ML375 (Synonyms: VU0483253)

目录号: HY-12567 纯度: 99.70%: FAQs
Data Sheet SDS COA 产品使用指南

摩尔计算器

ML375 (VU0483253) 是一种有效、高选择性、可透过血脑屏障和具有口服活性的 M5 mAChR 负变构调节剂 (NAM)，对人和大鼠 M5 的 IC₅₀ 分别为 300 nM 和 790 nM。ML375 对人和大鼠的 M1-M4 无活性。

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ML375 Chemical Structure

CAS No. : 1488362-55-5

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可免费申领三个不同产品的试用装。

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规格	价格	是否有货
10 mM * 1 mL in DMSO	￥1089	In-stock
1 mg	￥495	In-stock
5 mg	￥990	In-stock
10 mg	￥1665	In-stock
25 mg	￥3510	In-stock
50 mg	￥5985	In-stock
100 mg		询价
200 mg		询价

or 大包装询价

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(R)-ML375 In-stock

ML375 相关产品

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mAChR1 mAChR2 mAChR3 mAChR4 mAChR5

生物活性
纯度 & 产品资料
参考文献

生物活性

ML375 (VU0483253) is a potent, highly selective, brain-penetrant and orally active M5 mAChR negative allosteric modulator (NAM) with IC₅₀s of 300 nM and 790 nM for human and rat M5, respectively. ML375 is inactive at human and rat M1-M4^[1].

IC₅₀ & Target

mAChR5

细胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
CHO	IC₅₀	> 30 μM Compound: 8, ML375, VU0483253	Negative allosteric modulation of human muscarinic acetylcholine receptor M1 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo-4 AM staining-based fl Negative allosteric modulation of human muscarinic acetylcholine receptor M1 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo-4 AM staining-based fl	[PMID: 24164599]
CHO	IC₅₀	> 30 μM Compound: 8, ML375, VU0483253	Negative allosteric modulation of human muscarinic acetylcholine receptor M2 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo-4 AM staining-based fl Negative allosteric modulation of human muscarinic acetylcholine receptor M2 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo-4 AM staining-based fl	[PMID: 24164599]
CHO	IC₅₀	> 30 μM Compound: 8, ML375, VU0483253	Negative allosteric modulation of human muscarinic acetylcholine receptor M3 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo-4 AM staining-based fl Negative allosteric modulation of human muscarinic acetylcholine receptor M3 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo-4 AM staining-based fl	[PMID: 24164599]
CHO	IC₅₀	> 30 μM Compound: 8, ML375, VU0483253	Negative allosteric modulation of human muscarinic acetylcholine receptor M4 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo-4 AM staining-based fl Negative allosteric modulation of human muscarinic acetylcholine receptor M4 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo-4 AM staining-based fl	[PMID: 24164599]
CHO	IC₅₀	> 30 μM Compound: 8, ML375, VU0483253	Negative allosteric modulation of rat muscarinic acetylcholine receptor M1 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo-4 AM staining-based fluo Negative allosteric modulation of rat muscarinic acetylcholine receptor M1 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo-4 AM staining-based fluo	[PMID: 24164599]
CHO	IC₅₀	> 30 μM Compound: 8, ML375, VU0483253	Negative allosteric modulation of rat muscarinic acetylcholine receptor M2 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo-4 AM staining-based fluo Negative allosteric modulation of rat muscarinic acetylcholine receptor M2 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo-4 AM staining-based fluo	[PMID: 24164599]
CHO	IC₅₀	> 30 μM Compound: 8, ML375, VU0483253	Negative allosteric modulation of rat muscarinic acetylcholine receptor M3 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo-4 AM staining-based fluo Negative allosteric modulation of rat muscarinic acetylcholine receptor M3 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo-4 AM staining-based fluo	[PMID: 24164599]
CHO	IC₅₀	> 30 μM Compound: 8, ML375, VU0483253	Negative allosteric modulation of rat muscarinic acetylcholine receptor M4 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo-4 AM staining-based fluo Negative allosteric modulation of rat muscarinic acetylcholine receptor M4 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo-4 AM staining-based fluo	[PMID: 24164599]
CHO	IC₅₀	300 nM Compound: 8, ML375, VU0483253	Negative allosteric modulation of human muscarinic acetylcholine receptor M5 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo-4 AM staining-based fl Negative allosteric modulation of human muscarinic acetylcholine receptor M5 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo-4 AM staining-based fl	[PMID: 24164599]
CHO	IC₅₀	790 nM Compound: 8, ML375, VU0483253	Negative allosteric modulation of rat muscarinic acetylcholine receptor M5 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo-4 AM staining-based fluo Negative allosteric modulation of rat muscarinic acetylcholine receptor M5 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo-4 AM staining-based fluo	[PMID: 24164599]

体内研究
(In Vivo)

ML375（10-30 mg/kg；腹腔注射；一次）会减弱可卡因的增强作用和相对强度^[2]。
ML375 在啮齿类动物（雄性 Sprague-Dawley 大鼠，1 mg/kg IV，CL_p, 2.5 mL/min/kg，T_1/2, 80 小时）和非人灵长类动物（雄性食蟹猴，1 mg/kg，CL_p，3.0 mL/min/kg，T_1/2，10 小时）^[1]。
向雄性 SD 大鼠给予悬浮剂量后，ML375 还表现出高口服生物利用度 (%F, 80)，最大血浆浓度 (C_max) 为 1.4 μM，相应时间达到 C< sub>max (T_max) 为 7 小时^[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Male Sprague-Dawley rats (70 days old; 260-300 g) injected with cocaine^[2]
Dosage:	10 mg/kg, 30 mg/kg
Administration:	i.p.; once
Result:	Produced dose-related reductions in cocaine self-administration.

分子量

424.83

Formula

C₂₃H₁₅ClF₂N₂O₂

CAS 号

1488362-55-5

性状

固体

颜色

White to off-white

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

细胞实验：

DMSO 中的溶解度 : 40 mg/mL (94.16 mM; 超声加热助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.3539 mL	11.7694 mL	23.5388 mL
5 mM	0.4708 mL	2.3539 mL	4.7078 mL
10 mM	0.2354 mL	1.1769 mL	2.3539 mL

查看完整储备液配制表

* 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。

摩尔计算器
稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

浓度 _(start)

体积 _(start)

浓度 _(final)

体积 _(final)

动物溶解方案计算器

请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

每只动物的给药体积

μL

动物数量

只

由于实验过程有损耗，建议您多配一只动物的量

计算结果

工作液所需浓度 : mg/mL

纯度 & 产品资料

纯度: 99.70%

选择批次：

Data Sheet (620 KB) SDS (252 KB)

COA (298 KB) HNMR (159 KB) RP-HPLC (217 KB) LCMS (370 KB)

产品使用指南 (1538 KB)

参考文献

[1]. Patrick R Gentry, et al. Discovery of the first M5-selective and CNS penetrant negative allosteric modulator (NAM) of a muscarinic acetylcholine receptor: (S)-9b-(4-chlorophenyl)-1-(3,4-difluorobenzoyl)-2,3-dihydro-1H-imidazo[2,1-a]isoindol-5(9bH)-one (ML375). J Med Chem. 2013 Nov 27;56(22):9351-5. [Content Brief]

[2]. Barak W Gunter, et al. Selective inhibition of M 5 muscarinic acetylcholine receptors attenuates cocaine self-administration in rats. Addict Biol. 2018 Sep;23(5):1106-1116. [Content Brief]

ML375 相关分类

Neurological Disease

完整储备液配制表

可选溶剂	浓度溶剂体积质量	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.3539 mL	11.7694 mL	23.5388 mL	58.8471 mL
	5 mM	0.4708 mL	2.3539 mL	4.7078 mL	11.7694 mL
	10 mM	0.2354 mL	1.1769 mL	2.3539 mL	5.8847 mL
	15 mM	0.1569 mL	0.7846 mL	1.5693 mL	3.9231 mL
	20 mM	0.1177 mL	0.5885 mL	1.1769 mL	2.9424 mL
	25 mM	0.0942 mL	0.4708 mL	0.9416 mL	2.3539 mL
	30 mM	0.0785 mL	0.3923 mL	0.7846 mL	1.9616 mL
	40 mM	0.0588 mL	0.2942 mL	0.5885 mL	1.4712 mL
	50 mM	0.0471 mL	0.2354 mL	0.4708 mL	1.1769 mL
	60 mM	0.0392 mL	0.1962 mL	0.3923 mL	0.9808 mL
	80 mM	0.0294 mL	0.1471 mL	0.2942 mL	0.7356 mL

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

ML3751488362-55-5VU0483253ML 375ML-375VU 0483253VU-0483253mAChRMuscarinic acetylcholine receptorM5negativeallostericmodulatorNAMbrain-penetrantInhibitorinhibitorinhibit

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MedChemExpress (MCE) 只为有资质的科研机构、医药企业基于科学研究或药证申报的用途提供医药研发服务，不为任何个人或者非科研性质的、非用于药证申报使用等其他用途提供服务。

站点地图隐私声明

沪ICP备15051369号-4

上海工商

沪公网安备31011502019417

沪(浦)应急管危经许[2021]201709(QFYS)

营业执照（三证合一）

ML375 (Synonyms: VU0483253)

Customer Review

Other Forms of ML375: