MDR-652|cas:1933528-96-1|西域试剂

MDR-652,98.17%

产品编号：Bellancom-136363| CAS NO：1933528-96-1| 分子式：C₂₂H₂₃ClFN₃O₂S| 分子量：447.95

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-136363	￥2000.00	杭州北京（现货）
Bellancom-136363	￥3000.00	杭州北京（现货）
Bellancom-136363	￥8500.00	杭州北京（现货）
Bellancom-136363	￥12500.00	杭州北京（现货）

增值税发票√顺丰快递√订货电话：18601927057

MDR-652

产品介绍

MDR-652 是一种高效的特异性瞬时受体电位香草酸亚型 1 (TRPV1) 配体，具有激动剂活性。对 hTRPV1 和 rTRPV1 的 K_i 分别为 11.4 和 23.8 nM。对 hTRPV1 和 rTRPV1 的 EC₅₀ 分别为 5.05 和 93 nM。MDR-652 可用于缓解疼痛的研究。

生物活性

MDR-652 is a highly specific and efficacious transient receptor potential vanilloid 1 (TRPV1) ligand with agonist activity. The K_is are 11.4 and 23.8 nM for hTRPV1 and rTRPV1, respectively. The EC₅₀s are 5.05 and 93 nM for hTRPV1 and rTRPV1, respectively. Potent topical analgesic activity.

体外研究

体内研究

MDR-652 (0.5 and 5 mg/kg) displays a dose-dependent decrease of body temperature, supporting that MDR-652 displays TRPV1 agonism in the intact animal.
MDR-652 (5-10 mg/kg; i.p. and s.c.) blocks the neuropathic pain completely, indicating 100% maximum possible effect (MPE) .
MDR-652 has a promising topical pharmacokinetic profile.
MDR-652 has no significant toxicity. In a single-dose toxicity study, the LD₅₀ of MDR-652 is higher than 200 and 2000 mg/kg in i.p. and p.o. administration, respectively.

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

Animal Model:	ICR mouse
Dosage:	0.5 and 5 mg/kg
Administration:	Administered intraperitoneally; 7 hours
Result:	Decreased body temperature in a dose-dependent manner.

Animal Model:	Rats with spinal nerve ligation (SNL) model
Dosage:	1, 2, 5, and 10 mg/kg
Administration:	Administered intraperitoneally and subcutaneously; 24 hours
Result:	The i.p. administration exhibited an excellent and dose dependent analgesic profile with an ED₅₀ of 0.5-2 mg/kg. The subcutaneous injection (sc) also displayed an excellent analgesic outcome with maximum effect at 30 min after administration.

体内研究

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

Animal Model:	ICR mouse
Dosage:	0.5 and 5 mg/kg
Administration:	Administered intraperitoneally; 7 hours
Result:	Decreased body temperature in a dose-dependent manner.

Animal Model:	Rats with spinal nerve ligation (SNL) model
Dosage:	1, 2, 5, and 10 mg/kg
Administration:	Administered intraperitoneally and subcutaneously; 24 hours
Result:	The i.p. administration exhibited an excellent and dose dependent analgesic profile with an ED₅₀ of 0.5-2 mg/kg. The subcutaneous injection (sc) also displayed an excellent analgesic outcome with maximum effect at 30 min after administration.

性状

Solid

溶解性数据

In Vitro:

DMSO : 250 mg/mL (558.10 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.2324 mL	11.1620 mL	22.3239 mL
5 mM	0.4465 mL	2.2324 mL	4.4648 mL
10 mM	0.2232 mL	1.1162 mL	2.2324 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: ≥ 6.25 mg/mL (13.95 mM); Clear solution

此方案可获得 ≥ 6.25 mg/mL (13.95 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 62.5 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% corn oil
Solubility: ≥ 6.25 mg/mL (13.95 mM); Clear solution

此方案可获得 ≥ 6.25 mg/mL (13.95 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 62.5 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。