WAY-100635 Maleate

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WAY-100635 Maleate

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

1092679-51-0

包装与价格：

包装	价格(元)
10 mM * 1 mL in DMSO	电议
5mg	电议
10mg	电议
50mg	电议
100mg	电议
200mg	电议
500mg	电议

产品介绍

WAY-100635 maleate 是一种有效且具有选择性的5-hydroxytryptamine 1A (5-HT1A)受体拮抗剂，其IC₅₀值为 0.91 nM，K_i值为 0.39 nM。WAY-100635 maleate 对于5-HT1A和 α1-肾上腺素的pIC₅₀值分别为 8.9 和 6.6。WAY-100635 maleate 也是一种有效的多巴胺D₄受体激动剂。

生物活性

WAY-100635 maleate is a potent and selective5-hydroxytryptamine 1A (5-HT1A) receptorantagonist with anIC₅₀value of 0.91 nM andK_ivalue of 0.39 nM. WAY-100635 maleate haspIC₅₀values for5-HT1Aand α1-adrenergic receptors of 8.9 and 6.6, respectively. WAY-100635 maleate is also a potentdopamineD₄receptoragonist^[1]^[2]^[3].

IC₅₀& Target^[1]

sPLA2

8.87 (pIC₅₀)

sPLA2

9.71 (pA2)

体外研究
(In Vitro)

The functional properties and binding affinities of WAY-100635 are evaluated in HEK 293 cells stably expressing dopamine D_2Lor D_4.4receptors^[1].
WAY-100635 displays 940, 370, and 16 nM binding affinities at D_2L, D₃, and D_4.2receptors, respectively. Saturation analyses demonstrat that theK_dof [³H] WAY-100635 at D_4.2receptors is 2.4 nM. WAY-100635 is potent agonist in HEK-D_4.4cells withEC₅₀of 9.7 nM. WAY-100635 possesses high affinity for D_4.4receptor (3.3 nM)^[1].

体内研究
(In Vivo)

WAY-100635 (1 mg/kg; subcutaneous injection; male Sprague-Dawley rats) treatment abolishes the reduction of the severity of abstinence signs induced by Rhodiola rosea administration in nicotine-dependent rat^[2].

Animal Model:	Male Sprague-Dawley rats (220-240 g)^[2]
Dosage:	1 mg/kg
Administration:	Subcutaneous injection (Pharmacokinetic study)
Result:	Reduced total abstinence score, increased immobility time and the burying behavior was increased.

分子量

538.64

性状

Solid

Formula

C₂₉H₃₈N₄O₆

CAS 号

1092679-51-0

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

In Vitro:

DMSO : ≥ 250 mg/mL(464.13 mM)

H₂O : 25 mg/mL(46.41 mM;Need ultrasonic)

*"≥" 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	1.8565 mL	9.2826 mL	18.5653 mL
5 mM	0.3713 mL	1.8565 mL	3.7131 mL
10 mM	0.1857 mL	0.9283 mL	1.8565 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℃, 6 months; -20℃, 1 month (sealed storage, away from moisture)。-80℃ 储存时，请在 6 个月内使用，-20℃ 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： PBS
Solubility: 25 mg/mL (46.41 mM); Clear solution; Need ultrasonic and warming and heat to 60℃

*以上所有助溶剂都可在本网站选购。