JNJ-55511118 - CAS:2036081-86-2

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JNJ-55511118

目录号 : KCM12415 CAS No. : 2036081-86-2 纯度 : ≥98%

Data Sheet 产品使用指南

JNJ-55511118 is a negative modulator of AMPA receptors containing transmembrane AMPA receptor regulatory protein γ8 (TARP-γ8). It inhibits glutamate-induced calcium flux in HEK293F cells co-transfected with TARP-γ8 and either GluA1o, GluA1i, GluA2i, GluA3o, or GluA4o (ICs = 11.22, 12.3, 7.41, 38.02, and 15.85 nM, respectively). JNJ-55511118 is selective for GluA1o receptors containing TARP-γ8 over GluA1o receptors containing TARP-γ2, -γ3, -γ4, or -γ7 (ICs = >10 μM for all). It reduces peak glutamate-induced currents in acutely dissociated murine hippocampal neurons to 60.7% of control cells when used at a concentration of 1 μM. JNJ-55511118 (1 μM) reduces field excitatory postsynaptic potentials (fEPSPs) in the hippocampal CA1 region from wild-type, but not TARP-γ8 knockout, mice. It also inhibits corneal kindling-induced seizures in mice (ED = 3.7 mg/kg).

规格	价格	是否有货	数量
1mg		In-stock
5mg		In-stock
10mg		In-stock
25mg		In-stock

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Other Forms of Rapamycin:

Deudextromethorphan (AVP-786) In-stock
(S)-ATPO In-stock
AMPA receptor antagonist-3 In-stock
Guanylic acid (5'-GMP) In-stock
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生物活性

JNJ-55511118 is a selective TARP γ-8 binding AMPA receptor modulator with oral bioavailability and blood-brain barrier permeability, with a Ki of 26 nM. JNJ-55511118 reduces voluntary intake of sweetened alcohol in male mice. In rodent models, JNJ-55511118 inhibits hippocampal neurotransmission, reduces specific electroencephalogram frequency bands, induces transient hyperlocomotion, impairs learning and memory abilities, and exerts anticonvulsant effects. JNJ-55511118 is applicable to research related to alcohol use disorder and seizures.

体外研究

JNJ-55511118 is a potent and selective negative modulator of AMPA receptors containing TARP-γ8, with an average pIC50 range of 7.42 to 8.33 across human, rat, mouse, monkey, and canine GluA-γ8 combinations, and is inactive against TARP-type or TARP-free AMPA receptors lacking γ8.
JNJ-55511118 (1 μM; 50-60 s) inhibits glutamate-evoked currents in heterologously expressed AMPA receptors containing TARP-γ8 by accelerating desensitization and inactivation processes.
JNJ-55511118 exhibits weak antagonistic activity against the human 5-HT2B receptor (IC50 = 6 μM).

体内研究

JNJ-55511118 (0-10 mg/kg; p.o.; single dose) can significantly reduce multiple indicators of autonomous uptake of sweet wine in male C57BL/6J mice, but does not decrease the parameters related to autonomous consumption of sweet wine in female C57BL/6J mice. However, a dose of 10 mg/kg can alter rod discrimination behavior by increasing the number of responses to ineffective rods.
JNJ-55511118 (i.v./p.o., 0-10 mg/kg, single dose) can inhibit the population spike potential in the hippocampal CA1 region of anesthetized rats. Its intravenous injection ED50 is 0.4 mg/kg, and it can dose dependently reduce cortical EEG power in multiple frequency bands in freely moving rats. Transient hyperkinesia occurs at a dose of 10 mg/kg by gavage.
JNJ-55511118 (p.o.; single dose, 0-40 mg/kg) can produce potent and almost complete seizure protection in corneal and amygdala ignited mouse models, with an oral ED50 of 3.7 mg/kg. It can partially dose dependently produce seizure protection in the 6 Hz psychomotor epilepsy model of Mus musculus, with ED50 values of 18.3 mg/kg p.o. (32 mA) and 6.5 mg/kg p.o. (44 mA), respectively, increasing the seizure threshold of mice to PTZ.

Animal Model:	C57BL/6J (male/female)
Dosage:	1 mg/kg; 10 mg/kg
Administration:	p.o.; single dose
Result:	Reduced alcohol-reinforced response rate from 10 to 60 minutes post-administration compared to vehicle. Reduced total active lever presses, number of alcohol reinforcers earned, and alcohol intake (g/kg/1h) compared to vehicle. Decreased percentage of responses on the active lever from 92.4 (vehicle) to 76.5 ± 5 (1 mg/kg) and 75.7 (10 mg/kg). Increased inactive lever responding at 10 mg/kg dose. Showed no effect on open-field ambulatory distance in alcohol-exposed or sucrose-exposed mice at 1 mg/kg dose. Showed no effect on sucrose-only self-administration parameters. Showed no effect on alcohol-reinforced response rate, total active lever presses, number of alcohol reinforcers earned, or alcohol intake (g/kg/1h). Reduced percentage of responses on the active lever from 92 (vehicle) to 79.9 at 10 mg/kg dose. Increased inactive lever responding at 10 mg/kg dose. Showed no effect on sucrose-only self-administration parameters.

Animal Model:	albino CF1 (male)
Dosage:	0-40 mg/kg
Administration:	p.o.; single dose
Result:	Provided near-complete seizure protection at doses ≥5 mg/kg p.o.: 25/32 animals at these doses had Racine scores of 0, compared to 0/8 vehicle-treated animals. Fitted an ED₅₀ of 3.7 mg/kg p.o. for seizure protection, with an EC₅₀ of 938 ng/mL based on brain concentration. Provided partial seizure protection: at doses ≥10 mg/kg p.o., 12/32 animals were protected in the 32 mA model, and 11/40 animals were protected in the 44 mA model. Fitted an ED50 of 18.3 mg/kg p.o. for the 32 mA model (76% maximum protection, EC50 4644 ng/mL plasma concentration) and 6.5 mg/kg p.o. for the 44 mA model (22% maximum protection, EC50 2533 ng/mL plasma concentration). Significantly increased the PTZ threshold for clonus from 33.3 mg/kg to 49.5 mg/kg. Significantly increased the PTZ threshold for twitch from 30.7 g/kg to 42.4 mg/kg. Protected 11/12 rats from seizure, compared to 1/12 rats protected with vehicle. Significantly reduced mean afterdischarge duration from 92 seconds (vehicle) to 35 seconds.

分子式

C₁₄H₈ClF₃N₂O₂

分子量

328.67

CAS号

2036081-86-2

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

In Vitro:

DMSO : ≥ 100 mg/mL (304.26 mM)

* "≥" means soluble, but saturation unknown

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	3.0426 mL	15.2128 mL	30.4257 mL
5 mM	0.6085 mL	3.0426 mL	6.0851 mL
10 mM	0.3043 mL	1.5213 mL	3.0426 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-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。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： 10% DMSO → 40% PEG300 → 5% Tween-80 → 45% saline

Solubility: ≥ 2.5 mg/mL (7.61 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (7.61 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
2.

请依序添加每种溶剂： 10% DMSO → 90% (20% SBE-β-CD in saline)

Solubility: ≥ 2.5 mg/mL (7.61 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (7.61 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
3.

请依序添加每种溶剂： 10% DMSO → 90% corn oil

Solubility: 2.5 mg/mL (7.61 mM); Suspended solution; Need ultrasonic

此方案可获得 2.5 mg/mL (7.61 mM) 的均匀悬浊液，悬浊液可⽤于⼝服和腹腔注射。

以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。