhihan, Liu Shanshan, Ding Ning, Nice Edouard C., Huang Canhua, Bao Jinku, Gao Wei, Shi Zheng.  (2024)  Drug repurposing-based nanoplatform via modulating autophagy to enhance chemo-phototherapy against colorectal cancer.  JOURNAL OF NANOBIOTECHNOLOGY,  22  (1): (1-15).  [PMID:38658952] [10.1186/s12951-024-02416-5]

6. Jiawen Ji, Siyue Zhu, Xinping Hu, Jianhui Zhu, Sen Pang, Yongqiang Ma, Xuefeng Li.  (2025)  Enhanced residual risk of abamectin induced by 6PPD: in water, soil, and vegetables.  Environmental Science-Processes & Impacts,      [PMID:40099488] [10.1039/D5EM00053J]