Orvepitant maleate GW823296 maleate|cas:579475-24-4|西域试剂

Orvepitant maleate GW823296 maleate,99.99%

产品编号：Bellancom-122347A| CAS NO：579475-24-4| 分子式：C₃₅H₃₉F₇N₄O₆| 分子量：744.70

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用，

货号	价格	库存与货期
Bellancom-122347A	￥2000.00	杭州北京（现货）
Bellancom-122347A	￥3500.00	杭州北京（现货）
Bellancom-122347A	￥7000.00	杭州北京（现货）
Bellancom-122347A	￥11000.00	杭州北京（现货）
Bellancom-122347A	￥16500.00	杭州北京（现货）

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Orvepitant maleate GW823296 maleate

产品介绍

Orvepitant maleate (GW823296 maleate) 是一种有效，选择性，口服活性且耐受性良好的 neurokinin-1 (NK-1) 受体拮抗剂，对人 neurokinin-1 受体的 pK_i 为 10.2。Orvepitant maleate 可以穿越血脑屏障。Orvepitant maleate 可用于抑郁症和慢性顽固性咳嗽的研究。

生物活性

Orvepitant maleate (GW823296 maleate) is potent, selective, orally active and well-tolerated neurokinin-1 receptor (NK-1) antagonist with a pK_i of 10.2 for human neurokinin-1 receptor. Orvepitant maleate can across the blood-brain barrier. Orvepitant maleate has the potential for depressive disorder and chronic refractory cough (CRC) treatment.

体外研究

Orvepitant (Compound 3a) is further characterized in terms of the ability to functionally inhibit substance P (SP)-induced release of cytosolic Ca²⁺ in human neurokinin-1 receptor (hNK1)-CHO cells. Orvepitant (0.3-10 nM), pre-incubated for 1 h at 37℃ before adding the agonist SP, produces a non-surmountable antagonism of agonist concentration-response curve. For Orvepitant apparents pK_B value of 10.30.

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

体内研究

Orvepitant (Compound 3a; 0.3-10 mg/kg; Oral administration; marmoset) treatment shows a dose dependant reduction of the number of postures was observed at 1 mg/kg (34.9% reduction), 3 mg/kg (36.6% reduction) and 10 mg/kg (46.4% reduction), suggesting a potential anxiolytic-like effect of the compound.
Orvepitant (compound 3a) shows an oral bioavailability (F) of 17% in rat and 55% in dog, plasma clearance (Clp) of 29 mL/min/kg in rat and 6 mL/min/kg in dog and a half-life of 2.3 h in rat and 6.1 h in dog. As far as the brain penetration in rats is concerned, a B/P ratio of 1.2 is observed 5 min after the i.v. administration of a 1 mg/kg dose of Orvepitant.

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

Animal Model:	Human threat test in the marmoset (HTT)
Dosage:	0.3 mg/kg, 1 mg/kg, 3 mg/kg and 10 mg/kg
Administration:	Oral administration
Result:	A dose dependant reduction of the number of postures was observed at 1 mg/kg (34.9% reduction), 3 mg/kg (36.6% reduction) and 10 mg/kg (46.4% reduction).

体内研究

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

Animal Model:	Human threat test in the marmoset (HTT)
Dosage:	0.3 mg/kg, 1 mg/kg, 3 mg/kg and 10 mg/kg
Administration:	Oral administration
Result:	A dose dependant reduction of the number of postures was observed at 1 mg/kg (34.9% reduction), 3 mg/kg (36.6% reduction) and 10 mg/kg (46.4% reduction).

性状

Solid

溶解性数据

In Vitro:

DMSO : 30 mg/mL (40.28 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.3428 mL	6.7141 mL	13.4282 mL
5 mM	0.2686 mL	1.3428 mL	2.6856 mL
10 mM	0.1343 mL	0.6714 mL	1.3428 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: ≥ 5 mg/mL (6.71 mM); Clear solution

此方案可获得 ≥ 5 mg/mL (6.71 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 50.0 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。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 5 mg/mL (6.71 mM); Clear solution

此方案可获得 ≥ 5 mg/mL (6.71 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 50.0 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。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 5 mg/mL (6.71 mM); Clear solution

此方案可获得 ≥ 5 mg/mL (6.71 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 50.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。