Lesogaberan hydrochloride AZD-3355 hydrochloride|西域试剂

Lesogaberan hydrochloride AZD-3355 hydrochloride,98.0%

产品编号：Bellancom-10061B| 分子式：C₃H₁₀ClFNO₂P| 分子量：177.54

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货号	价格	库存与货期
Bellancom-10061B	￥4000.00	杭州北京（现货）
Bellancom-10061B	￥6800.00	杭州北京（现货）
Bellancom-10061B	￥13500.00	杭州北京（现货）

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Lesogaberan hydrochloride AZD-3355 hydrochloride

产品介绍

Lesogaberan (AZD-3355) hydrochloride 是一种有效的选择性 GABA_B 受体激动剂，对人重组 GABA_B 受体的 EC₅₀ 为 8.6 nM。通过脑膜中 [³H]GABA 结合位移测量，Lesogaberan hydrochloride 对大鼠 GABA_B 和 GABA_A 受体的亲和力 (K_is)：分别为 5.1 nM 和 1.4 μM。Lesogaberan hydrochloride 通过外周作用模式抑制短暂的食管下括约肌松弛。

生物活性

Lesogaberan (AZD-3355) hydrochloride is a potent and selective GABA_B receptor agonist with an EC₅₀ of 8.6 nM for human recombinant GABA_B receptor. The affinity (K_is) of Lesogaberan hydrochloride for rat GABA_B and GABA_A receptors, as measured by displacement of [³H]GABA binding in brain membranes: 5.1 nM and 1.4 μM, respectively. Lesogaberan hydrochloride inhibits transient lower esophageal sphincter relaxation through a peripheral mode of action.

体外研究

Lesogaberan hydrochloride (3-30 nM) enhances human islet cell proliferation in vitro.

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

Cell Proliferation Assay

Cell Line:	Human islet cells
Concentration:	3, 10, and 30 nM
Incubation Time:	4 days
Result:	Had a small but nonsignificant promitotic effect at 3 nM, while treatment at higher dosages (10 and 30 nM) led to a 2-3-fold increase in proliferation relative to that of islets cultured in medium alone.

体内研究
(In Vivo)

Lesogaberan hydrochloride potently stimulates recombinant human GABA_B receptors and inhibits transient lower esophageal sphincter relaxation (TLESR) in dogs, with a biphasic dose-response curve.
Oral Lesogaberan (0.08 mg/mL; 48 hours) hydrochloride protects human islet β-cells from apoptosis in islet grafts in mice.
Lesogaberan (7 μmol/kg) hydrochloride shows high oral availability (88% in the dog and 100% in the rat) and relatively low systemic clearance in female SpragueDawley rats.

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

Animal Model:	Diabetic NOD/scid mice were implanted with human islets
Dosage:	0.08 mg/mL
Administration:	48 hours
Result:	Significantly reduced the percentages of apoptotic islet cells and increased the frequency of insulin⁺ β-cells in human islet grafts.

Animal Model:	Female Sprague Dawley rats
Dosage:	7 μmol/kg (Pharmacokinetic Analysis)
Administration:	Oral
Result:	High oral availability (88% in the dog and 100% in the rat) and relatively low systemic clearance. Plasma protein binding was 1% in rat and human plasma.

体内研究

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

Animal Model:	Diabetic NOD/scid mice were implanted with human islets
Dosage:	0.08 mg/mL
Administration:	48 hours
Result:	Significantly reduced the percentages of apoptotic islet cells and increased the frequency of insulin⁺ β-cells in human islet grafts.

Animal Model:	Female Sprague Dawley rats
Dosage:	7 μmol/kg (Pharmacokinetic Analysis)
Administration:	Oral
Result:	High oral availability (88% in the dog and 100% in the rat) and relatively low systemic clearance. Plasma protein binding was 1% in rat and human plasma.

体内研究

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

Animal Model:	Diabetic NOD/scid mice were implanted with human islets
Dosage:	0.08 mg/mL
Administration:	48 hours
Result:	Significantly reduced the percentages of apoptotic islet cells and increased the frequency of insulin⁺ β-cells in human islet grafts.

Animal Model:	Female Sprague Dawley rats
Dosage:	7 μmol/kg (Pharmacokinetic Analysis)
Administration:	Oral
Result:	High oral availability (88% in the dog and 100% in the rat) and relatively low systemic clearance. Plasma protein binding was 1% in rat and human plasma.

性状

Viscous liquid

溶解性数据

In Vitro:

DMSO : 240 mg/mL (1351.81 mM; Need ultrasonic)

H₂O : 100 mg/mL (563.25 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	5.6325 mL	28.1627 mL	56.3253 mL
5 mM	1.1265 mL	5.6325 mL	11.2651 mL
10 mM	0.5633 mL	2.8163 mL	5.6325 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 (stored under nitrogen)。-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： PBS
Solubility: 100 mg/mL (563.25 mM); Clear solution; Need ultrasonic
2.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 6 mg/mL (33.80 mM); Clear solution

此方案可获得 ≥ 6 mg/mL (33.80 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 60.0 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
3.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 6 mg/mL (33.80 mM); Clear solution

此方案可获得 ≥ 6 mg/mL (33.80 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 60.0 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
4.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 6 mg/mL (33.80 mM); Clear solution

此方案可获得 ≥ 6 mg/mL (33.80 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 60.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。