2. GPCR/G Protein Neuronal Signaling
  3. Dopamine Receptor
  4. L-745870 hydrochloride

L-745870 hydrochloride 

目录号: HY-14325B 纯度: 99.91%
COA 产品使用指南

摩尔计算器

L-745870 hydrochloride 是一种有效的，选择性的可透过血脑屏障和具有口服活性的多巴胺 D4 受体拮抗剂，Ki 为 0.43 nM，而对 D2 (Ki 为 960 nM) 和 D3 (Ki 为 2300 nM) 受体的亲和力相对较弱，对 5-HT2 受体，sigma 位点和 α-肾上腺素受体表现出中等亲和力。

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L-745870 hydrochloride Chemical Structure

L-745870 hydrochloride Chemical Structure

CAS No. : 1173023-36-3

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥693
In-stock
1 mg ￥400
In-stock
5 mg ￥630
In-stock
10 mg ￥1080
In-stock
50 mg ￥3420
In-stock
100 mg ￥4950
In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

Customer Review

Other Forms of L-745870 hydrochloride:

L-745870 hydrochloride 相关抗体

Top Publications Citing Use of Products

查看 Dopamine Receptor 亚型特异性产品:

查看所有亚型
Dopamine Receptor D1 Receptor D2 Receptor D3 Receptor D4 Receptor D5 Receptor

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

L-745870 hydrochloride is a potent, selective, brain-penetrant and orally active dopamine D4 receptor antagonist with a Ki of 0.43 nM. L-745870 hydrochloride shows weaker affinity for D2 (Ki of 960 nM) and D3 (Ki of 2300 nM) receptors, and exhibits moderate affinity for 5-HT2 receptors, sigma sites and α-adrenoceptors[1][2][3].

IC50 & Target[3]

Human D4 Receptor

4.3 nM (Ki)

D2 Receptor

960 nM (Ki)

D3 Receptor

2300 mM (Ki)

体外研究
(In Vitro)

L-745870 is capable of antagonizing the ability of D4 receptors to inhibit agonist-induced stimulation of [35S]-GTPgS binding; blocking the inhibition of forskolin-stimulated adenylate cyclase activity in transfected human embryonic kidney (HEK293) and Chinese hamster ovary (CHO) cells; blocking dopamine-induced inhibition of Ca2+ currents in transfected GH4C1 pituitary cells; inhibiting D4 activation of cloned G protein-coupled inwardly rectifying K+ channels; and antagonizing dopamine-induced stimulation of extracellular acidification in transfected cells[1].

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

L-745870 hydrochloride 相关抗体:
体内研究
(In Vivo)

L-745870 has good pharmacokinetic properties (20-60% oral bioavailability and plasma t1/2 2.1-2.8 hours) in both rat and monkey, and excellent brain penetration with high brain to plasma ratios in rat[1].
Following oral administration to squirrel monkeys, L745870 (10 mg/kg p.o.) induces mild sedation and extrapyramidal motor symptoms, notably bradykinesia, became apparent at 30 mg/kg. Lower doses of L-745870 has no observable behavioural effects in monkeys[1].

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

363.28

Formula

C18H20Cl2N4
CAS 号
性状

固体

颜色

Light yellow to yellow

运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据
细胞实验： 

DMSO 中的溶解度 : 32.26 mg/mL (88.80 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

0.1 M HCL 中的溶解度 : 25 mg/mL (68.82 mM; 超声助溶; 酸性条件溶解 (HCL 调节，pH≈3))

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.7527 mL 13.7635 mL 27.5270 mL
5 mM 0.5505 mL 2.7527 mL 5.5054 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 (sealed storage, away from moisture)。-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)

质量
=
浓度
×
体积
×
分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

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

g

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: 99.91%

COA (265 KB) LCMS (264 KB)

产品使用指南 (1538 KB)
参考文献

L-745870 hydrochloride 相关分类

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 (sealed storage, away from moisture)。-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。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
0.1 M HCL / DMSO 1 mM 2.7527 mL 13.7635 mL 27.5270 mL 68.8174 mL
5 mM 0.5505 mL 2.7527 mL 5.5054 mL 13.7635 mL
10 mM 0.2753 mL 1.3763 mL 2.7527 mL 6.8817 mL
15 mM 0.1835 mL 0.9176 mL 1.8351 mL 4.5878 mL
20 mM 0.1376 mL 0.6882 mL 1.3763 mL 3.4409 mL
25 mM 0.1101 mL 0.5505 mL 1.1011 mL 2.7527 mL
30 mM 0.0918 mL 0.4588 mL 0.9176 mL 2.2939 mL
40 mM 0.0688 mL 0.3441 mL 0.6882 mL 1.7204 mL
50 mM 0.0551 mL 0.2753 mL 0.5505 mL 1.3763 mL
60 mM 0.0459 mL 0.2294 mL 0.4588 mL 1.1470 mL
DMSO 80 mM 0.0344 mL 0.1720 mL 0.3441 mL 0.8602 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:

L-7458701173023-36-3L745870L 745870Dopamine ReceptorHumandopamineD4receptorbrainpenetrationneurolepticsInhibitorinhibitorinhibit

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